Intracellular targeting of oligonucleotides

Abstract

Delivery constructs, cargo conjugates, pharmaceutical compositions, and their use for the treatment of disease are disclosed.

Description

INTRACELLULAR TARGETING OF OLIGONUCLEOTIDESCROSS-REFERENCE TO RELATED APPLICATIONS

[0001] This application claims the benefit of U. S. Provisional Patent. Application Number 63 / 737,028, filed December 20, 2024; U. S. Provisional Patent Application Number 63 / 758,786, filed February 14, 2025; U. S. Provisional Patent Application Number 63 / 779,909 filed March 28, 2025; and U. S. Provisional Patent Application Number 63 / 859,568 filed August 7, 2025, each of which is incorporated herein by reference in its entirety.SEQUENCE LISTING

[0002] This application contains a Sequence Listing electronically submitted via Patent Center to the United States Patent and Trademark Office as an xml file entitled “0655_000105W001_ST26.xml” having a size of 190,835 bytes and created on December 19, 2025. The information contained in the Sequence Listing is incorporated by reference herein.FIELD

[0003] The present disclosure relates to delivery constructs, and compounds that include a delivery construct.BACKGROUND

[0004] Biologic macromolecules, such as proteins and nucleic acids hold enormous potential as therapeutic agents, especially against targets that are challenging for conventional small molecule drug modalities. However, a major problem in bringing such therapies to the clinic is their limited ability to gain access to the intracellular compartment when administered systemically. Carrier systems, such as polymers, cationic liposomes or chemical modifications, have been used facilitate intracellular delivery of macromolecular therapeutics. Still, intracellular delivery efficiency by these approaches is often low and improved delivery systems to increase efficacy of intracellular delivery have remained elusive.

[0005] The present disclosure addresses this and other issues.SUMMARY

[0006] The present disclosure relates to delivery constructs and cargo conjugates of delivery¬ constructs for delivering a cargo into a cell.

[0007] In embodiments, a compound includes a delivery construct of Formula I(i)Formula I(i)OR2HAAI£-.111 r(AA4^Jw3or a pharmaceutically acceptable salt thereof,where:OR2200i ■s H oral, a2, a3, and a4 are each independently 0 or 1 and at least 1 of a2, a3, and a4 is 1;bl, b2, and b3 are each independently 0 or 1 and at least one of bl, b2, and b3 is 1;LI, 1.2, and L3 are each independently a linker covalently coupling two adjacent motifs;AA1 is an amino acid residue or a peptide that comprises 2 to 10 amino acid residues;AA2, AA3, and AA4 are each independently an amino acid residue or a peptide that comprises 2 to 6 amino acid residues, wherein at least one of AA2, AA3, and AA4 present in the compound comprises a hydrophobic or a hydrophilic amino acid;n is an i teger from 1 to 3;y is an integer from 1 to 5;R1, R2, R3, R4, R5, R6, and R7are each independently the side chain an amino acid.

[0008] In embodiments, a compound includes a delivery construct of Formula 1(A):Formula 1(A):™ H R20-(AA1}~Nor a pharmaceutically acceptable salt thereof,where a3 is 1; and R20, AA1, al, xl, j 1, wl, y, n, R1, R2, R3, R4, R5, R6, R7, x2, j2, and AA3, defined herein.

[0009] In embodiments a compound includes a delivery construct of Formula 1(A) provided that: (a) AA1 comprises a sequence selected from: K(me)-K(rae)-K(me)-R(me)-K(me), RBKKBR, RBRRBR, and YArVRRrGPR;(b) the cCPP is cyclo[Bta-G-Bta-GRGRQ] or cyclo[GfFGrGrQ],(c) AA3 comprises a sequence selected from: Bip-BRBRB, BRB-Bip, BR-Bip-RB. FK, K- Bip, Nal-BRBRB, R-Bta, R-Bta-B, rf, RFB, RFE, R-Nal, and V-Cit;(d) xl is 2 and x2 is 4,(e) xl is 0 and x2 is 2, 4, or 8;(f) AA1 comprises kkkrk and Az\2 comprises R-Bip; or(g) AA1 consists of KKRK and AA2 comprises R-Bip.

[0010] In embodiments, a compound includes a delivery’ construct of Formula 1(A) selected from those listed in Tables 4A-4H.

[0011] In embodiments, a compound includes a delivery construct of Formula 1(A), wherein the delivery construct is covalently attached to a reactive handle M and the compound is of Formula III(A):Formula III(A):wherein ml is 1 and M is a reactive handle,

[0012] In embodiments, a compound of Formula III(A) selected from those listed in Tables 10A-10H. In embodiments of the compounds of Tables 10A-10H, M is the OH of the carboxylic acid of the C -terminal amino acid residue of AA3.

[0013] In embodiments, a compound includes a delivery construct of Formula 1(A), wherein the delivery construct is covalently attached to a cargo or a coupling group (M') and the compound is of Formula V(A):Formula V(A):HR20(AA15H-N (M’l™ cargom*wherein m* is 0 or 1; andM' comprises -NH-,, or a heteroaryl wherein t is an integer from 0 to 10.

[0014] In embodiments, a compound of Formula V(A) selected from those listed in Tables 17A- 17H. In embodiments of the compounds of Tables 17A-17H, m* is 0.

[0015] In embodiments, a compound includes a delivery construct of Formula 1(B):Formula 1(B):or a pharmaceutically acceptable salt thereof,wherein a3 is 1, R40is H or CH3, and R20, AA1, al, xl, j 1, wl, y, n, R1, R2, R, R4, R5, R6, R', x2, j2, AA3, x3, and j3 are defined herein.

[0016] In embodiments a compound includes a delivery construct of Formula 1(B) provided that: (a) AA1 comprises a sequence selected from: KGKRK, KKGRK, KKKGK, kkkrk, KKKRKF, KKKRKR, KKRKG, KKRKK, KKRKK, KKTRK, RBRRBR, RFGRK, TKKRK, and YArVRRrGPR;(b) the cCPP is cyclo[FGFGRrRQ], cyclo[4-Pyr-G-4-Pyr-GRGRQ], cyclofFAFARGRQ], cyclo[AGFGRGRQ], cyclo[F-G(N-me)-FGRGRQ], cyclo[FGAGRGRQ], cyclo[FGF-G(N-me)- RGRQ], cyclo[FGFG-Agp-G-Agp-Q], cyclo[FGFRHRHQ], cyclo[G-f(N-me)-FGrGrQ], cyclo[Gf-Nal-GrGrQ], cyclo[GFRGFRGQ], cyclo[GyYGrGrQ], cyclo[Pcpa-G-Pcpa-GRGRQ], cyclo[Phe(4-CN)-G-Phe(4-CN)GRGRQ],(c) AA3 comprises a sequence selected from: Agp-Bip, Agp-F, Cit-F, EF, FGR, FR, HoAr-Bip, KE, KRKR, Pcpa-F, PKKKRKV, R(me)-F(N-me), R-2-Pyr, R-3-Pyr, R-4-Pyr, R-Bip, R-Bip-R, R-Bta, if R-F(I), RFK, RFRF, RGF, R-Hph, RL, R-Nal, R-Nal-R, RPF, R-Phe(3-CN), R-Phg, RRFF, R-Trp(5-F), R-Tyr(Ph), RW, RY, and SF;(d) AA3 consists ofF orR;(e) xl is 0 or 4;(f) x2 is 8;(g) xl is 2 and x2 is 2, or(h) xl is 2, x2 is 2, and x3 is 2.

[0017] In embodiments, a compound includes a delivery construct of Formula 1(B) selected from those listed in Tables 5A-5E.

[0018] In embodiments, a compound includes a delivery’ construct of Formula 1(B), wherein the delivery construct is covalently attached to a reactive handle M and the compound is of Formula 111(B):Formula III(B):(AA3| k 0 / pf A X3 J QIwherein ml is 1 and M is a reactive handle.

[0019] In embodiments, a compound of Formula III(B) selected from those listed in Tables 11A-11E. In embodiments of the compounds of Tables 11A-11E, M is the OH.

[0020] In embodiments, a compound includes a delivery' construct of Formula 1(B), wherein the delivery construct is covalently attached to a cargo or a coupling group (M') and the compound is of Formula V(B):Formula V(B):H I / A 6wherein m* is 0 or 1; ando-i.\1' comprises -NH-, ', or a heteroaryl wherein t is an integer from 0 to 10.

[0021] In embodiments, a compound of Formula V(B) selected from those listed in Tables ISA- ISE. In embodiments of the compounds of Tables 18A-18E, m* is 0.

[0022] In embodiments, a compound includes a delivery construct of Formula 1(C):Formula 1(C):^28 H (AA1). NV(AA3) aS / 400R4 or a pharmaceutically acceptable salt thereof,wherein a3 and a4 are 1 and R20, AA1, al, xl, j 1, wl, y, n, R1, R2, R3, R4, R5, R6, R7, x2, j2, AA3, x3, j3, and AA4, are defined herein.

[0023] In embodiments a compound includes a delivery construct of Formula 1(C) provided that: AA1 comprises K(me)-K(me)-K(me)-R(me)-K(me), KBKBKBRBK, KKKHH, N(Arg)-B- N(Arg)-N(Arg)-B-N(Arg), N(k)-N(k)-N(k)-N(Arg)-N(k), RBRRBR, RFKKRFK, or YArVRRrGPR;(b) the cCCP is cyclo[GFFGRGRQ], cyclo[GFRGFRGQ], or cyclo[RFGGRFGQ];(c) AA3 comprises Bip, FRF, KR, R-(4-Pyr), rf, RGF, or R-Nal;(d) xlis 0,(e) x2 is 8;(f) x2 is 8 and x3 is 4, or(g) x2 is 2, x3 is 2, x4 is 4 and AA3 comprises Nal.

[0024] In embodiments, a compound includes a delivery construct of Formula 1(C) selected from those listed in Tables 6A-6E.

[0025] In embodiments, a compound includes a delivery' construct of Formula 1(C), wherein the delivery construct is covalently attached to a reactive handle M and the compound is of Formula III(C):Formula III(C):wherein ml is 1 and M is a reactive handle.

[0026] In embodiments, a compound of Formula III(C) selected from those listed in Tables 12A-12E. In embodiments of the compounds of Tables 12A-12E, M is the OH of the carboxylic acid of the C -terminal amino acid residue of AA4.

[0027] In embodiments, a compound includes a delivery construct of Formula (C), wherein the delivery construct is covalently attached to a cargo or a coupling group (NT) and the compound is of Formula V(C):Formula V(C):wherein m* is 0 or 1, andOM' comprises -NH-, is11r11!, or a heteroaryl wherein t is an integer from 0 to 10.

[0028] In embodiments, a compound of Formula V(C) selected from those listed in Tables 19A- 19E. In embodiments of the compounds of Tables 19A-19E, m* is 0.

[0029] In embodiments, a compound includes a delivery construct of Formula 1(D):Formula 1(D):or a pharmaceutically acceptable salt thereof,wherein a2 and a3 are 1 and R20, AA1, al, xl, j 1, wl, y, n, R1, R2, R3, R4, R5, R6, R7, x2, j2, A3, x3, j3, and AA4, are defined herein,

[0030] In embodiments, a compound includes a delivery construct of Formula 1(D), wherein the delivery construct is covalently attached to a reactive handle M and the compound is of Formula 111(D):Formula III(D):wH b, H R«~(AA1)-N< AM X B / / ., X UAA3) l~ — (M)T X f 1AA2^ y WvSlf ’ « 3 h ^1 o Av6t2 o WNHwt / (Hwherein ml is 1 and M is a reactive handle.

[0031] In embodiments, a compound includes a delivery construct of Formula 1(D), wherein the delivery construct is covalently attached to a cargo or a coupling group (M') and the compound is of Formula V(D):Formula V(D):'I HR2CL(AA1) -NJ, (AA3}™™~(M')~~ cargo a1 t'-- 'X2 oFormula D»1wherein m* is 0 or 1; andO•M' comprises -NH-, < H '* -, or a heteroaryl wherein t is an integer from 0 to 10.

[0032] In embodiments, a compound includes a delivery construct of Formula 1(E):Formula 1(E):or a pharmaceutically acceptable salt thereof,wherein a2 is 1 and R20, AA1, al, xl, j 1, wl, y, n, R1, R2, R3, R4, R5, R6, R7, AA2, x2, and j2, are defined herein.

[0033] In embodiments a compound includes a delivery construct of Formula 1(E) provided that: (a) x2 is 2 or 8;(b) AA2 comprises R-Bip; or(c) AA1 comprises KKKRK, cCPP is cyclofFGFGRGRQ], AA2 comprises RF, and x2 is 4.

[0034] In embodiments, a compound includes a delivery' construct of Formula 1(E) selected from those listed in Table 7.

[0035] In embodiments, a compound includes a delivery construct of Formula 1(E), wherein the delivery' construct is covalently attached to a reactive handle M and the compound is of Formula 111(E):Formula III(E):wherein ml is 1 and M is a reactive handle.

[0036] In embodiments, a compound of Formula III(E) is selected from those listed in Table 13. In embodiments of the compounds of Table 13, M is the OH.

[0037] In embodiments, a compound includes a delivery construct of Formula 1(E), wherein the delivery' construct is covalently attached to a cargo or a coupling group (M') and the compound is of Formula V(E):Formula V(E):wherein m* is 0 or 1; andM' comprises -NH-,or a heteroaryl wherein t is an integer from 0 to 10.

[0038] In embodiments, a compound of Formula V(E) selected from those listed in Table 20. In embodiments of the compounds of Table 20, m* is 0.

[0039] In embodiments, a compound includes a delivery construct of Formula 11(F):Formula 11(F):= H / ;.: H 9 / \ ° H R28~(AA1)~tN4 x--.. Lrk i IM x. Ji J- 031 ' Ji - H Uk X(AA4}.^, A.V H OpkfH Y NV"-'" THV' ((AAAA33))'RI,k H *2j2 ° / M h ' r -A Vi Oi x3 o ” ' *4w \l V / NH OY‘ft 0 O R1N HNHo^,NH- N „■>^40' x^-R" R* Nn HN"'° V-NH y Rs>-■< V* oO |^4 or a pharmaceutically acceptable salt thereof,wherein x4 is an integer from I to 14; j4 is integer from 1 to 4; R40is H or CHJ; and R20, AA1, al, xl, jl, wl, y, n, R1, R2, R3, R, R', R6, R7, x2, j2, AA3, x3, J3. AA4, ml, and M are defined herein.

[0040] In embodiments, a compound includes a delivery construct of Formula 11(F) selected from those listed in Table 8.

[0041] In embodiments, a compound includes a delivery construct of Formula 11(F), wherein the delivery construct is covalently attached to a reactive handle M and the compound is of Formula IV(F):Formula IV(F):i H - RZO-~(AA1}-4N J d,, A -Nj,-x Ilk (AA4)xM < AA3) V or <2 x3y p. % R’ HN- o NHR40R2RNHR5ywherein ml is 1 and M is a reactive handle.

[0042] In embodiments, a compound of Formula IV(F) selected from those listed in Table 14. In embodiments of the compounds of Table 14, M is the OH.

[0043] In embodiments, a compound includes a delivery construct of Formula 11(F), wherein the delivery construct is covalently attached to a cargo or a coupling group (M') and the compound is of Formula VI(F):Formula VI(F):. oH,, P H H 0 (AA1J N-,, A, A <.—. W JAA4). A.0.1, ■ A I 'W NA Tbf "(AA3) V 'O / W) -cargo xl 0 *2 )2 ' is ’W H ' 'x4- »>•'O o R1N HR- H OR40„-R2HN OH hUr « R® ( o 6 k4wherein m* is 0 or 1; andoM' comprises -NH-,', or a heteroaryl wherein t is an integer from 0 to 10.

[0044] In embodiments, a compound of Formula VI(F) selected from those listed in Table 21. In embodiments of the compounds of Table 21, m* is 0.

[0045] In embodiments, a compound comprising a delivery construct selected from the delivery constructs shown in FIGS. 4A, 5A, 6A, 7A, 8A, 9A, 10A, 11A, 12A, ISA, 14A, ISA, 16A, 17A, 18A, 19A, 20A, 21 A, 22, 23A, 24A, 25A, and 26A

[0046] In embodiments, a compound selected from a compound shown in FIGS. 4C, 5B, 6B, 7B, 8B, 9B, 10B, 11B, 12B, 13B, 14B, 15B, 16B, 17B, 18B, 19B, 20B, 21B, 22B, 23B, 24B, 25B, and 26B.

[0047] In embodiments, a compound selected from the compounds shown in FIG. 4D, 5C, 6C, 7C, 8C, 9C, 10C, 11C, 12C, 13C, 14C, 15C, 16C, 17C, 18C, 19C, 20C, 21C, 22C, 23C, 24C, 25C, and 26C.

[0048] In embodiments cargo is comprises a therapeutic moiety In embodiments, cargo comprises a polypeptide, a small molecule, an oligonucleotide, one or more components of gene editing machinery, or any combination thereof. In embodiments, cargo comprises an antisense oligonucleotide (ASO). In embodiments, cargo comprises a PMO.

[0049] The present disclosure also provides compositions, such as pharmaceutical compositions that include a compound of the present disclosure.

[0050] The present disclosure also provides a method comprising administering a composition of the present disclosure to a subject.

[0051] BRIEF DESCRIPTION OF THE FIGURES

[0052] FIG. 1 shows modified nucleosides and nucleotides that can be used in antisense oligonucleotides described herein. Structures 1-3 (1 phosphorothioate; 2:=:(Sc5-Rp)-a,]3-CAN; 3 = phosphorodiamidate morpholino (PMO)) are dinucleotides showing phosphate backbone and / or sugar modifications; 4 (2-thio-dT) is a base modification; 5-8 (5 = 2 -OMe-RNA; 6 = 2 O-MOE-RNA; 7 = 2'F-RNA; 8 = 2'F-ANA) are 2' sugar modifications; 9-11 are constrained nucleotides; 12-14 (9 = LNA; 10 = (S)-cET; 11 = tcDNA; 12 = FHNA; 13 = (S)5 '-C-methyl; 14 = UNA) areadditional sugar modification; and 15-18 (15= A- VP; 16 = methyl phosphonate; 17 = 5' phosphorothioate; 18 = (S)-5'-C-methyl with phosphate) are 5' phosphate stabilization modifications; 19 is a morpholino sugar. Reformatted from Khvorova, A., et al., Nat. Biotechnol.2017 Mar; 35(3): 238-248.

[0053] FIG. 2 shows a methylenemorpholine sugar (structure 1) and a three nucleotide phosphorodiamidate morpholino oligomer (structure 2).

[0054] FIG. 3 shows a peptide nucleic acid (PNA).

[0055] FIGS. 4A-4E show the structures of delivery construct 904a (FIG. 4A), and compounds 904b (FIG. 4B), 904c (FIG. 4C), 904d (FIG. 4D), and 904e (FIG. 4E) that include delivery construct 904a.

[0056] FIGS. 5A-4D show the structures of delivery construct 905a (FIG. 4A), and compounds 905b (FIG. SB), 905c (FIG. 5C), and 905d (FIG. 5E) that include delivery construct 905a.

[0057] FIGS. 6A-6D show the structures of delivery construct 906a (FIG. 6A), and compounds 906b ( FIG. 6B), 906c (FIG. 6C), and 906d (FIG. 6E) that include delivery construct 906a

[0058] FIGS. 7A-7D show the structures of delivery construct 907a (FIG. 7A), and compounds 907b (FIG. 7B), 907c (FIG. 7C), and 907d (FIG. 7E) that include delivery construct 907a

[0059] FIGS. 8A-8D show the structures of delivery construct 908a (FIG. 8A), and compounds 908b (FIG. 8B), 908c (FIG. 8C), and 908d (FIG. 8E) that include delivery construct 908a.

[0060] FIGS. 9A-9D show the structures of delivery construct 909a (FIG. 9A), and compounds 909b (FIG. 9B), 909c (FIG. 9C), and 909d (FIG. 9E) that include delivery construct 909a.

[0061] FIGS. 10A-10D show the structures of delivery construct 910a (FIG. 10A), and compounds 910b (FIG. 10B), 910c (FIG. 10C), and 910d (FIG. 10E) that include delivery construct 910a.

[0062] FIGS. 11A-11D show the structures of delivery construct 911a (FIG. 11A), and compounds 911b (FIG. 11B), 911c (FIG. 11C), and 911d (FIG. HE) that include delivery construct 911a.

[0063] FIGS. 12 -12D show the structures of delivery construct 912a (FIG. 12A), and compounds 912b (FIG. 12B), 912c (FIG. 12C). and 912d (FIG. 12E) that include delivery construct 912a.

[0064] FIGS. 13A-13D show the structures of delivery construct 913a (FIG. 13A). and compounds 913b (FIG. 13B), 913c (FIG. 13C), and 913d (FIG. 13E) that include delivery construct 913a.

[0065] FIGS. 1 A-14D show the structures of delivery construct 914a (FIG. 14A), and compounds 914b (FIG. 14B), 914c (FIG. 14C), and 914d (FIG. 14E) that include delivery construct 914a.

[0066] FIGS. 15A-15D show the structures of delivery construct 915a (FIG. ISA), and compounds 915b (FIG. 15B), 915c (FIG. 15C), and 915d (FIG. 15E) that include delivery construct 915a

[0067] FIGS. 16A-16D show the structures of delivery construct 916a (FIG. 1 A), and compounds 916b (FIG. I6B), 916c (FIG. 16C), and 916d (FIG. 16E) that include delivery construct 916a.

[0068] FIGS. 17A-17D show the structures of deliver)- construct 917a (FIG. 17A), and compounds 91 b (FIG. 17B), 917c (FIG. 17C), and 917d (FIG. 17E) that include delivery’ construct 917a.

[0069] FIGS. 18A-18D show the structures of delivery construct 918a (FIG. ISA), and compounds 918b (FIG. 18B), 918c (FIG. 18C), and 918d (FIG. 18E) that include delivery construct 918a

[0070] FIGS. 19A-19D show the structures of delivery construct 919a (FIG. 19A), and compounds 919b (FIG. 19B), 919c (FIG. 19C), and 919d (FIG. I E) that include delivery construct 919a.

[0071] FIGS. 20A-20D show the structures of delivery construct 920a (FIG. 20A), and compounds 920b (FIG. 20B), 920c ( FIG. 20C), and 920d (FIG. 20E) that include delivery construct 920a.

[0072] FIGS. 21A-21D show the structures of delivery construct 921a (FIG. 21 A), and compounds 921b (FIG. 21B), 921c (FIG. 21C), and 921d (FIG. 21E) that include delivery construct 921a

[0073] FIGS. 22A-22D show the structures of delivery construct 922a (FIG. 22A), and compounds 922b (FIG. 22B), 922c (FIG. 22C), and 922d (FIG. 22E) that include delivery construct 922a.

[0074] FIGS. 23A-23D show the structures of delivery construct 923a (FIG. 23A). and compounds 923b (FIG. 23B), 923c (FIG. 23C), and 923d (FIG. 23E) that include delivery construct 923a.

[0075] FIGS. 24A-24D show the structures of delivery construct 924a (FIG. 24A), and compounds 924b (FIG. 24 B), 924c (FIG. 24C), and 924d (FIG. 24E) that include delivery construct 924a.

[0076] FIGS. 25A-25D show the structures of delivery construct 925a (FIG. 25A), and compounds 925b (FIG. 25B), 925c (FIG. 25C), and 925d (FIG. 25E) that include delivery construct 925a

[0077] FIGS. 26A-26D show the structures of delivery construct 926a (FIG. 26A), and compounds 926b (FIG. 26B), 926c (FIG. 26C), and 926d (FIG. 26E) that include delivery construct 926a.

[0078] FIGS. 27A-27C show synthetic schemes for synthesizing the compound Ac-KKKRK-miniPEG2-K(cyclo[FGFG GRQ])-PEGs-R-Bip-PMO. Synthesis includes resin loading and sequence elongation (FIG. 27A), deallylation and cyclization (FIG. 27B), and conjugation of the EEV with the PMO (FIG. 27C).DETAILED DESCRIPTION

[0079] The present disclosure describes delivery constructs, compounds that include a delivery construct, delivery construct-cargo conjugates, compositions containing a compound that includes a delivery construct and / or the delivery construct-cargo conjugate, and methods of administration of the compositions The delivery construct can be conjugated to a variety of cargos designed to elicit a biological response. A compound can include a delivery' construct. A compound can include a delivery construct covalently bonded to reactive handle A delivery construct can be conjugated to a variety of cargos to from a delivery construct-cargo conjugate A cargo of a delivery' construct-cargo conjugate can be designed to elicit a biological responseTheT delivery construct, also called an endosomal escape vehicle (EEV), is designed to facilitate cell penetration and / or endosomal escape. The delivery'- construct includes a cyclic cell penetrating peptide (cCPP) and exocyclic amino acids and / or peptide components.

[0080] An amino acid is a compound of the Rr formu 1la R o o, or O. w,here q is 0 or 1 and R is a side chain that is H or an organic group that has a molecular weight of less than 300 g / mol. An organic group is any motif that comprises carbon and hydrogen atoms, and optionally, one or more nitrogen atoms, sulfur atoms, oxygen atoms, or any combination thereof. When q is 0, the amino acid is an alpha-amino acid since the amino group is attached to the alpha carbon of the carbonyl. When q is 1, the amino acid is a beta-amino acid since the amino group is attached to the beta carbon of the carbonyl. When q is 1, R can be coupled to the alpha carbon of the carbonyl (beta-2-amino acid) or the beta carbon of the carbonyl (beta-3-amino acid). If present, the stereocenter of the amino acid can be L or D. An amino acid may be a natural amino acid or an unnatural amino acid. The term natural amino acid refers to the L- and D-forms of the 20 proteogenic amino acids including arginine, histidine, lysine, aspartic acid, glutamic acid, serine, threonine, asparagine, glutamine, cysteine, glycine, proline, alanine, valine, isoleucine, leucine, methionine, phenylalanine, tyrosine, and tryptophan. The term unnatural amino acid refers to the L- and D-forms of amino acids that include a side chain that is different from the natural amino acids, a side chain that is attached to the amino group of the amino acid, an amino acid having a methyl substituent attached to the alpha or beta carbon in addition to another side chain being attached to the alpha or beta carbon, or any combination thereof. Examples of unnatural amino acids include, but are not limited to, 6-N-methyllysine; 6-N,6-N-dim ethyllysine; 6-N,6-N,6-N-trimethyllysine; citrulline; 3-(2-naphthyl)-alanine; 3-(l-naphthyl)-alanine; 3-(3-benzothienyl)-alanine, tetrahydro-isoquinoline-3-carboxylic acid (Tic); 2-furylalanine; 2-J II,. OHn H2N Y thienylalanine; biphenylalanine; homoarginine;; O; fluorotryptophan (e.g., 5-fluorotryptophan); fluorotyrosine (3 -fluorotyrosine);A AT <A. OH,1 OHH2N'y H2N Y iodophenylalainine; O (2-pyridylalanine; 2-pyridine); & (3- 1*1 f 'CN OHH2N' ' Y°Hpyridylalanine; 3 O-Pyr); (2-pyridylalanine; 4-Pyr); ® (Tyr(Phe)); o. HN;v, NH2NH x“'2fA OHH2N o A oO ni JL(Tyr(Ph));OH(N(Arg)); and ((N(Lys)).

[0081] The terms “amino acid side chain” or “side chain” refer to the characterizing R substituent bound to the alpha-carbon, beta-carbon, or the amino group of an amino acid.

[0082] An amino acid may be incorporated into a larger compound via one or two amide bonds. When covalently coupled to a larger compound by one or two amide bonds, the amino acid may be referred to as an amino acid residue or as an amino acid.

[0083] Amino acids and / or amino acid residues may be referred to using their full name, their conventional three letter abbreviation, or their conventional one letter abbreviation. When using the one letter abbreviation, capital letters indicate L-amino acids or residues, and lower-case letters indicate D-amino acids or residues. For example, arginine may be referred to as Arg, R, or r. Various amino acids and their abbreviations are listed in Table 1.Table I.Amino Acid Abbreviations Abbreviations L-amino acid D-amino acid Alanine Ala (A) ala (a) Arginine Arg (R) arg (r) Asparagine Asn (N) asn (n) Aspartic acid Asp (D) asp (d) Cysteine Cys (C) cys (c) Citrulline Cit citCyclohexylalanine Cha chaAmino Acid Abbreviations Abbreviations L-amino acid D-amino acid 2,3-diaminopropionic acid Dap dap4-fluorophenylalanine 4F-Phe 4F-phe2-furyl alanine 2-FurA 2-fura Glutamic acid Glu (E) glu (e) Glutamine Gin (Q) gin (q) Glycine Gly (G) - N-methylated glycine Gly(N-me) (G(N-me)) - Histidine His (H) his (h) Homoarginine HoArg Hoarg Tsoleucine He (I) ile (i) Leucine Leu (L) leu (1) Lysine Lys (K) lys (k) Methionine Met (M) met (m)3-(2-naphthyl)-alanine Nal, 2-Nal nal, 2-nal, or d2- nal3-(l -naphthyl )-alanine 1-Nal 1-nal Norleucine Nle nle Phenylalanine Phe (F) phe (f)N-methylated phenylalanine Phe(N-me); (F(N-me) phe(N-me); (f(N- me) Phenylglycine Phg phgProline Pro (P) pro (p) Sarcosine Sar sarSerine Ser (S) ser (s) Threonine Thr (T) thr (y) Tyrosine Tyr (Y) tyr (y) Tryptophan Trp (W) trp (w) Tetrahydro-isoquinoline-3-carboxylic acid Tic tic Thienylalanine ThienA thiena Valine Vai (V) val (v)T ert-buty 1 -alani ne Tie tie Penicillamine Pen Pen Homoarginine HomoArg homoarg Methyl-leucine MeLeu meLeu3-(3-benzothienyl)-alanine Bta bta4,4'-Biphenylalanine (biphenylalanine) Bip bip6-N-Methyllysine K(me) k(me)6-N,6-N-Dimethyllysine K(me)s k(me)26-N,6-N,6-N-Dimethyllysine K(me)3 k(me)2N-methyl arginine R(me) r(me) Ornithine Oro oro2-pyridylalanine 2-Pyr 2-pyr3-pyridylalanine 3-Pyr 3-pyrAmino Acid Abbreviations Abbreviations L-amino acid D-amino acid 4-pyridylalanine 4-Pyr 4-pyr Tyr(Ph); Y(Ph) tyr(Ph); y(Ph)Jx ^OHY b0) C Phe(3-CN); F(3-CN) phe(3-CN); f-(3- CN)A, OHH? N Y0CN Phe(4-CN); F(3-CN) phe(4-CN); f-(4- CN) XX A OHH2N Y63-cy anophenylalanine5-Fluorotyrptophan Trp(5-F); W(5F) trp(5-F); w(5F) lodophenylalainine Phe(I), F(1 ) Phe(I), f(I) H2^ Agp agp62-amino~3 -guanid inopropionic acidPara-chlorophenylalanine, 4-chloro- Pepa pepa or dPcpa phenylalanine (Fenclonine)O- J< Y Y 'OHA1A J NHCh2zHomophenylalanine Hph hph or dHph AY OL 1 A.YOHNH2Phenylglycine Phg phg or dPhgAmino Acid Abbreviations Abbreviations L-amino acid D-amino acid k'y Ok L 1y OHNH2HN,, NH-2i"'"0HN.' OHN-(3 -guani di n opropy 1 )gl y cin e, N( A rg),N(R), N(r)MH,Jk’0HN JlOHN-(4-aminobutyl)glvcine, N(Lys), N(K),N(k)

[0084] In embodiments, the amide nitrogen of an amino acid residue in a compound of the present disclosure can be methylated (-CH3). Such amino acid residues can be described as the N-methylated amino acid name or the amino acid shorthand followed by (N-me), me, or (me). For example, a compound of the present disclosure can include N-methylated phenylalanine (F(N-me), f(N-me)), or N-methylated glycine (G(N-me) N-methylated arginine (R(N-me), r(N- me)).

[0085] The cCPP and / or the exocyclic amino acids or exocyclic peptides can include one or more hydrophilic amino acids, one or more hydrophobic amino acids, or both. Amino acids can be grouped as hydrophobic or hydrophilic based on the chemical composition of their side chain.

[0086] Amino acids having a side chain that is charged in an aqueous solution at pH 7.4 are hydrophilic. Such amino acids can be referred to as charged amino acids or charged amino acid residues. Examples of charged amino acids include, but are not limited to, the alpha or betaNHg HN. ^NH2INHA OHH2N y ['■' 9HH.amino acids of histidine; arginine; homoarginine;9 OH; ornithine; 6-N-methylysine; 6-N,6-N-dimethyllysine; 6-N,6-N,6-N- HH 2r'' 9dimethyllysine; lysine;'' 9H ■ aspartic acid; citrulline; ornithine; and glutamic acid.

[0087] Amino acids having an uncharged side chain that comprises an aromatic group are hydrophobic. In some embodiments they are an alpha or beta amino acid. Such amino acids can be referred to as aromatic amino acids or aromatic amino acid residues. Examples of aromatic amino acid include, but are not limited to, the alpha or beta amino acids of phenylalanine; tryptophan; tyrosine; phenylalanine; 3-(2-naphthyl)-alanine; 3-(l-naphthyl)-alanine; 3-(3- benzothienyl)-alanine; tetrahydro-isoquinoline-3-carboxylic acid; 2 -furylalanine; 2 -thienylal; biphenylalanine; iodophenylalanine; fluorotryptophan (e.g.„ 5 -fluorotry ptophan); fluorotyrosineH NA'<'0HM AZOH(3-fluorotyrosine); ® (2-pyridylalanine; 2-pyridine); 9 (3-pyridyl alanine, 3-Pyr); (2 -pyridylalanine; 4-Pyr); (Phe(3-CN,.o.. A f X ~J r £J IX O V, 1 nu, A,, OH, O HX Y X J ii CN)); O (Phe(4-CN)); (Tyr(Ph)); OH ■ para-chlorophenylalanine; homophenylalanine; and phenylglycine.

[0088] Amino acids having a hydrocarbon side chain that is not charged and does not include an aromatic group are hydrophobic. Such amino acids can be referred to as uncharged, not aromatic, hydrocarbon amino acids or residues. Examples of uncharged, not aromatic, hydrocarbon amino acids include, but are not limited to, glycine, proline, and the alpha or beta amino acids of alanine, valine, leucine, and isoleucine.

[0089] Amino acids that have an uncharged side chain that does not include an aromatic group and has a ratio of carbon atoms to heteroatoms of 1.5:1 or less are hydrophilic. Examples of such amino acids include, but are not limited to, the alpha or beta amino acids of serine, threonine, asparagine, and glutamine.

[0090] Amino acids that have an uncharged side chain that does not include an aromatic group and has a ratio of carbon atoms to heteroatoms of greater than 1.5:1 are hydrophilic.Delivery constructs

[0091] The present disclosure describes compounds that include a delivery construct. A delivery construct can be covalently attached to any suitable atom, moiety, or component.

[0092] In embodiments a delivery construct is covalently attached to a reactive handle (M), a bonding group (M'), a cargo, or a cargo through a bonding group (Mr). M, M', and cargo are defined herein.

[0093] In embodiments, a delivery construct covalently attached a reactive handle (M). A reactive handle can be used to covalently couple a delivery construct to another compound. For example, a reactive handle can be used to covalently couple a delivery construct to a cargo.

[0094] In embodiments, a delivery construct is covalently attached to bonding group (M'). A bonding group (M') can link the delivery' construct to another molecule. In embodiments, a delivery' construct is covalently attached to a cargo through a bonding group (M’). In embodiments, a delivery' construct is covalently attached directly to a cargo.

[0095] In embodiments, a compound includes a delivery construct of Formula I:Formula I:or a pharmaceutically acceptable salt thereof,where:OJbR20is H or / al, a2, a3, and a4 are each independently 0 or 1 and at least 1 of a2, a3, and a4 is 1;bl, b2, and b3 are each independently 0 or 1 and at least one of bl, b2, and b3 is 1;LI, L2, and L3 are each independently a linker covalently coupling two adjacent motifs, AA1 is an amino acid residue or a peptide that comprises 2 to 10 amino acid residues;AA2, AA3, and AA4 are each independently an amino acid residue or a peptide that comprises 2 to 6 amino acid residues, wherein at least one of AA2, AA3, and AA4 present in the compound comprises a hydrophobic or a hydrophilic amino acid;n is an integer from 1 to 3;y is an integer from 1 to 5,R1, R2, R3, R4, R5, Rfa, and R7are each independently the side chain an amino acid.

[0096] In embodiments, a compound includes a delivery construct of Formula II:Formula II:or a pharmaceutically acceptable salt thereof,where:OR20isH or'l",al 0 or 1;bl is 0 or 1;LI, L2, L3, and L4 are each independently a linker covalently coupling two adjacent motifs, AA1 is an amino acid residue or a peptide comprising 2 to 10 amino acid residues;AA3 and AA4 are each independently an amino acid residue or a peptide that includes 2 to 6 amino acid residues, wherein at least one of AA3 and AA4 includes a hydrophobic or a hydrophilic amino acid;n is an integer from 1 to 3;y is an integer from 1 to 5; and

[0097] R1, R2, R3, R4, Ry R6, and R7are each independently the side chain an amino acid The variables (R20, al, a2, a3, a4, bl, b2, b3, LI, L2, L3, L4, AA1, AA2, AA3, AA4, n, y, R1, R2, R3, R", R5, R6, and R7) in Formula I and Formula II can have any identity described herein for the respective variable.[009S] In embodiments, a delivery construct of Formula I or Formula II can be covalently attached to OH, M, cargo, or the M' of M'-cargo at the point of attachment bond wherein M is a reactive handle described herein, M' is a bonding group described herein, and cargo is a cargo described herein In embodiments, a delivery construct of Formula I or Formula II is covalently- attached to M. In embodiments, a delivery construct of Formula I or Formula II is covalently attached to the M' of M'-cargo. In embodiments, a delivery construct of Formula I or Formula II is covalently attached to cargo. In embodiments, M is OH

[0099] In embodiments, when a delivery construct of Formula I or Formula II is covalently attached to a PMO cargo, the delivery construct is covalently bonded to the 3’ end of the PMO. In embodiments, when a delivery construct of Formula I or Formula II is covalently attached to the 3' end of a PMO cargo, the delivery construct is covalently attached to the morpholino nitrogen of the 3' end of the PMO.

[0100] FIGS. 4A-4E show' an example of compounds that include a delivery construct of Formula I (4A), where the delivery construct is covalently attached to M (FIG. 4B, where ml is 1), covalently attached to OH (FIG, 4C), covalently attached to a cargo through M' (when m* is 1) or covalently attached to a cargo (FIG. 4D), and covalently attached to the morpholino nitrogen of the 3' end of a PMO cargo.

[0101] The delivery constructs of Formula I and Formula II comprises a cyclic cell penetrating peptide (cCPP). The cCPP comprises the amino acid residues characterized by R1, R2, R3, R4, R5, R6, and R7. The amino acid residues or peptides of AA1, AA3, and AA4 (if present) are exocyclic amino acids residues or peptides. cCPP notation is described herein.

[0102] Examples of delivery constructs of Formula I include those listed in Tables 2A-2C and examples of compounds of Formula II include those listed in Table 2D. In Tables 2A-2D, the _terminal indicates; Ac is -C(O)CH3; the cCPP is written as JA(cyclo[XAXBXcXDXEXFXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acidresidues with the side chain R1, R2, R\ R4, R5, R6, and R7, respectively, YAis the cCPP bridging amino acid residue, and JAis the bridging exocyclic amino acid residue (see, for example, the cCPP description herein); “miniPEGf’ indicates -(CH2-CH2-O)2-CH2-CO-; and “PEG#” indicates -(CH2-CH2-O)#-CH2-CO- or -(CH2-CH2-O)#-CH2-CH2-CO- where # indicates to the number of -CH2-CH2-O- units. In embodiments of the delivery' constructs of Tables 2A-2C, each instance of “PEG2” refers to -(CH2-CH2-O)2-CH2-CO- (i.e., “miniPEG2”) and each instance of “PEG#” refers to (CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2. In embodiments, each instance of “PEG?” refers to ~(CH2-CH2-O)2-CH -CH2-CO- and each instance of “PEG#” refers to -(CH2-CH2-O -CH2-CH2-CO- where # is an integer greater than 2. Table 2A.SEQ IDNo. Delivery ConstructNOs: Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ]> PEGi2-Bip-BRBRB- 18, 40, KI(z\c-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-Bip-BRBRB-) 35 Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ]> PEGi2-Nal-BRBRB- 18, 40, K2(Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal-BRBRB-) 36 Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-B- K3 18, 40 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bta-B-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BRB-Bip- 13, 40, K4(Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-BRB-Bip-) 29 Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ]> PEGi2-BR-Bip-RB- 18, 40, K5(Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-BR-Bip-RB-) 85 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-B- K6 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-B-)Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEGs-RF- K7 18, 38 (Ac-PKKKRKV-miniPEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-RF-)Ac-KKKRK-PEG2-K(cyclo[GfFGrGrQ])-PEG8-RF- K8 13, 44 (Ac-KKKRK-miniPEG2-K(cyclo[GfFGrGrQ])-PEG8-RF-)Ac-kkkRK-PEG2-K(cyclo[GffGrGrQ])-PEG8-RF- K9 11, 44 (Ac-kkkRK-miniPEG2-K(cyclo[GfFGrGrQ])-PEG8-RF-)Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8- K10 18, 38 (Ac-PKKKRKV-miniPEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-)Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEGs-K-Bip- KU 20, 40 (Ac-RBRRBR-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-K-Bip-)Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF- KI 2 12, 40(Ac-kkkrk-miniPEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-)SEQ I D No. Delivery ConstructNOs:Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal- K13 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-rf- KI 4 13, 40 (Ac-K. KKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PECh-rf-)KI 5 Ac-RBKKBR-K(cyclo[FGFGRGRQ])-PEG8-R-Bip- 80, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FK- KI 6 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-FK-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bta- KI 7 13, 40 (Ac-KKKRK-miiiiPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-)Ac-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])- PEGs-RF- KI 8 14, 40 (Ac-K(me)-K(me)-K(me)-R(me)-K(me)-miniPEG2- K(cyclo|FGFGRGRQ|)-PEG8-RF-)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Val-Cit- KI 9 18, 40 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-Val-Cit-)Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF- K20 21, 40 (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-)K21 Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEGs-Bip- 20, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-PEG2- K22 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-PEG2-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG2- K23 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-R-Bta- 13, 40 miniPEG2-)Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG2-KF-PEGi- K24 20, 40 (Ac-RBRRBR-K(cyclo[FGFGRGRQ])-miniPEG2-KF-PEG4-)Ac-KKKRK-PEG2-K(cyclo[FGFRHRHQ])-PEG2-RF-PEG4- K25 13, 42 (Ac-KKKRK-miniPEG2-K(cyclo[FGFRHRHQ])-miniPEG2-RF-PEG4-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bta-PEG2- K26 13, 40 (Ac-KK. KRK-miniPEG2-K(cyclo[FGFGRGRQ)-PEG4-R-Bta-miniPEG2-)Ac-YArVRRrGPR-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4- K27 (Ac-YArV7RRrGPR-miniPEG2-K(cyclo[FfFGRGRQ])-miniPEG2-RF- 21, 39 PEG4-)Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEG8- K28 40, 18 (Ac-K(cyclo[FGFGRGRQ])-miniPEG2-PKKKRKV-PEG8-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-Bip- K29 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-rf-PEG4-Bip- 13, 40) _ _SEQ I D No. Delivery ConstructNOs: Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-F- K30 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PECj4- 18, 40 F-)Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bta- K31 (Ac-RBRRBR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 20, 40 Bta-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Nal- K32 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 13, 40 Nal-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG₈-RF-PEG4-Nal- K33 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG«-RF-PEG4-Nal-)Ac-PKKKRKV-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG2-Nal- K34 (Ac-PKKKRKV-miniPEG2-K(cyclo[FfFGRGRQ])-miniPEG2-RF- 18, 39 miniPEG2-Nal~)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-Bip- K35 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-KF-PEG4- 13, 40 Bip-)Ac-KKKRK-PEG2-K(cyclo[FfFGRGRQ])-PEGi2-(2-Nal)-PEG2-(2-Nal)- K36 (Ac-KKKRK-miniPEG2-K(cyclo[FfFGRGRQ])-PEGi2-(2-Nal)- 13, 39 miniPEG2-(2-Nal)-)Ac-KKKRK-PEG2-K(cyclo[FfFGRGRQ])-PEGi2-Bip-PEG2-Bip- K37 (Ac-KKKRK-miniPEG2-K(cyclo[FfFGRGRQ])-PEGi2-Bip-miniPEG2- 13, 39 Bip-)Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEGi2-Nal-PEG2-Nal- K38 20, 39 (Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEGi2-Na!-niiniPEG2-Nal-)Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-PEG2-Nal- K39 20, 40 (Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-niiniPEG2-Nal-)K40 Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bip- 1, 40 K41 Ac-kkkrk-PEG2-K(cycjo[FGFGRGRQ])-PEGs-R-Bip- 12, 40 K42 Ac-KKKRK-PECh-K(cyclo[FGFGRGRQ])-PEG2-RF- 13, 40 K43 Ac-TKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 9, 40 K44 Ac-KKTRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 8, 40 K45 Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG4- 21, 40 K46 Ac-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ]> PEG2-RG-PEG4- 13, 55 K47 Ac-KKKRK-PEG2-K(cyclo[G-f(N-nie)-FGrGrQ])-PEG2-RF-PEG4- 13, 55 K48 Ac-KKKRK-PEG2-K(cyclo[Gf-Nal-GrGrQ])-PEG2-RF-PEG4- 13, 56 K49 Ac-KKKRK-PEG2-K(cyclo[GyYGrGrQ])-PEG2-RF-PEG4- 13, 58 K50 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-PEG4- 13, 40 K51 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG2- 13, 40K52 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip- 13, 40SEQ I D No. Delivery ConstructNOs: K53 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-PEG4- 13, 40 K54 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFR-PEG4- 13, 40 K55 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-R-PEG4- 13, 40 K56 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-R-PEG4- 13, 40 K57 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4- 13, 40 K58 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG8- 13, 40 K59 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4- 13, 40 K60 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(3-Pyr)-PEG4- 13, 40 K61 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(2-Pyr)-PEG4- 13, 40 K62 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(4-Pyr)-PEG4- 13, 40 K63 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phe(3-CN)-PEG4- 13, 40 K64 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Trp(5-F)-PEG4- 13, 40 K65 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Tyr(Ph)-PEG4- 13, 40 K66 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-HoArg-Bip-PEG4- 13, 40 K67 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-rf-PEG4- 13, 40 K68 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R(me)-F(N-me)-PEG4- 13, 40 K69 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-(4-Pyr)-PEG4-Nal- 13, 40 K70 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4-F- 13, 40 Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-RF- K71 13, 46 PEG4- Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-R-Bip- K72 13, 46 PEG4- K73 Ac-KKKRK-PEG4-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 13, 40 K74 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG4- 13, 4013, 40, K75 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFRF-PEG4- 33 13, 40, K76 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RRFF-PEG4- 86 K77 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4- 40 K78 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KFKF-PEG4- 40, 32 K79 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-EF-PEG4- 13, 40 K80 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-PEG4- 13, 40 K81 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FGR-PEG4- 13, 40 Ac-KKKRK-PEG2-K(cyclo[Phe(4-CN)-G-Phe(4-CN)-GRGRQ])-PEG2- K82 13, 59 RF-PEGs- K83 Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-K-PEG4- 1, 40 K84 Ac-KKRK-PEG2-K(cyclo[FGFGRrRQ])-PEG2-RF-PEG4- 1, 53 K85 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ]-PEG2-RF(I)-PEG4- 13, 40K86 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FR-PEG4- 13, 40SEQ ID No. Delivery ConstructNOs: K87 Ac-KKKRKR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-F-PEG4- 17, 40 K88 Ac-KKKRKF-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG4- 16, 40 K89 Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4- 13, 57 K90 Ac-KKKRK-PEG2-K(cyclo[FFGRRGQ])-PEG2-RF-PEG4- 13, 49 K91 Ac-KGKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 3, 40 K92 Ac-KKGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 4, 40 K93 Ac-KKKGK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 5, 40 K94 Ac-KKRKG-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 6, 40 K95 Ac-KKRKK-PEG2-K(cyclo[FGFG-Cit-GRQ])-PEG2-RF-PEG4- 7, 51 K96 Ac-KKRKK-PEG2-K(cyclo[FGFGRG-Cit-Q])-PEG2-RF-PEG4- 7, 52 K97 Ac-KKRKK-PEG2-K(cyclo[AGFGRGRQ])-PEG2-RF-PEG4- 7, 47 K98 Ac-KKRKK-PEG2-K(cyclo[FGAGRGRQ])-PEG2-RF-PEG4- 7, 50 K99 Ac-KKKGK-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4- 5, 39 KI 00 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-SF-PEG4- 13, 40 K101 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RL-PEG4- 13, 40 KI 02 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RY-PEG4- 13, 40 KI 03 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PFG2-RW-PEG4- 13, 40 KI 04 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Cit-F-PEG4- 13, 40 KI 05 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-Bip- 13, 40 KI 06 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-R-Bip-PEG8- 13, 40 KI 07 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG4- 13, 40 KI 08 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG2- 13, 40 KI 09 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RPF-PEG4- 13, 40 KI 10 Ac-KKKRK-PEG2-K(cyclo[FGF-G(N-me)-RGRQ])-PEG2-RPF-PEG4- 13, 60 Kill Ac-KKKRK-PEG2-K(cyclo[F-G(N-me)-FGRGRQ])-PEG2-RPF-PEG4- 13, 61 KI 12 Ac-KKKRK-PEG2-K(cyclo[FAFARGRQ])-PEG2-RF-PEG4- 13, 62 KI 13 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-Bip-PEG4- 13, 40 KI 14 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-F-PEG4- 13, 40KI 15 Ac-KKKRK-PEG2-K(cyclo[FGFG-Agp-G-Agp-Q])-PEG2-RF-PEG4- 13, 63 Table 2B.SEQ IDNo. Delivery ConstructNOs: K116 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4- 13, 40 K117 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQl)-PEG4-RF-PEG2- 13, 40 KI 18 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQl)-PEG2-R-Phg-PEG4- 13, 40 K119 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQl)-PEG2-RFE- 13, 40 KI 20 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Hph-PEG4- 13, 40K121 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Pcpa-F-PEG4- 13, 40SEQ ID No. Delivery ConstructNOs: KI 22 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4- 13, 40 KI 23 Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQT)-PEG2-RF-PEG4- 12, 40 K124 Ac-KKKRK-PEG2-K(cyclorPcpa-G-Pcpa-GRGRQ])-PECh-RF-PEG4- 13, 64K125 Ac-RFGRK-PEG2-K(cyclo[FGFGRGRQ|)-PEG4-RF-PEG4- 22, 40 Table 2C.SEQ IDNo. Delivery ConstructNOs:Ac-KKKHH-PEG2-K(cyclo[FGFGRGRQl)-PEG2-RF-PEG4-Bip- KI 26 (Ac-KKKHH-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 15, 40 Bip-)Ac-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])- PEG2-RF-PEG4-Bip- Ki 27 14, 40 (Ac-K(me)-K(nie)-K(me)-R(me)-K(nie)-miniPEG2- K(cyclo[FGFGRGRQ])-mimPEG2-RF-PEG4-Bip-)Ac-KBKBKBRBK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- KI 28 (Ac-KBKBKBRBK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 23, 40 PEG4-Bip-)Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-Bip- KI 29 (Ac-KKKRK-miniPEG2-K(cyclo[GFRGFRGQ])-miniPEG2-RF-PEG4- 13, 57 Bip-)Ac-KKKRK-PEG2-K(cyclo[GRFGRFGQ])-PEG2-RF-PEG4-Bip- K130 ( Ac-KKKRK-mini PEG2-K(cyclo[GRFGRFGQ] )-miniPEG2-RF-PEG4- 13, 66 Bip-)Ac-RFKKRFK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- K131 (Ac-RFKKRFK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 24, 40 Bip-)Ac-YArVRRi-GPR-PECn-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- KI 32 (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 24, 40 PEG4-)Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- KI 33 (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 21, 40 PEGj-Bip-)Ac-KKKRK-PEG2-K(cyclo[RFGGRFGQ])-PEG2-RF-PEG4-Bip- KI 34 (Ac-KKKRK-miniPEG2-K(cyclo[RFGGRFGQ])-miniPEG2-RF-PEG4- 13, 67 Bip-)Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-PEG2-K(cyclo[FGFGRGRQ])- PEG2-RF-PEG4-Bip- K135 25, 40 (Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-miniPEG2- K(cvclo[FGFGRGRQl)-miniPEG2-RF'-PECi4-Bip-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- KI 36 (Ac-KKKRK-miniPEG2-K(cvclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 13, 40W) _ ' _SEQ ID No. Delivery ConstructNOs: Ac-(N(Arg))-B-(N(Arg))-(N(Arg))-B-(N(Arg))-K(cyclo[FGFGRGRQ])- PEG2-RF-PEG4-Bip- KI 37 26, 40 (Ac-(N(Arg))-B-(N(Arg))-(N(Arg))-B-(N(Arg))-K(cyclo[FGFGRGRQ])- miniPEG2-RF-PEG4-Bip-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FRF-PEG4-Bip- KI 38 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-FRF-PEG4- 13, 40 Bip-)Ac-KKKRK-PEG2-K(cyclo[GFFGRGRQ])-PEG2-RF-PEG4-Bip- KI 39 (Ac-KKKRK-miniPEG2-K(cvclo[GFFGRGRQ])-miniPEG2-RF-PEG4- 13, 65liPj _; _Table 2D.SEQ IDNo. Delivery ConstructNOs: KI 40 Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEGs-RF-PEG4- 40, 18 KI 41 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG2-F-PEG4- 40, 18KI 42 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-PEG4- 13, 40

[0103] The constructs disclosed are organized to illustrate a progressive structural hierarchy. Tables 2A-2D show delivery constructs with a terminal which signifies a point ofattachment bond “I ” in which the construct can be attached to any moiety or substituent, including, but not limited to, a reactive handle (M), a coupling group (M'), a cargo, or other chemical entity. Tables 9A-9D show a delivery construct covalently attached to a reactive handle (M). The reactive handle can be used to conjugate the compound to any moiety or substituent, including, but not limited to, a cargo or other chemical entity Tables 15A-15D show compounds that include a delivery construct conjugated to a cargo (also called cargo¬ conjugates) either directly (when m* is 0) or through a bonding group (AT) (when m* is 1). Tables 16A-16D show compounds that include a delivery construct conjugated to a PMO cargo. Table 3.Delivery construct with terminal indicating a Constructs begin with point of attachment bondTables 2A-2Dthe letter “K”Constructs begin with Delivery construct covalently attached to Tables 9. A-9Dthe letter “L” reactive handle (Al)Constructs begin with Delivery construct covalently attached attached Tables 15A-15Dthe letter “M” to a cargo via coupling group M' Constructs begin withTables 16A-16D Delivery construct attached to a PMO cargothe letter “NT

[0104] It is understood that when SEQ ID NO(S) are listed after a compound, the SEQ ID NO(S) appear in the order (from left to right) in which they appear in the compound (from left to right). For example, Ac-KKKRK-PEG2-K(cyclo[GFFGRGRQ])-PEG2-RF-PEG4-Bip-M- includes SEQ ID NOS: 13 and 65 and can be thought of as, for example, Ac-KKKRK(SEQ ID NO:13)-PEG2-K(cyclo[GFFGRGRQ(SEQ ID NO:65)])-PEG2-RF-PEG4- or Ac-(SEQ ID NO: 13)-PEG2- K(cyclo[SEQ ID NO:65])-PEG2-RF-PEG4-.

[0105] In embodiments, a compound comprises a delivery construct selected from K7, K8, or K9, wherein “PEG2” is (CH2-CH2-O)2-CH2-CH2-CO.

[0106] In embodiments, a compound including a delivery' construct can be Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8 (SEQ ID NOS: 18, 38), wherein PEGz is -(CH2-CH2-O)2-CH2-CH2-CO- or ~(CH2-CH2-O)2-CH2-CO-, and PEG8 is -(CH2-CH2-O)8-CH2-C(O)- or - (CH2-CH2-O)8-CH2-CH2-CO-.

[0107] FIGS. 4A, 5A, 6A, 7A, 8A, 9A, 10A, 11A, 12A, 13A, 14A, 15A, 16A, 17A, 18A, 19A, 20A, 21A, 22A, 23A, 24A, 25A, and 26A show the structures of delivery constructs 904a, 905a, 906a, 907a, 908a, 909a, 910a, 911a, 912a, 913a, 914a, 914a, 915a, 916a, 917a, 918a, 919a, 920a, 921a, 922a, 923a, 924a, 925a, and 926a.

[0108] Delivery construct 904a (FIG. 4A) is Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-PEG2-Nal- (e.g., see K39 in Table 2A, see also Cll(a) in Table 6D), wherein PEG4 is -(CH2-CH2-O)-CH2-CH2-CO- and PEG2 is -(CH2-CH2-O)-CH2-C(O)-.

[0109] Delivery construct 905a (FIG. 5A) is Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG8-Bip-(e.g, see K21 in Table 2A, see also A17(a) in Table 4C), wherein PEG8 is -(CH2-CH2-O)8-CH2-CH2-CO-.

[0110] Delivery' construct 906a (FIG. 6A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2- RF-PEG4-Nal- (e.g., see K32 in Table 2A, see also C2(a) in Table 6A), wherein PEG2 is -(CH2- CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-.

[0111] Delivery construct 907a (FIG. 7A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs- RF-PEG4-Nal- (e.g., see K33 in Table 2A, see also 03(a) in Table 6A), wherein PEG2 is -(CH2-CH2-O)-CH2-CO-, PEG8 is -(CH2-CH2-O)8-CH2-CH2-C(O)-, and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)- [01121 Delivery construct 908a (FIG. 8A) is Ac-PKKKRKV-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG2-Nal- (e g., see K34 in Table 2A, see also C6(a) in Table 6C), wherein PEG2is (CH2-CH2-O)2-CH2-CO-.

[0113] Delivery' construct 909a (FIG. 9A) is Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-F- (e.g., see K30 in Table 2A, see also C5(a) in Table 6B), wherein PEG2 is - (CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-.

[0114] Delivery construct 910a (FIG. 10A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])- PEG4-R-Bta-PEG2- (e.g., see K26 in Table 2A, see also B4(a) in Table 5A), wherein PEG2 is - (CH2-CH2-O)2-CH22-CO- and PEG4 is -(CH2-CH22-O)4-CFI2-CH2-C(O)-.

[0115] Delivery construct 911a (FIG. 11A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])- PEG2-rf-PEG4-Bip- (e.g., see K29 in Table 2A, see also Cl(a) in Table 6A), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-.

[0116] Compound 912a (FIG. 12A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFRF-PEG4- (e.g., see K75 in Table 2A, see also B38(a) in Table 5C), wherein PEG2 is -(CH2-CFI2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-.

[0117] Delivery construct 913a (FIG. 13A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFR-PEG4- (e.g., see K54 in Table 2A, see also B18(a) in Table 5C), wherein PEG2 is - (CH2-CH2-O)2-CH2-CO- and PEG4 is -(CH2-CF{2-O)4-CH2-CH2-C(O)-.

[0118] Delivery' construct 914a (FIG. 14A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])- PEG2-R-Tyr(Ph)-PEG4- (e.g., see K65 in Table 2A, see also B29(a) in Table 5C), wherein PEG2 is (CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-.

[0119] Delivery' construct 915a (FIG. 15A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-F-PEG4- (e.g., see K114 in Table 2A, see also B74(a) in Table 5C), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is ~(CH2-CH2-O)4-CH2-CH2-C(O)-.

[0120] Delivery construct 916a (FIG. 16A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4- (e.g., see K77 in Table 2A, see also B41(a) in Table 6A), wherein PEG2 is - (CH2-CH2-O)2-CH2-CO-.

[0121] Delivery construct 917a (FIG. 17A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG2- (e.g., see K51 in Table 2A, see also B16(a) in Table 5C), wherein PEG2 is - (CH2-CH2-O)2-CH2-CO-.

[0122] Delivery construct 918a (FIG. ISA) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])- PEG4-RF-PEG4- (e.g., see K116 in Table 2B, see also B76(a) in Table 5D), wherein PEG2 is - (CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-.

[0123] Delivery construct 919a (FIG. 19A) is Ac-KKKRKR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-F-PEG4- (e.g., see K87 in Table 2A, see also B51(a) in Table 5C), wherein PEG2 is ~ (CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-

[0124] Delivery construct 920a (FIG. 20A) is Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4- (e.g., see K89 in Table 2A, see also B53(a) in Table 5C), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-.

[0125] Delivery construct 921a (FIG. 21A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])- PEGs-R-Nal-PEG4- (e.g., see K57 in Table 2A, see also B21(a) in Table 5C), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO-, PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-, and PEG8 is -(CH2-CH2-O)8-CH2-CH2-C(O)-.

[0126] Delivery construct 922a (FIG. 22A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RPF-PEG4- (e.g., see K109 in Table 2A, see also B69(a) in Table 5C), wherein PEG2 is - (CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-.

[0127] Delivery construct 923a (FIG. 23A) is Ac-KKKRKF-PEG2-K(cyclo[FGFGRGRQ])- PEG2-R-PEG4- (e g., see K88 in Table 2A, see also B52(a) in Table 5C), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-.

[0128] Delivery construct 924a (FIG. 24A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FR-PEG4- (e.g., see K86 in Table 2A, see also B50(a) in Table 5C), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-.

[0129] Delivery construct 925a (FIG. 25A) is Ac-KKKRK-PEG4-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- (e.g., see K86 in Table 2A, see also B37(a) in Table 5C), wherein PEG2 is - (CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-.

[0130] Delivery' construct 926a (FIG. 26A) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-Bip- (e.g., see K35 in Table 2A, see also C4(a) in Table 6A), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-.

[0131] In embodiments, a compound that includes a delivery construct selected from 904a, 905a, 906a, 907a, 908a, 909a, 910a, 911a, 912a, 913a, 914a, 915a, 916a, 917a, 918a, 919a, 920a, 921a, 922a, 923a, 924a, 925a, or 926a.

[0132] In embodiments, a compound includes the delivery construct 904a. In embodiments, a compound includes the delivery construct 905a. In embodiments, a compound includes the delivery construct 906a. In embodiments, a compound includes the delivery construct 907a. In embodiments, a compound includes the delivery construct 908a. In embodiments, a compound includes the delivery construct 909a. In embodiments, a compound includes the delivery construct 910a In embodiments, a compound includes the delivery construct 911a. In embodiments, a compound includes the delivery construct 912a. In embodiments, a compound includes the delivery construct 913a. In embodiments, a compound includes the delivery construct 914a. In embodiments, a compound includes the delivery construct 915a. In embodiments, a compound includes the delivery construct 916a. In embodiments, a compound includes the delivery construct 917a. In embodiments, a compound includes the delivery¬ construct 918a. In embodiments, a compound includes the delivery- construct 919a. In embodiments, a compound includes the delivery construct 920a In embodiments, a compound includes the delivery- construct 921a. In embodiments, a compound includes the delivery-construct 922a In embodiments, a compound includes the delivery construct 923a. In embodiments, a compound includes the delivery construct 924a. In embodiments, a compound includes the delivery construct 925a In embodiments, a compound includes the delivery construct 926a.

[0133] In embodiments, a compound including a delivery of Formula I can include a delivery-construct of Formula I(i):Formula I(i)OR28-(AA%.111A pAA4l4or a pharmaceutically acceptable salt thereof, where:wl, w2, and w3 are each independently 0 or 1;xl, x2, and x3 are each independently an integer from 1 to 14;j I, j 2, and j 3 are each independently an integer from 1 to 4; andR20, AA1, al, y, n, R1, R2, R3, R4, R', R6, R7, AA2, a2, AA3, a3, AA4, and a4, are defined herein, where at least one of a2, a3, and a4 is 1 and at least one of w2 and w3 is 1.

[0134] The variables (R20, wl, w2, w3, xl, x2, x3, jl, j2, j3, al, a2, a3, a4, bl, b2, b3, LI, L2, L3, L4, AA1, AA2, AA3, AA4, n, y, R1, R2, R3, R4, R5, R6, and R'') in Formula I(i) can have any identity described herein for the respective variable.

[0135] In embodiments, a delivery construct of Formula I(i) can be covalently attached to OH, M, cargo, or the M' of M'-cargo at the point of attachment bond wherein M is a reactive handle described herein, M' is a bonding group described herein, and cargo is a cargo described herein. In embodiments, a delivery construct of Formula I(i) is covalently attached to M In embodiments, a delivery construct of Formula I(i) is covalently attached to the M' of M'-cargo. In embodiments, a delivery construct of Formula I(i) is covalently attached to a cargo. In embodiments, M is OH.

[0136] In embodiments, a delivery' construct of Formula I(i) may be of Formula 1(A):Formula 1(A):or a pharmaceutically acceptable salt thereof,wherein a3 is 1; and R20, AA1, al, xl, j 1, wl, y, n, R1, R2, R3, R4, R5, R6, R7, x2, j 2, and AA3, defined herein.

[0137] In embodiments of Formula 1(A),(a) AA1 comprises a sequence selected from: K(me)-K(me)-K(me)-R(me)-K(me), RBKKBR, RBRRBR, and YArVRRrGPR;(b) the cCPP is cyclo[Bta-G-Bta-GRGRQ] or cyclofGfFGrGrQ];(c) AA3 comprises a sequence selected from: Bip-BRBRB, BRB-Bip, BR-Bip-RB, FK, K-Bip, Nal-BRBRB, R-Bta, R-Bta-B, rf, RFB, RFE, R-Nal, and V-Cit;(d) xl is 2 and x2 is 4;(e) xl is 0 and x2 is 2, 4, or 8;(f) AA1 comprises kkkrk and AA2 comprises R-Bip; or(g) AA1 consists of KKRK and AA2 comprises R-Bip.

[0138] In embodiments of Formula 1(A). AA1 comprises a sequence selected from K(me)-K(me)-K(me)-R(me)-K(me), RBKKBR, RBRRBR, and YArVRRrGPR.

[0139] In embodiments of Formula 1(A), the cCPP is cyclo[Bta-G-Bta-GRGRQ] or cyclo[GfFGrGrQ],

[0140] In embodiments of Formula 1(A), AA3 comprises a sequence selected from: Bip- BRBRB, BRB-Bip, BR-Bip-RB, FK, K-Bip, Nal-BRBRB, R-Bta, R-Bta-B, rf, RFB, RFE, R- Nal, and V-Cit.

[0141] In embodiments of Formula 1(A), xl is 2 and x2 is 4.

[0142] In embodiments of Formula 1(A), xl is 0 and x2 is 2, 4, or 8

[0143] In embodiments of Formula 1(A), AA1 comprises kkkrk and AA2 comprises R-Bip.

[0144] In embodiments of Formula 1(A), AA1 consists of KKRK and AA2 comprises R-Bip.

[0145] In embodiments of Formula 1(A),indicates that the C -terminal amino acid residue of AA3 does not include the C -terminal OH of the carboxylic acid in the delivery construct.

[0146] Examples of delivery constructs of Formula 1(A) include those listed in Table 4 -4H InTables 4A-4H, the terminal indicates; Ac is -C(O)CH3; the cCPP is written as JA(cyclo[XAXBXcXDXEXFXGYA]) whereXA, XB, Xc, XD, XE, XF, and XGare amino acid residues with the side chain R1, R2, R3, R4, R5, R6, and R7, respectively, YAis the cCPP bridging amino acid residue, and JAis the bridging exocyclic amino acid residue (see, for example, the cCPP description herein); “miniPEG?” indicates ~(CH2-CH2-O)2-CH2-CO-, and “PEG#” indicates -(CH2-CH2-O)#-CH2-CO- or -(CH2-CH2-O)#-CH2-CH2-CO- where # indicates to the number of -CH2-CH2-O- units. In embodiments of the delivery constructs of Tables 4A-4H, each instance of “PEGi” refers to -(CH2-CH2-O)2-CH2-CO- (i.e., “miniPEG2”) and each instance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2. In embodiments of the delivery constructs of Tables 4A-4H, each instance of “PEG2” refers to - (CH2-CH2-O)2-CH2-CH2-CO- and each in stance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2.Table 4A.SEQ IDNo. Delivery ConstructNOs:Alfa) Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG12-Bip-BRBRB- 18, 40, 35SEQ ID No. Delivery ConstructNOs: (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-Bip-BRBRB-)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal-BRBRB- A2(a) 18, 40, 36 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal-BRBRB-)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bta-B- A3(a) 18, 40 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-B-)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BR-Bip-RB- A4(a) 18, 40, 85 Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-BR-Bip-RB- Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Val-Cit- A5(a) 18, 40Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-Val-Cit- Table 4B.SEQ IDNo. Delivery ConstructNOs: Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-B- A6(a) 13, 40(Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-B-)Ac-KKKRK -PEG2-K(cyc] o[FGFGRGRQ])-PEG 12-BRB-Bip- A7(a) 13, 40, 29(Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG12-BRB-Bip-) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Nal- A8(a) 13, 40(Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-rf- A9(a) 13, 40Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-rf- Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FK- A10(a) 13, 40(Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-FK-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta- A11(a) 13, 40(Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-)Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF- A12(a) 12, 40(Ac-kkkrk-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-)A 13(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip- 13, 40A14(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF- 13, 40 Table 4C.No. Delivery Construct SEQ ID NOs:Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-K-Bip- A15(a) 20, 40 (Ac-RBRRBR-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-K-Bip-)A16(a) Ac-RBKKBR-K(cyclo[FGFGRGRQ])-PEG8-R-Bip- 80, 40A17(a) Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG8-Bip- 20, 40 Table 4D.SEQ IDNo. Delivery ConstructNOs: Ac-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])- PEGs-RF- A18(a) 14, 40 (Ac-K(me)-K(nie)-K(me)-R(me)-K(me)-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-)SEQ ID No. Delivery ConstructNOs: Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF- A19(a) 21, 40(Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-)Table 4E.No. Delivery Construct SEQ ID NOs:Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-RF- A20(a) 18, 38(Ac-PKKKRKV-miniPEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-RF-)Table 4F.SEQ IDNo. Delivery ConstructNOs: Ac-KKKRK-PEG2-K(cyclo[GflFGrGrQ])-PEG8-RF- A21(a) 13, 44 (Ac-KKKRK-miniPEG2-K(cyclo[GfFGrGrQ])-PEG8-RF-)Ac-kkkRK-PEG2-K(cyclo[GfFGrGrQ])-PEG8-RF- A22(a) 11, 44(Ac-kkkRK-miniPEG2-K(cyclo[GfFGrGrQ])-PEG8-RF-)Table 4G.SEQ IDNo. Delivery ConstructNOs: A23(a) Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip- 1, 40A24(a) Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip- 12, 40 Table 4H.SEQ IDNo. Delivery ConstructNOs:A25(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFE- 13, 40

[0147] In embodiments, a compound includes a delivery construct selected from any one of Tables 4A-4H. In embodiments, a compound includes a delivery construct selected from Table 4A. In embodiments, a compound includes a delivery construct selected from Table 4B In embodiments, a compound includes a delivery construct selected from Table 4C. In embodiments, a compound includes a delivery construct selected from Table 4D. In embodiments, a compound includes a delivery construct selected from Table 4E. In embodiments, a compound includes a delivery construct selected from Table 4F. In embodiments, a compound includes a delivery construct selected from Table 4G. In embodiments, a compound includes a delivery construct selected from Table 4H.

[0148] In embodiments, a delivery construct of Formula I(i) may be of Formula 1(B):Formula 1(B):O<YR'NLZ"-7 b'R3O 1,4 or a pharmaceutically acceptable salt thereof,wherein a3 is I, R40is H or CH3, and R20, AA1, al, xl, j I, wl, y, n, R1, R2, R3, R4, R5, R6, R', x2, j2, AA3, x3, and j3 are defined herein.

[0149] In embodiments, R40is H. In embodiments, R40is CH3. When R40is CH3, the amino acid of the cCPP having the R2side chain can is N-methylated (e.g, N-methylated phenylalanine (f(N-me) or F(N-me)), N-methylated glycine (G(N-me)), and the like).

[0150] In embodiments of Formula 1(B):(a) AA1 comprises a sequence selected from: KGKRK, KKGRK, KKKGK, kkkrk, KKKRKF, KKKRKR, KKRKG, KKRKK, KKRKK, KKTRK, RBRRBR, RFGRK, TKKRK, and YArVRRrGPR;(b) the cCPP is cyclo[FGFGRrRQ], cyclo[4-Pyr-G-4-Pyr-GRGRQ], cyclofFAFARGRQ], cyclo[AGFGRGRQ], cyclo[F-G(N-me)-FGRGRQ], cyclo[FGAGRGRQ], cyclo[FGF-G(N-me)- RGRQ], cyclo[FGFG-Agp-G-Agp-Q], cyclo[FGFRHRHQ], cyclo[G-f(N-me)-FGrGrQ], cyclo[Gf-Nal-GrGrQ], cyclo[GFRGFRGQ], cyclo[GyYGrGrQ], cyclo[Pcpa-G-Pcpa-GRGRQ], cyclo[Phe(4-CN)-G-Phe(4-CN)GRGRQ];(c) AA3 comprises a sequence selected from: Agp-Bip, Agp-F, Cit-F, EF, FGR, FR, HoAr-Bip, KE, KRKR, Pcpa-F, PKKKRKV, R(me)-F(N-me), R-2-Pyr, R-3-Pyr, R-4-Pyr, R-Bip, R-Bip-R, R-Bta, rf, R-F(I), RFK, RFRF, RGF, R-Hph, RL, R-Nal, R-Nal-R, RPF, R-Phe(3-CN), R-Phg, RRFF, R-Trp(5-F), R-Tyr(Ph), RW, RY, and SF;(d) A A3 consists of F or R;(e) xl is 0 or4;(f) x2 is 8;(g) xl is 2 and x2 is 2, or(h) xl is 2, x2 is 2, and x3 is 2.

[0151] In embodiments of Formula 1(B), AA1 comprises a sequence selected from: KGKRK, KKGRK, KKKGK, kkkrk, KKKRKF, KKKRKR, KKRKG, KKRKK, KKRKK, KKTRK, RBRRBR, RFGRK, TKKRK, and YArVRRrGPR

[0152] In embodiments of Formula 1(B), the cCPP is cyclo[FGFGRrRQ], cyclo[4-Pyr-G-4-Pyr-GRGRQ], cyclo[FAFARGRQ], cyclo[AGFGRGRQ], cyclo[F-G(N-me)-FGRGRQ], cyclo[FGAGRGRQ], cyclo[FGF-G(N-me)-RGRQ], cyclo[FGFG-Agp-G-Agp-Q], cyclo[FGFRHRHQ], cyclo[G-f(N-me)-FGrGrQ], cyclo[Gf-Nal-GrGrQ], cyclo[GFRGFRGQ], cyclo[GyYGrGrQ], cyclo[Pcpa-G-Pcpa-GRGRQ], cyclo[Phe(4-CN)-G-Phe(4-CN)GRGRQ].

[0153] In embodiments of Formula 1(B), A A3 comprises a sequence selected from: Agp-Bip, Agp-F, Cit-F, EF, FGR, FR, HoAr-Bip, KE, KRKR, Pcpa-F, PKKKRKV, R(me)-F(N-me), R-2-Pyr, R-3-Pyr, R-4-Pyr, R-Bip, R-Bip-R, R-Bta, rf, R-F(I), RFK, RFRF, RGF, R-Hph, RL, R-Nal, R-Nal-R, RPF, R-Phe(3-CN), R-Phg, RRFF, R-Trp(5-F), R-Tyr(Ph), RW, RY, and SF.

[0154] In embodiments of Formula 1(B), AA3 consists of F or R.

[0155] In embodiments of Formula 1(B), xl is 0 or 4.

[0156] In embodiments of Formula 1(B), x2 is 8.

[0157] In embodiments of Formula 1(B), xl is 2 and x2 is 2.

[0158] In embodiments of Formula 1(B), xl is 2, x2 is 2, and x3 is 2.

[0159] Examples of delivery constructs of Formula 1(B) include those listed in Table 5A-4E. InTables 5A-5E, the terminal indicates; Ac is -C(O)CH3; the cCPP is written as JA(cyclo[XAXBXcXDXEXFXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with the side chain R1, R2, R\ R4, R5, R6, and R7, respectively, Y ' is the cCPP bridgingamino acid residue, and JAis the bridging exocyclic amino acid residue (see, for example, the cCPP description herein); “miniPEGi” indicates -(CH2-CH2-O)2-CH2-CO-; and “PEG#” indicates -(CH2-CH2-O)#-CH2-CO- or ~-(CH₂-CH₂-O)#-CH₂-CH₂-CO- where # indicates to the number of -CH2-CH2-O- units. In embodiments of the delivery constructs of Tables 5A-5E, each instance of “PEG2” refers to (CH2-CH2-O)2-CH2-CO- (i.e., “miniPEG2”) and each instance of “PEG#” refers to -(CH₂-CH₂-O)#-CH₂-CH₂-CO- where # is an integer greater than 2. In embodiments of the delivery constructs of Tables 5A-5E, each instance of “PEG2” refers to -(CH₂-CH₂-O)₂-CH₂-CH₂-CO- and each instance of “PEG#” refers to -(CH₂-CH₂-O)#-CH₂-CH₂-CO- where # is an integer greater than 2.Table 5A.SEQ IDNo. Delivery ConstructNOs: Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG₈-R-Bip-PEG2- Bl(a) 13, 40 (Ac-KKKRK-miniPEG₂-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-PEG2-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG2- B2(a) (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-R-Bta- 13, 40 miniPEG₂-)Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4- B3(a) 20, 40 (Ac-RBRRBR-K(cyclo[FGFGRGRQ])-miniPEG2-KF-PEG4-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bta-PEG2- B4(a) 13, 40(Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bta-miniPEG2-)Table 5B.SEQ IDNo.Delivery Construct NOs: Ac-KKKRK-PEG2-K(cyclo[FGFRHRHQ])-PEG2-RF-PEG4- B5(a) 13, 42 (Ac-KKKRK-miniPEG2-K(cyclo[FGFRHRHQl)-miniPEG2-RF-PEG4-)Ac-YArVRRrGPR-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4- B6(a) (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FfFGRGRQ])-miniPEG2-RF- 21, 39 PEG4-)Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEG8- B7(a) 40, 18(Ac-K(cyclo[FGFGRGRQl)-miniPEG2-PKKKRKV-PEG₈-)Table 5C.SEQ IDNo. Delivery ConstructNOs: B8(a) Ac-TKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 9, 40 B09(a) Ac-KKTRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 8, 40 B10(a) Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG4- 21, 40Bll(a) Ac-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ])-PEG2-RG-PEG4- 13, 55SEQ ID No. Delivery ConstructNOs: B12(a) Ac-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ])-PEG2-RF-PEG4- 13, 55 Bl 3(a) Ac-KKKRK-PEG2-K(cyclo[Gf-Nal-GrGrQ])-PEG2-RF-PEG4- 13, 56 B14(a) Ac-KKKRK-PEG2-K(cyclo[GyYGrGrQ])-PEG2-RF-PEG4- 13, 58 B15(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-PEG4- 13, 40 Bl 6(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG2- 13, 40 B17(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-PEG4- 13, 40 B18(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFR-PEG4- 13, 40 Bl 9(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-R-PEG4- 13, 40 B20(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-R-PEG4- 13, 40 B21(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4- 13, 40 B22(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG8- 13, 40 B23(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4- 13, 40 B24(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(3-Pyr)-PEG4- 13, 40 B25(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(2-Pyr)-PEG4- 13, 40 B26(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(4-Pyr)-PEG4- 13, 40 B27(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phe(3-CN)-PEG4- 13, 40 B28(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Trp(5-F)-PEG4- 13, 40 B29(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Tyr(Ph)-PEG4- 13, 40 B30(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-HoArg-Bip-PEG4- 13, 40 B31(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-rf-PEG4- 13, 40 B32(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R(me)-F(N-me)-PEG4- 13, 40 B33(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-(4-Pyr)-PEG4-Nal- 13, 40 B34(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4-F- 13, 40 Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-RF- B35(a) 13, 46 PEG₄- Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-R-Bip- B36(a) 13, 46 PEG4- B37(a) Ac-KKKRK-PEG4-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 13, 40 B38(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG4- 13, 40 B39(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFRF-PEG4- 13, 40, 33 B40(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RRFF-PEG4- 13, 40, 86 B41(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4- 13, 40 B42(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KFKF-PEG4- 40, 32 B43(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-EF-PEG4- 13, 40 B44(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-PEG4- 13, 40 B45(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FGR-PEG4- 13, 40 Ac-KKKRK-PEG2-K(cyclo[Phe(4-CN)-G-Phe(4-CN)-GRGRQ])-PEG2- B46(a) 13, 59 RF-PEG4-B47(a) Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-K-PEG4- 1, 40SEQ ID No. Delivery ConstructNOs: B48(a) Ac-KKRK-PEG2-K(cyclo[FGFGRrRQ])-PEG2-RF-PEG4- 1, 53 B49(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ]-PEG2-RF(I)-PEG4- 13, 40 B50(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FR-PEG4- 13, 40 B51(a) Ac-KKKRKR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-F-PEG4- 17, 40 B52(a) Ac-KKKRKF-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG4- 16, 40 B53(a) Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4- 13, 57 B54(a) Ac-KKKRK-PEG2-K(cyclo[FFGRRGQ])-PEG2-RF-PEG4- 13, 49 B55(a) Ac-KGKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 3, 40 B56(a) Ac-KKGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG₂-RF-PEG4- 4, 40 B57(a) Ac-KKKGK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 5, 40 B58(a) Ac-KKRKG-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 6, 40 B59(a) Ac-KKRKK-PEG2-K(cyclo[FGFG-Cit-GRQ])-PEG2-RF-PEG4- 7, 51 B60(a) Ac-KKRKK-PEG2-K(cyclo[FGFGRG-Cit-Q])-PEG2-RF-PEG4- 7, 52 B61(a) Ac-KKRKK-PEG2-K(cyclo[AGFGRGRQ])-PEG2-RF-PEG4- 7, 47 B62(a) Ac-KKRKK-PEG2-K(cyclo[FGAGRGRQ])-PEG2-RF-PEG4- 7, 50 B63(a) Ac-KKKGK-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4- 5, 39 B64(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-SF-PEG4- 13, 40 B65(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RL-PEG4- 13, 40 B66(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RY-PEG4- 13, 40 B67(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RW-PEG4- 13, 40 B68(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Cit-F-PEG4- 13, 40 B69(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RPF-PEG4- 13, 40 B70(a) Ac-KKKRK-PEG2-K(cyclo[FGF-G(N-me)-RGRQ])-PEG2-RPF-PEG4- 13, 60 B71(a) Ac-KKKRK-PEG2-K(cyclo[F-G(N-me)-FGRGRQ])-PEG2-RPF-PEG4- 13, 61 B72(a) Ac-KKKRK-PEG2-K(cyclo[FAFARGRQ])-PEG2-RF-PEG4- 13, 62 B73(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-Bip-PEG4- 13, 40 B74(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-F-PEG4- 13, 40B75(a) Ac-KKKRK-PEG2-K(cyclo[FGFG-Agp-G-Agp-Q])-PEG2-RF-PEG4- 13, 63 Table 5D.SEQ IDNo. Delivery ConstructNOs: B76(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4- 13, 40 B77(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG2- 13, 40 B78(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phg-PEG4- 13, 40 B79(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Hph-PEG4- 13, 40 B80(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Pcpa-F-PEG4- 13, 40 B81(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4- 13, 40B82(a) Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 12, 40SEQ ID No. Delivery ConstructNOs: B83(a) Ac-KKKRK-PEG2-K(cyclo[Pcpa-G-Pcpa-GRGRQ])-PEG2-RF-PEG4- 13, 64B84(a) Ac-RFGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4- 22, 40 Table 5E.SEQNo. Delivery Construct ID NOs: Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- 24, 40B85(a) (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-)

[0160] In embodiments, a compound includes a delivery construct selected from any one of Tables 5A-5E. In embodiments, a compound includes a delivery construct selected from Table 5A. In embodiments, a compound includes a delivery construct selected from Table 5B In embodiments, a compound includes a delivery construct selected from Table 5C In embodiments, a compound includes a delivery construct selected from Table 5D. In embodiments, a compound includes a delivery construct selected from Table 5E.

[0161] In embodiments, a delivery' construct of Formula I(i) may be of Formula 1(C):Formula 1(C):R20-(AA4)6or a pharmaceutically acceptable salt thereof,wherein a3 and a4 are 1 and R20, AA 1, al, xl, j 1, wl, y, n, R1, R2, R3, R4, R5, R6, R7x2, j2, AA3, x3, j3, and AA4, are defined herein,

[0162] In embodiments of Formula 1(C);(a) AA1 comprises K(me)-K(me)-K(me)-R(me)-K(me), KBKBKBRBK, KKKHH, N(Arg)- B-N(Arg)-N(Arg)-B-N(Arg), N(k)-N(k)-N(k)-N(Arg)-N(k), RBRRBR, RFKKRFK, or YArVRRrGPR;(b) the cCCP is cyclo[GFFGRGRQ], cyclo[GFRGFRGQ], or cyclo[RFGGRFGQ];(c) AA3 comprises Bip, FRF, KR, R-(4-Pyr), rf, RGF, or R-Nal;(d) xl is 0;(e) x2 is 8;(f) x2 is 8 and x3 is 4; or(g) x2 is 2, x3 is 2, x4 is 4 and AA3 comprises Nah

[0163] In embodiments of Formula 1(C),(a) AA1 comprises K(me)-K(me)-K(me)-R(me)-K(me), KBKBKBRBK, KKKHH, N(Arg)- B-N(Arg)-N(Arg)-B-N(Arg), N(k)-N(k)-N(k)-N(Arg)-N(k), RBRRBR, RFKKRFK, or YArVRRrGPR,(b) the cCCP is cyclo[GFFGRGRQ], cyclo[GFRGFRGQ], or cyclo[RFGGRFGQ];(c) A A3 comprises Bip, FRF, KR, R-(4-Pyr), RGF, or R-Nal;(d) xl is 0;(e) x2 is 8;(f) x2 is 8 and x3 is 4, or(g) x2 is 2, x3 is 2, x4 is 4 and AA3 comprises Nal.

[0164] In embodiments of Formula 1(C), AAl comprises K(me)-K(me)-K(me)-R(me)-K(me), KBKBKBRBK, KKKHH, N(Arg)-B-N(Arg)-N(Arg)-B-N(Arg), N(k)-N(k)-N(k)-N(Arg)-N(k), RBRRBR, RFKKRFK, or YArVRRrGPR

[0165] In embodiments of Formula 1(C), the cCCP is cyclo[GFFGRGRQ], cyclo[GFRGFRGQ], or cyclo[RFGGRFGQ],

[0166] In embodiments of Formula 1(C), AA3 comprises Bip, FRF, KR, R-(4-Pyr), rf, RGF, or R-Nal.

[0167] In embodiments of Formula 1(C), AA3 comprises Bip, FRF, KR, R-(4-Pyr), RGF, or R-Nal.

[0168] In embodiments of Formula 1(C), xl is 0.

[0169] In embodiments of Formula 1(C), x2 is 8.

[0170] In embodiments of Formula 1(C), x2 is 8 and x3 is 4.

[0171] In embodiments of Formula 1(C), x2 is 2, x3 is 2, x4 is 4 and AA3 comprises Nal.

[0172] In embodiments of Formula 1(C),indicates that the C -terminal amino acid residue of AA4 does not include the C-terminal OH of the carboxylic acid in the delivery construct.

[0173] Examples of delivery constructs of Formula 1(C) include those listed in Tables 6A-6E. InTables 6A-6E, the terminal indicates; Ac is -C(O)CH₃; the cCPP is written as JA(cyclo[XAXBXcXDXEXFXGYA]) where XA, XB, Xc, XDXE, XF, and XGare amino acid residues with the side chain R1, R2, R3, R4, R5, R6, and R7, respectively, YAis the cCPP bridging amino acid residue, and JAis the bridging exocyclic amino acid residue (see, for example, the cCPP description herein); “miniPEG2” indicates -(CH2-CH2-O)2-CH2-CO-; and “PEG#” indicates -(CH₂-CH₂-O)#-CH₂-CO- or -(CH₂-CH₂-O)#-CH₂-CH₂-CO- where # indicates to the number of -CH2-CH2-O- units. In embodiments of the delivery constructs of Tables 6A-6E, each instance of “PEG2” refers to -(CH2-CH2-O)2-CH2-CO- (i e., “miniPEG ”) and each instance of “PEG#” refers to -(CH₂-CH₂-O)#-CH₂-CH₂-CO- where # is an integer greater than 2. In embodiments of the delivery constructs of Tables 6A-6E, each instance of “PEG2” refers to -(CH₂-CH₂-O)₂-CH₂-CH₂-CO- and each instance of “PEG#” refers to -(CH₂-CH₂-O)#-CH₂-CH₂-CO- where # is an integer greater than 2.Table 6A.SEQ IDNo. Delivery ConstructNOs: Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-Bip- Cl(a) 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-rf-PEG4-Bip-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Nal- C2(a) (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-Nal- 13, 40 )Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG₈-RF-PEG4-Nal- C3(a) 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG4-Nal-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG₄-Bip- C4(a) (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-KF-PEG4- 13, 40_Table 6B.SEQ IDNo. Delivery ConstructNOs: Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-F- C5(a) 18, 40(Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-F-) Table 6C.SEQ IDNo. Delivery ConstructNOs: Ac-PKKKRKV-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG2-Nal- C6(a) (Ac-PKKKRKV-miniPEG2-K(cyclo[FfFGRGRQ])-miniPEG2-RF- 18, 39 miniPEG2-Nal-)Ac-KKKRK-PEG2-K(cyclo[FfFGRGRQ])-PEGi2-(2-Nal)-PEG2-(2-Nal)- C7(a) (Ac-KKKRK-miniPEG2-K(cyclo[FtFGRGRQ])-PEGi2-(2-Nal)-miniPEG2- 13, 39 (2-Nal)-)Ac-KKKRK-PEG2-K(cyclo[FfFGRGRQ])-PEGi2-Bip-PEG2-Bip- C8(a) (Ac-KKKRK-miniPEG2-K(cyclo[FfFGRGRQ])-PEGi2-Bip-miniPEG2-Bip- 13, 39 )C9(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-Bip- 13, 40 Table 6D.SEQ IDNo. Delivery ConstructNOs: Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bta- Cl 0(a) (Ac-RBRRBR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-Bta- 20, 40 )Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-PEG2-Nal- C11(a) 20, 39 (Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-miniPEG2-Nal-)Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEGi2-Nal-PEG2-Nal- C12(a) 20, 40(Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEGi2-Nal-miniPEG2-Nal-)Table 6E.SEQ IDNo. Delivery ConstructNOs: Ac-KKKHH-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- (Ac-KKKHH-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 15, 40 C13(a) PEG4-Bip~)Ac-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2- K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- 14, 40 (Ac-K(me)-K(me)-K(me)-R(me)-K(me)-miniPEG2- C14(a) K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-Bip-)Ac-KBKBKBRBK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4~Bip- 23, 40 (Ac-KBKBKBRBK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-C15(a) RF-PEG4-Bip-)SEQ ID No. Delivery ConstructNOs: Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-Bip- (Ac-KKKRK-miniPEG2-K(cyclo[GFRGFRGQ])-miniPEG2-RF- 13, 57 C16(a) PEG‘i-Bip-)Ac-KKKRK-PEG2-K(cyclo[GRFGRFGQ])-PEG2-RF-PEG4-Bip- (Ac-KKKRK-miniPEG2-K(cyclo[GRFGRFGQ])-miniPEG2-RF- 13, 66 C17(a) PEG₄-Bip-)Ac-RFKKRFK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- (Ac-RFKKRFK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 24, 40 C18(a) PEG4-Bip-)Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4- Bip- 21, 40 (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2- C19(a) RF-PEG4-Bip-)Ac-KKKRK-PEG2-K(cyclo[RFGGRFGQ])-PEG2-RF-PEG4-Bip- (Ac-KKKRK-miniPEG2-K(cyclo[RFGGRFGQ])-miniPEG2-RF- 13, 67 C20(a) PEG4-Bip-)Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-PEG2- K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- 25, 40 (Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-miniPEG2- C21(a) K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-Bip-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 13, 40 C22(a) PEG4-Bip-)Ac-(N(Arg)-B-(N(Arg))-(N(Arg))-B-(N(Arg))- K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- 26, 40 (Ac-(N(Arg))-B-(N(Arg))-(N(Arg))-B-(N(Arg))- C23(a) K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-Bip-)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FRF-PEG4-Bip- (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-FRF- 13, 40 C24(a) PEG4-Bip-)Ac-KKKRK-PEG2-K(cyclo[GFFGRGRQ])-PEG2-RF-PEG4-Bip- (Ac-KKKRK-miniPEG2-K(cyclo[GFFGRGRQ])-miniPEG2-RF- 13, 65C25(a) PEG4-Bip-)

[0174] In embodiments, a compound includes a delivery construct selected from any one of Tables 6A-6E In embodiments, a compound includes a delivery construct selected from Table 6A In embodiments, a compound includes a delivery construct selected from Table 6B In embodiments, a compound includes a delivery construct selected from Table 6C. In embodiments, a compound includes a delivery construct selected from Table 6D. In embodiments, a compound includes a delivery construct selected from Table 6E.

[0175] In embodiments, a delivery construct of Formula I(i) may be of Formula 1(D):Formula 1(D):or a pharmaceutically acceptable salt thereof,wherein a2 and a3 are 1 and R20, AA1, al, xl, j 1, wl, y, n, R1, R2, R3, R4, R5, R6, R7, AA2, x2, j2, and AA3, are defined herein.

[0176] A delivery construct of Formula I(i) can be a delivery construct of Formula 1(D).-1-

[0177] In embodiments of Formula 1(D), indicates that the C-terminal amino acid residue of AA3 does not include the C-terminal OH of the carboxylic acid in the delivery construct.

[0178] In embodiments, a delivery construct of Formula I(i) may be of Formula 1(E):Formula 1(E):for a pharmaceutically acceptable salt thereof,wherein a2 is 1 and R20, AA1, al, xl, j 1, wl, y, n, Rl, R2, R3, R4, R5, R6, R7, AA2, x2, and j2, are defined herein.

[0179] In embodiments of Formula 1(E):(a) x2 is 2 or 8;(b) AA2 comprises R-Bip; or(c) AA1 comprises KKKRK, cCPP is cyclofFGFGRGRQ], AA2 comprises RF, and x2 is 4.

[0180] In embodiments of Formula 1(E), x2 is 2 or 8.

[0181] In embodiments of Formula 1(E), AA2 comprises R-Bip.

[0182] In embodiments of Formula 1(E), AA1 comprises KKKRK, cCPP is cyclofFGFGRGRQ], AA2 comprises RF, and x2 is 4.

[0183] A delivery construct of Formula I(i) can be a delivery construct of Formula 1(E).

[0184] Examples of deliver)' constructs of Formula 1(E) include those listed in Table 7. In Table7, the terminal indicates; Ac is -C(O)CH3; the cCPP is written as JA(cyclo[XAXBXcXDXEXFXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with the side chain R1, R2, R3, R4, R5, R’, and R7, respectively, YAis the cCPP bridging amino acid residue, and JAis the bridging exocyclic amino acid residue (see, for example, the cCPP description herein); “miniPEG ” indicates -(CH2-CH2-O)2-CH -CO-, and “PEG#” indicates (CH2-CH2-O)#-CH2-CO- or-(CH2-CH2-O)#-CH2-CH2-CO- where # indicates to the number of -CH2-CH2-O- units. In embodiments of the delivery constructs of Table 7, each instance of “PEG?” refers to -(CH2-CH2-O)2-CH2-CO- (i.e., “tniniPEGi”) and each instance of “PEG#” refers to (CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2. In embodiments of the delivery constructs of Table 7, each instance of “PEG ” refers to -(CFb- CH2-O)2-CH2-CH2-CO- and each instance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2.Table 7.No. Delivery Construct SEQ ID NOs: El Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-R-Bip-PEG8- 13, 40 E2 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG4- 13, 40E3 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG2- 13, 40

[0185] In embodiments, a compound includes a delivery construct selected from Table 7.

[0186] A delivery’ consfruct of Formula I(i) can be a delivery construct of Formula 1(E).

[0187] In embodiments, a delivery construct of Formula II may be of Formula 11(F):Formula 11(F):H 9 / \ ° H o R28~(AA1)~tN4 x--.. U'k i IM x. Ji J- 03 ' Ji - H k; H Op kfn Y N \ '••''? YV' ((AAAA33))''R. A(k,ol, A,< iW * k " / > i Vi Oi k Hx2j2 x3 Q ” ** w \l V / NH 0Y ‘ft 0 O R1N HNHo^,NH^40' -N x^-R" R* Nn HN"'° o-V NH RsZR’ o6 R4or a pharmaceutically acceptable salt thereof,wherein x4 is an integer from 1 to 14; j4 is integer from 1 to 4; R40is H or CHJ; and R20, AA1, al, xl, jl, wl, y, n, R1, R2, R3, R, Ry R6, R7, x2, j2, AA3, x3, j3, AA4, ml, and M are defined herein.

[0188] x4 is an integer from 1 to 14. x4 can be 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, or 14. x4 can be 2, 4, 6, 8, 10, or 12. x4 can be 2, 4, 8, or 12. x4 can be 2. x4 can be 4. x4 can be 6. x4 can be 8. x4 can be 12.

[0189] j4 can be integer from 1 to 4. 0. j4 can be 1, j4 can be 2. j4 can be 3 j4 can be 4.

[0190] A delivery construct of Formula II can be a delivery construct of Formula 11(F).

[0191] Examples of compounds of Formula 11(F) include those listed in Table 8. In Table 8, theterminal indicates*; Ac is -C(O)CH3; the cCPP is written as JA(cyclo[XAXBXcXDXEXFXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with the side chain R1, R2, R3, R4, R5, R6, and R7, respectively, YAis the cCPP bridging amino acid residue, and JAis the bridging exocyclic amino acid residue (see, for example, the cCPP description herein); “miniPEGi” indicates -(CH2-CH2-O)2-CH2-CO-; and “PEG#” indicates -(CH2-CH2-O)#-CH2-CO- or ~-(CH₂-CH₂-O)#-CH₂-CH₂-CO- where # indicates to the number of -CH2-CH2-O- units. In embodiments of the delivery constructs of Table 8, each instance of “PEG2” refers to -~(CH2-CH2-O)2-CH2-CO- (i.e., “miniPEG2”) and each instance of“PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2. In embodiments of the delivery constructs of Table 8, each instance of “PEG2” refers to -(CH2-CH2-O)2-CH2-CH -CO- and each instance of “PEG#” refers to ~-(CH -CH2-O)#-CH2-CH2-CO-where # is an integer greater than 2.Table 8SEQ IDNo. Delivery ConstructNOs: Fl(a) Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEG8-RF-PEG4- 40, 18 F2(a) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG2-F-PEG4- 40, 18W) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-PEG4- 13, 40Compounds of the present disclosure that include a delivery construct

[0192] In embodiments, a deliver}' construct Formulae I(i), 1(A), 1(B), 1(C), 1(D), 1(E), or 11(F), can be covalently attached to a reactive handle (M) to form a compound the includes a delivery construct In embodiments, a reactive handle can be OH.

[0193] In embodiments a compound of the present disclosure can be of Formula III:Formula III:— N X R^^(AA1)8T(L1)MY '(AA2)ai(^or a pharmaceutically acceptable salt thereof,where:Oal, a2, a3, and a4 are each independently 0 or 1 and at least 1 of a2, a3, and a4 is 1;bl, b2, and b3 are each independently 0 or 1 and at least one of bl, b2, and b3 is 1;LI, L2, and L3 are each independently a linker covalently coupling two adjacent motifs;AA1 is an amino acid residue or a peptide that comprises2 to 10 amino acid residues;AA2, AA3, and AA4 are each independently an amino acid residue or a peptide that comprises 2 to 6 amino acid residues, where at least one of AA2, AA3, and AA4 present in the compound comprises a hydrophobic or a hydrophilic amino acid;n is an integer from 1 to 3,y is an integer from 1 to 5;ml is 0 or 1;M includes a reactive handle; andR1, R2, R3, R4, R5, R6, and R7are each independently an amino acid side chain.

[0194] A delivery construct of Formula I can be of Formula III wherein the delivery construct of Formula I is covalently attached M.

[0195] Formula III comprises a cyclic cell penetrating peptide (cCPP). In Formula III the cCPP comprises the amino acid residues characterized by Rl, R2, R3, R4, R5, R6, and R7. In Formula I, the amino acid residues or peptides of AAL AA2, AA3, and AA4 are exocyclic amino acid residues or peptides.OA

[0196] In embodiment R20is ". For example, in embodiments when al is 1, the amino group of the N-terminal amino acid residue of AA1 can be acetylated (-C(O)-CH3). In other embodiments when al is 1, the amino group of the N-terminal amino acid of AA1 is not acetylated.

[0197] al, a2, a3, and a4 are each independently 0 or 1 where at least one of a2, a3, and a4 is 1. In embodiments, at least one of a2 and a3 is 1. al can be 1. al can be 0 a2 can be 1. a2 can be 0. a3 can be 1. a3 can be 0.

[0198] In embodiments, al is 1, and only one of a2, a3, and a4 is 1. In embodiments, al is 0, a2 is 0, a3 is 1, and a4 is 0. In embodiments, al is 1, a2 is 0, a3 is 1, and a4 is 0 In embodiments, al is 1, a2 is 0, a3 is 1, and a4 is 1. In embodiments, al is 0, a2 is 0, a3 is 1, and a4 is 1.

[0199] In embodiments, al is 1, a2 is 1, a3 is 1, and a4 is 0. In embodiments, al is 0, a2 is 1, a3 is 1, and a4 is 0. In embodiments, al is I, a2 is 1, a3 is 0, and a4 is 0. In embodiments, al is 0, a2 is 1, a3 is 0, and a4 is 0.

[0200] bl, b2, b3, and b4 are each independently 0 or 1 where at least one of bl, b2, and b3 is 1. In embodiments, at least one of bl and b2 is 1. bl can be 1. bl can be 0. b2 can be 1. b2 can be 0. b3 can be 1. b3 can be 1 In embodiments, bl is 1, b2 is 1, and b3 is 0. In embodiments, bl is 0, b2 is 1, and b3 is 0. In embodiments, bl is 1, b2 is 1, and b3 is 1. In embodiments, bl is 0, b2 is 1, and b3 is 1.

[0201] In embodiments, al is 1, a2 is 1, a3 is 0, a4 is 0, bl is 1, b2 is 1, and b3 is 0. In embodiments, al is 0, a2 is 1, a3 is 0, bl is 1, b2 is 1, and b3 is 0. In embodiments, al is 0, a2 is 1, a3 is 0, bl is 0, b2 is 1, and b3 is 0.

[0202] In embodiments, al is 1, a2 is 0, a3 is 1, a4 is 0, bl is 1, b2 is 1, and b3 is 1. In embodiments, al is 0, a2 is 0, bl is 1, b2 is 1, and b3 is 1. In embodiments, al is 0, a2 is 0, bl is 0, b2 is 1, and b3 is 1.

[0203] In embodiments, al is 1, a2 is 0, a3 is 1, a4 is 1, bl is 1, b2 is 1, and b3 is 1. In embodiments, al is 1, a2 is 0, a3 is 1, a4 is 1, bl is 1, b2 is 1, and b3 is 1. In embodiments, al is 1, a2 is 0, a3 is 1, a4 is 1, bl is 0, b2 is 1, and b3 is 1

[0204] In embodiments, al is 1, a2 is 1, a3 is 1, a4 is 0, bl is 1, b2 is 1, and b3 is 0, In embodiments, al is 1, a2 is 1, a3 is 1, a4 is 0, bl is 1, b2 is 1, and b3 is 0. In embodiments, al is 1, a2 is 1, a3 is 1, a4 is 0, bl is 0, b2 is 1, and b3 is 0.In embodiments, al is 1, a2 is 1, a3 is 0, a4 is 0, bl is 1, b2 is 1, and b3 is 0. In embodiments, al is 0, a2 is 1, a3 is 0, a4 is 0, bl is 1, b2 is 1, and b3 is 0. In embodiments, al is 0, a2 is 1 „ a3 is 0, a4 is 0, bl is 0, b2 is 1, and b3 is 0.

[0205] In embodiments, a compound of the present disclosure can be of Formula IV:Formula IV:or a pharmaceutically acceptable salt thereof,where:OR20isH or,al 0 or 1;bl is 0 or 1;LI, L2, L3, and L4 are each independently a linker covalently coupling two adjacent motifs, AA1 is an amino acid residue or a peptide that includes 2 to 10 amino acid residues;AA3 and AA4 are each independently an amino acid residue or a peptide that comprises 2 to 6 amino acid residues, wherein at least one of AA3 and AA4 comprises a hydrophobic or a hydrophilic amino acid;n is an integer from 1 to 3;y is an integer from 1 to 5;ml is 0 or 1;M includes a reactive handle; andR1, R2, R3, R4, R5, R6, and R7are each independently the side chain an amino acid.

[0206] Formulae IV comprises a cyclic cell penetrating peptide (cCPP). The cCPP comprises the amino acid residues characterized by R1, R2, R3, R4, R5, R6, and R'. In Formula IV, the amino acid residues or peptides of AA1, AA3, and AA4 are exocyclic amino acids residues or peptides.OJ-

[0207] In embodiments, R20is ' L. In embodiments when al is 1, the amino group of the N-terminal amino acid residue of AA1 can be acetylated (-C(O)-CH3). In embodiments when al is 1, the amino group of the N-terminal amino acid of AA1 is not acetylated.

[0208] al can be 0 or 1. al can be 0. a l can be 1.

[0209] bl can be 0 or 1. bl can be 0. bl can be 1.

[0210] In embodiments, al is 0 and bl is 0. In embodiments al is 0 and bl is 1. In embodiments al is 1 and bl is 0. In embodiment, al is 1 and bl is 1.Linker: LI, L2, L3, L4 and combinations thereof

[0211] LI, L2, L3, and L4 are each independently a linker covalently coupling two adjacent motifs.

[0212] LI, L2, L3, and L4 (if present) can each independently comprise, for example, one or more ethers, one or more esters, one or more ketones, one or more amides, one or more alkylenes, or any combination thereof. In embodiments, LI, L2, L3, and L4 (if present) can each independently comprise one or more amides. In embodiments, LI, L2, L3, L4 (if present) can each independently comprise one or more ethers. In embodiments, LI, L2, L3, and L4 (if present) can each independently comprise one or more alkylenes. In embodiments, LI, L2, L3, and L4 (if present) can each independently comprise one or more alkylenes of length Cl to C5. In embodiments, LI, L2, L3, and L4 (if present) can each independently comprise one or more alkylenes of length Cl, C2, C3, C4, or C5. In embodiments, LI, L2, L3, and L4 (if present) can each independently comprise one or more alkylenes of length Cl. In embodiments, LI, L2, L3, and L,4 (if present) can each independently comprise one or more alkylenes of length C2. In embodiments, LI, L2, L3, and L4 (if present) can each independently comprise one or more alkylenes of length C3. In embodiments, LI, L2, L3, and L4 (if present) can each independentlycomprise one or more alkylenes of length C4. In embodiments, LI, L2, L3, and L4 (if present) can each independently comprise one or more alkylenes of length C5,

[0213] In embodiments, LI, L2, L3, and L4 (if present) can each independently comprise one or more poly(ethylene glycol) (PEG) units (-CH2-CH2-O-). In embodiments, LI, L2, L3, and L4 (if present) can each independently comprise 1 to 14 PEG units. In embodiments where any of LI, L2, L3, and L4 include more than one PEG unit, the PEG units can be continuous or discontinuous. For example, in embodiments where any of LI, L2, L3, and L4 include more than one PEG unit, the PEG units or groups of PEG units may be separated with a dialkyl, an amide, an ester, or a combination of a dialkyl and amide or a dialkyl and an ester.

[0214] In embodiments, one or more of LI, L2, L3, and L4 present in the compound compriseswhere p is an integer from 1 to 14 and s is and integer from 1 to 4. s can be 1. s can be 2. s can be 3. s can be 4. In embodiments, p can be 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, or 14 and s can be 1, 2, 3, or 4. In embodiments, p can be 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, or 14 and s can be 1 or 2. In embodiments, p is 2, 4, 6, 8, 10, 12, or 14 and s is 1. In embodiments, p is 2, 4, 6, 8, 10, 12, or 14 and s is 2. In embodiments, p is 2, 4, 8, or 12 and s is 1, In embodiments, p is 2, 4, 8, or 12 and s is 2. In embodiments, p is 2 and s is 1. In embodiments, p is 2 and s is 2. In embodiments, p is 4 and s is 1. In embodiments, p is 4 and s is 2. In embodiments, p is 8 and s is 1. In embodiments, p is 8 and s is 2. In embodiments, p is 8 and s is 2. In embodiments, p is 12 and s is 1. In embodiments, p is 12 and s is 2.

[0215] In embodiments, bl is 1 LI compriseswhere p and s are definedherein. In embodiments, b2 is 1 and L,2 compriseswhere p and s aredefined herein. In embodiments, L.2 compriseswhere p and s are definedherein. In embodiments, b3 is 1 and L3 compriseswhere p and s are defined herein.

[0216] In embodiments, bl is 1, b2 is 1, b3 is 0, and LI and L2 both comprisewhere p and s are defined herein and can be the same or different for L I Hop w and L2. In embodiments, bl is 0, b2 is 1, b3 is 0, and LI comprises•'P 6 where p and s are defined herein.

[0217] In embodiments, bl is 1, b2 is 1, b3 is 1, and L, L2, and L3 all comprisevwhere p and s are defined herein and can be the same or different for LI, L2, and L3. In embodiments, bl is 0, b2 is 1, b3 is 1, and L2 and L3 both comprise H1P rtwwhere p and s are defined herein and can be the same or different for LI,cHzand L2. In embodiments, bl is I and LI, L2, L3, and L4 all comprise55o where p and s are defined herein and can be the same or different for LI, L2, L3, and L4. Inembodiments, bl is 0 and L2, L3, and L4 all comprisewhere p and s are defined herein and can be the same or different for L2, L3, and L4.Amino Acid(s): AAI

[0218] AAI, when present (al is 1), is a single amino acid residue or a peptide of 2 to 10 amino acid residues.

[0219] AAI comprises 1 to 10 amino acid residues e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10 amino acid residues. In embodiment, AAI comprises 2 to 8 amino acid residues or 2 to 6 amino acid residues. In embodiments, AAI is a single amino acid residue. In embodiments, AAI is a 2-residue peptide. In embodiments, AAI is a 3-residue peptide In embodiments, AAI is a 4-residue peptide. In embodiments, AAI is a 5-residue peptide. In embodiments, AAI is a 6-residue peptide. In embodiments, AAI is a 7-residue peptide. In embodiments, AAI is an 8-residue peptide. In embodiments, AAI is a 9-residue peptide. In embodiments, AAI is a 10-residue peptide.

[0220] The amino acid residues in AAI can have D- or L-stereochemistry. The amino acid residues of AAI may all be D-amino acids. The amino acid residues of AAI may all be L-amino acids. The amino acid residues of AAI may be a combination of D-amino acids and L-amino acids.

[0221] In embodiments, AA I comprises one of the following sequences: K, KK, RK, KFK, KRK, KKK, KKRK (SEQ ID NO. 1), KKFRK (SEQ ID NO. 2), KGKRK (SEQ ID NO: 3), KKGRK (SEQ ID NO: 4), KKKGK (SEQ ID NO: 5), KKRKG (SEQ ID NO: 6), KKRKK (SEQ ID NO: 7), KKTRK (SEQ ID NO: 8), TKKRK (SEQ ID NO: 9), pkkkrkv (SEQ ID NO: 10), kkkRK (SEQ ID NO: 11), kkkrk (SEQ ID NO: 12), KKKRK (SEQ ID NO: 13), K(me)-K(me)-K(me)-R(me)-K(me) (SEQ ID NO: 14), TKKRK (SEQ ID NO: 15), KKKRKF (SEQ ID NO: 16), KKKRKR (SEQ ID NO: 17), PKKKRKV (SEQ ID NO: 18), RBKKRB (SEQ ID NO: 19), RBRRBR (SEQ ID NO: 20), YArVRRrGPR (SEQ ID NO: 21), RFGRK (SEQ ID NO: 22), KKKHH (SEQ ID NO: 15), KBKBKBRBK (SEQ ID NO: 23), RFKKRFK (SEQ ID NO: 24), RBKKBR (SEQ ID NO: 80), N(Lys)-N(Lys)-N(Lys)-N(Arg)-N(Lys) (SEQ ID NO: 25), N(Arg)-B-N(Arg)-N(Arg)-B-N(Arg) (SEQ ID NO: 26), or N(Lys)-N(Lys)-N(Lys)-N(Arg)-N(Lys) (SEQ ID NO: 27).

[0222] In embodiments, AAI comprises K. In embodiment, AAI comprises KK. In embodiments, AA I comprises RK In embodiments,?\A I comprises RFK In embodiments, AAI comprises KRK. In embodiments, AAI comprises KKK. In embodiments, AAI comprises KKRK (SEQ ID NO: 1). In embodiments, AAI comprises KKFRK (SEQ ID NO: 2). In embodiments, AAI comprises KGKRK (SEQ ID NO: 3). In embodiments, AAI comprisesKKGRK (SEQ ID NO: 4). In embodiments, AAI comprises KKKGK (SEQ ID NO: 5). In embodiments, AAI comprises KKRKK (SEQ ID NO: 7). In embodiments, AAI comprises KKRKG (SEQ ID NO: 6). In embodiments, AA1 comprises KKTRK (SEQ ID NO: 8). In embodiments, AA1 comprises TKKRK (SEQ ID NO: 9). In embodiments, AA1 comprises pkkkrkv (SEQ ID NO: 10)In embodiments, AA1 comprises kkkRK (SEQ ID NO: 11). In embodiments, AA1 comprises kkkrk (SEQ ID NO: 12). In embodiments, AA1 comprises kkkRK (SEQ ID NO: 11). In embodiments, AA1 comprises KKKRK (SEQ ID NO: 10). In embodiments, AA1 comprises KKKRK (SEQ ID NO: 13). In embodiments, AA1 comprises KKRK (SEQ ID NO: 1) In embodiments, AAI comprises K(me)-K(me)-K(me)-R(me)-K(me) (SEQ ID NO: 14). In embodiments, AAI comprises TKKRK (SEQ ID NO: 15). In embodiments, AAI comprises KKKRKF (SEQ ID NO: 16). In embodiments, AAI comprises KKKRKR (SEQ ID NO: 17). In embodiments, AAI comprises PKKKRKV (SEQ ID NO: 18). In embodiments, AAI comprises RBKKRB (SEQ ID NO: 19). In embodiments, AAI comprises RBRRBR (SEQ ID NO: 20). In embodiments, AAI comprises YArVRRrGPR (SEQ ID NO: 21). In embodiments, AAI comprises RFGRK (SEQ ID NO: 22). In embodiments, AAI comprises KKKHH (SEQ ID NO: 15) In embodiments, A AI comprises KBKBKBRBK (SEQ ID NO: 23). In embodiments, AAI comprises RFKKRFK (SEQ ID NO: 24). In embodiments, A AI comprises RBKKBR (SEQ ID NO: 80). In embodiments, A I comprises N(Lys)-N(Lys)-N(Lys)-N(Arg)-N(Lys) (SEQ ID NO: 25). In embodiments, AAI comprises N(Arg)-B-N(Arg)-N(Arg)-B-N(Arg) (SEQ ID NO: 26).Amino Acid(s): AA2, AA3, AA4, and combinations thereof

[0223] AA2, AA3, and AA4 are each independently an amino acid residue or a peptide that comprises 2 to 6 amino acid residues. The total number of amino acids in each of AA2, AA3, and AA4 can vary.

[0224] AA2 can include 1 to 6 amino acid residues. AA2 can include 1 amino acid residue. AA2 can include 2 amino acid residues. AA2 can include 3 amino acid residues. AA2 can include 4 amino acid residues. AA2 can include 5 amino acid residues. AA2 can include 6 amino acid residues.

[0225] AA3 can include 1 to 6 amino acid residues. AA3 can include 1 amino acid residue. AA3 can include 2 amino acid residues. AA3 can include 3 amino acid residues. A A3 can include 4amino acid residues. AA3 can include 5 amino acid residues. AA3 can include 6 amino acid residues.

[0226] AA4 can include 1 to 6 amino acid residues. AA4 can include 1 amino acid residue. AA4 can include 2 amino acid residues. AA4 can include 3 amino acid residues. AA4 can include 4 amino acid residues. AA4 can include 5 amino acid residues. AA4can include 6 amino acid residues.

[0227] The sum of amino acid residues in the combination of AA2, A A3, and AA4 present in the compound can vary, for example, from I to 18. The sum of amino acid residues in the combination of AA2, AA3, and AA4 present in the compound can be 1 to 16. The sum of amino acid residues in the combination of AA2, AA3, and AA4 present in the compound can be 1 to 14. The sum of amino acid residues in the combination of AA2, AA3, and AA4 present in the compound can be 1 to 12. The sum of amino acid residues in the combination of AA2, AA3, and AA4 present in the compound can be 1 to 10. The sum of amino acid residues in the combination of AA2, AA3, and?\A4 present in the compound can be 1 to 8. The sum of amino acid residues in the combination of AA2, AA3, and AA4 present in the compound can be 2 to 8. The sum of amino acid residues in the combination of AA2, AA3, and AA4 present in the compound can be 2 to 6. The sum of amino acid residues in the combination of AA2, AA3, and AA4 present in the compound can be 2 to 4. The sum of amino acid residues in the combination of AA2, AA3, and AA4 present in the compound can be 1, 2, 3, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14, 15, or 16.

[0228] In embodiments when a2 is 0, a3 is 1, and a4 is 0, AA3 can comprise 1 to 6 amino acid residues. In embodiments when a2 is 0, a3 is 1, and a4 is 0, AA3 comprises 1 amino acid residue. In embodiments when a2 is 0, a3 is 1, and a4 is 0, AA3 comprises 2 amino acid residues. In embodiments when a2 is 0, a3 is 1, and a4 is 0, A. A3 comprises 3 amino acid residues. In embodiments when a2 is 0, a3 is 1, and a4 is 0, AA3 comprises 4 amino acid residues. In embodiments when a2 is 0, a3 is 1, and a4 is 0, AA3 comprises 5 amino acid residues. In embodiments when a2 is 0, a3 is 1, and a4 is 0, AA3 comprises 6 amino acid residues.

[0229] In embodiments when a2 is 0, a3 is 1, and a4 is 1, the sum of amino acid residues in AA3 and AA4 is 2 or 3. In embodiments when a2 is 0, a3 is 1, and a4 is 1, the sum of amino acid residues in AA3 and AA4 is 2. In embodiments when a2 is 0, a3 is 1, and a4 is 1, the sum of amino acid residues in AA3 and AA4 is 3.

[0230] In embodiments when a2 is 1, a3 is 1, and a4 is 0, the sum of amino acid residues in AA3 and A 4 is 2 to 6. In embodiments when a2 is I, a3 is 1, and a4 is 0, the sum of amino acid residues in AA3 and AA4 is 3. In embodiments when a2 is 1, a3 is 1, and a4 is 0, the sum of amino acid residues in AA3 and AA4 is 4. In embodiments when a2 is 1, a3 is 1, and a4 is 0, the sum of amino acid residues in AA3 and AA4 is 5. In embodiments when a2 is 1, a3 is 1, and a4 is 0, the sum of amino acid residues in AA3 and AA4 is 6.

[0231] In embodiments, the sum of amino acid residues in AA3 and AA4 is 2 to 6. In embodiments, the sum of amino acid residues in AA3 and AA4 is 3. In embodiments, the sum of amino acid residues in AA3 and AA4 is 4, In embodiments, the sum of amino acid residues in AA3 and AA4 is 5. In embodiments, the sum of amino acid residues in AA3 and AA4 is 6.

[0232] In embodiments when a2 is 1, a3 is 0, and a4 is 0, AA2 comprises 1 amino acid residue.

[0233] At least one of AA2, AA3, and AA4 present in the compound comprises at least one hydrophobic or hydrophilic amino acid residue. In embodiments, at least one of AA2, AA3, and A 4 present in the compound comprises at least one hydrophobic amino acid residue. In embodiments, at least one of AA2, AA3, and AA4 present in the compound comprises at least one hydrophilic amino acid residue.

[0234] In embodiments, the combination of AA2, AA3, and AA4 present in the compound comprises two or more hydrophilic amino acid residues. In embodiments, the two or more hydrophilic amino acid residues may be a part of a single peptide in AA2, AA3, or AA4. For example, in embodiments where a2 is 1, a.3 is 1, or a4 is 1, one or more of AA2, AA3, and AA4 can include a peptide having two or more hydrophilic amino acid residues. In embodiments, one or both of AA3, and AA4 can include a peptide having two or more hydrophilic amino acid residues. Within a single AA2, A A3, or AA4 group present in a compound, the two or more hydrophilic amino acids may be contiguous or separated by one or more additional amino acid residues, such as one or more hydrophobic amino acid residues. In embodiments, the two or more hydrophilic amino acid residues may independently be present between AA2, AA3, and AA4 present in the compound. For example, in embodiments where a3 and a4 are 1, each of AA3 and AA4 can independently have one or more hydrophilic amino acid residues.Additionally, in embodiments where a2 and a3 are 1, each of AA2 and AA3 can independently have one or more hydrophilic amino acid residues.. In embodiments,each of AA3 and AA4 canindependently have one or more hydrophilic amino acid residues. In embodiments, each of AA2 and A A3 can independently have one or more hydrophilic amino acid residues.

[0235] In embodiments, the combination of AA2, AA3, and AA4 present in the compound comprises at least one hydrophobic amino acid residue. In embodiments, the combination of AA2, AA3, and AA4 present in the compound comprises two or more hydrophobic amino acid residues. In embodiments, the two or more hydrophobic amino acid residues may be a part of a single peptide in AA2, AA3, or AA4. For example, in embodiments where a2 is 1, a3 is 1, or a4 is 1, one or more of AA2, AA3, and AA4 can include a peptide having two or more hydrophobic amino acid residues. For example, in embodiments, AA3, AA4, or both can include a peptide having two or more hydrophobic amino acid residues. Within a single AA2, AA3, or AA4 group present in a compound, the two or more hydrophobic amino acids may be contiguous or separated by one or more additional amino acid residues, such as one or more hydrophilic amino acid residues. In embodiments, the two or more hydrophobic amino acid residues may independently be present in the combination of AA2, AA3, and AA4. For example, in embodiments of where a3 and a4 are 1, each of AA3 and AA4 can independently have one or more hydrophobic amino acid residues. Additionally, in embodiments of where a2 and a3 are 1, each of AA2 and AA3 can independently have one or more hydrophobic amino acid residues. In embodiments, A A3 and AA4 can each independently have one or more hydrophobic amino acid residues. In embodiments, AA3 and AA4 can each independently have one or more hydrophobic amino acid residues

[0236] In embodiments, the combination of AA2, AA3, and AA4 present in the compound comprises at least one hydrophilic amino acid residue and at least one hydrophobic amino acid residue.

[0237] The at least one hydrophilic amino acid residue and the at least one hydrophobic amino acid residue may be present in a single peptide in AA2, AA3, or AA4 present in the compound. For example, in embodiments where a2 is I, AA2 can include at least one hydrophilic amino acid residue and at least one hydrophobic amino acid residue. In embodiments of where a3 is 1, AA3 can include at least one hydrophilic amino acid residue and at least one hydrophobic amino acid residue. In embodiments of where a4 is 1, AA4 can include at least one hydrophilic amino acid residue and at least one hydrophobic amino acid residue. In embodiments of, AA3 can include at least one hydrophilic amino acid residue and at least one hydrophobic amino acidresidue. In embodiments, AA4 can include at least one hydrophilic amino acid residue and at least one hydrophobic amino acid residue.

[0238] The at least one hydrophilic amino acid residue and the at least one hydrophobic amino acid residue may independently be present in at least two of AA2, AA3, and AA4 present in the compound. For example, in embodiments when at least two of a2, a3 and a4 are 1, the at least one hydrophobic amino acid residue and the at least one hydrophilic amino acid residue may independently be present between at least two of AA2, AA3, and AA4. In embodiments, the at the at least one hydrophobic amino acid residue and the at least one hydrophilic amino acid residue may independently be present between AA3 and AA4.

[0239] The combination of AA2, AA3, and AA4 present in a compound of can have one or more hydrophilic amino acid residues and one or more hydrophilic amino acid residues. In some embodiments, the ratio of hydrophilic amino acid residues to hydrophobic amino acid residues in the combination of AA2, AA3, and AA4 present in the compound is 1 to 1. For example, in embodiments, the combination of AA2, AA3, and AA4 present in the compound has the same number of hydrophobic amino acids and hydrophilic amino acids. In other embodiments, the ratio of hydrophilic amino acid residues to hydrophobic amino acid residues in the combination of AA2, AA3, and AA4 present in the compound is not 1 to 1. For example, in embodiments, in embodiments, the combination of A2, A A3, and AA4 present in the compound has a different number of hydrophobic amino acids and hydrophilic amino acids.

[0240] In embodiments, the combination of AA2, AA3, and AA4 present in a compound has a greater number of hydrophilic amino acid residues than hydrophobic amino acid residues. As such, in embodiments, the combination of AA2, AA3, and AA4 present in the compound comprises 1.1 to 5 hydrophilic amino acid residues or more for every 1 hydrophobic amino acid. For example, in embodiments, the combination of AA2, AA3, and AA4 present in the compound comprises 2 hydrophilic amino acid residues and 1 hydrophobic amino acid residue; 3 hydrophilic amino acid residues and 1 or 2 hydrophobic amino acid residues; 4 hydrophilic amino acid residues, 1, 2, or 3 hydrophobic amino acid residues; or 5 hydrophilic amino acid residues,!, 2, 3, or 4 hydrophobic amino acid residues

[0241] In some embodiments, the combination of AA2, AA3, and AA4 present in a compound has a greater number of hydrophobic amino acid residues than hydrophilic amino acid residues. As such, in embodiments, the combination of AA2, AA3, and AA4 present in the compoundcomprises 1.1 to 3 hydrophobic amino acid residues for every 1 hydrophilic amino acid. For example, in embodiments, the combination of AA2, AA3, and AA4 present in the compound comprises 2 hydrophobic amino acid residues and 1 hydrophilic amino acid residue; 3 hydrophobic amino acid residues and 1 or 2 hydrophilic amino acid residues; or 4 hydrophobic amino acid residues and 2 or 3 hydrophilic amino acid residues.

[0242] One of more of AA2, AA3, and AA4 present in a compound can individually have a ratio of hydrophilic amino acid residues to hydrophobic amino acid residues of 1 to 1. For example, in embodiments when a2 is 1, AA2 can be a peptide having the same number of hydrophilic amino acid residues as hydrophobic amino acid residues. In embodiments, when a3 is 1, AA3 can be a peptide having the same number of hydrophilic amino acid residues as hydrophobic amino acid residues. In embodiments, when a4 is 1, AA4 can be a peptide having the same number of hydrophilic amino acid residues as hydrophobic amino acid residues. In embodiments, AA3 can be a peptide having the same number of hydrophilic amino acid residues as hydrophobic amino acid residues. In embodiments, AA4 can be a peptide having the same number of hydrophilic amino acid residues as hydrophobic amino acid residues

[0243] One of more of AA2, AA3, and AA4 present in a compound of can individually have a ratio of hydrophilic amino acid residues to hydrophobic amino acid residues that is not 1 to 1. For example, in embodiments when a2 is 1, AA2 can be a peptide having a different number of hydrophilic amino acid residues and hydrophobic amino acid residues. In embodiments when a3 is 1, AA3 can be a peptide having a different number of hydrophilic amino acid residues and hydrophobic amino acid residues. In embodiments when a4 is I, AA4 can be a peptide having a different number of hydrophilic amino acid residues and hydrophobic amino acid residues. In embodiments of, AA3 can be a peptide having a different number of hydrophilic amino acid residues and hydrophobic amino acid residues. In embodiments, AA4 can be a peptide having a different number of hydrophilic amino acid residues and hydrophobic amino acid residues.

[0244] One of more of AA2, AA3, and AA4 present in a compound of can individually have a ratio of hydrophilic amino acid residues to hydrophobic amino acid residues that is 1 to 1 and one or more of AA2, AA3, and AA4 present in the compound can individually have a ratio of hydrophilic amino acid residues to hydrophobic amino acid residues that is not 1 to 1. For example, in embodiments where a2 is 1 or 0, a3 is 1, and a4 is 1, either AA2 or AA4 can have a ratio of hydrophilic amino acid residues to hydrophobic amino acid residues that is 1 to 1 and the / 1AA2 or AA4 can have a ratio of hydrophilic amino acid residues to hydrophobic amino acid residues that is not I to 1. In embodiments where a2 is 1, a3 is 1, and a4 is 1 or 1, either A A2 or AA3 can have a ratio of hydrophilic amino acid residues to hydrophobic amino acid residues that is 1 to 1 and the AA2 or AA3 can have a ratio of hydrophilic amino acid residues to hydrophobic amino acid residues that is not 1 to 1. In embodiments, either AA3 or AA4 can have a ratio of hydrophilic amino acid residues to hydrophobic amino acid residues that is 1 to 1 and the AA3 or AA4 can have a ratio of hydrophilic amino acid residues to hydrophobic amino acid residues that is not 1 to 1.

[0245] In embodiments, each hydrophobic amino acid residue of each of AA2, A A3, and AA4 present in a compound is independently an aromatic amino acid residue; an uncharged, not aromatic, hydrocarbon amino acid residues; an amino acid residue that does not have a side chain, or any combination thereof. In embodiments, each hydrophobic amino acid residue of each of AA2, AA3, and AA4 present in the compound is independently an aromatic amino acid residue. In embodiments, each hydrophobic amino acid residue of each of AA2, AA3, and AA4 present in the compound is independently an uncharged, not aromatic, hydrocarbon amino acid residue or an amino acid residue that does not have a side chain. In embodiments, the combination of hydrophobic amino acid residues in the combination of each of AA2, AA3, and AA4 present in the compound is includes at least one aromatic amino acid residue and at least one amino acid residue having no side chain.

[0246] In embodiments, each aromatic amino acid residue of each of AA2, AA3, and AA4 present in a compound is selected from L- or D-phenylalanine, L- or D-naphthylalanine, L- or D-3-benzotheinyl alanine, L- or D-biphenylalanine, L- or D-tyrosine, L-or D-2-pyridylalanine, L-or -D-3 -pyridyl alanine, L- or D-4-pyridylalanine, L- or D- O, L-or D-u A®, iodophenylalanine, L- or D- 5-fluorotyrptophan, L- or D-tyrosine, L- or D-tyrptophan, L- or D-parachlorophenylalanine, L- or D-homophenylalnine, or L- or D-phenylglyine. In embodiments, each an uncharged, not aromatic, hydrocarbon amino acid residue in each of AA2, AA3, and AA4 in the compound is L- or D-valine or L- or D-proline. In embodiments, each amino acid residue having a no side chain is selected from glycine and beta¬ alanine.

[0247] In embodiments, each hydrophobic amino acid residue of each of AA2, AA3, and AA4 present in a compound is independently a charged amino acid. In embodiments, each charged amino acid residue hydrophobic in each of AA2, A A3, and AA4 in the compound is selectedQfrom L- or D-arginine, L- or D-homoarginine, L- or D-, L- or D-L- or D-lysine, L- or D-serine, L- or D-citrulline, or L- or D-glutamic acid.

[0248] In embodiments, the combination of AA2, AA3, and AA4 present in a compound comprises one or more hydrophilic amino acids independently selected from L- or D-arginine, L-A*.HN NHA.1 OH IY o H^SYHor D-homo-arginine, L- or D-, L- or D- 0, L- or D-citrulline, L- or D-lysine, L- or D-serine, L- or D-histidine, or L- or D-glutamic acid; and one or more hydrophobic amino acids independently selected from L-or D-phenylalanine, L- or D-naphthylalanine, L-or D-biphenylalanine, L- or D-3-benzotheinyl alanine, beta-alanine, L-or D-2-pyridylalanine, L- or -D-3 -pyridyl alanine, L- or D-4-pyridylalanine, L- or D-MXJ XrXl< H.2NX.. OHHH2hNlA Y / ^CNO, L -or D- ®, iodophenylalanine. L- or D- 5-fluorotyrptophan, L- or D-tyrptophan, L- or D-tyrosine, L- or D-parachlorophenylalanine, L- or D-homophenylalnine, or L- or D-phenylglyine, L- or D-proline, or L- or D-valine.

[0249] The absolute configuration of hydrophilic and / or hydrophobic amino acids in each of AA2, AA3, and AA4 present in a compound can vary. For example, in embodiments, each of AA2, AA3, and AA4 present in the compound can independently have any suitable combination of one or more of Agp, agp, R, r, FIoArg, Hoarg, F, f, B, b, E, e, Nal, nal, Bip, bip, Bta, bta, K, k, V, v, Cit, cit, G, Y, y, W, w, P, p, 2-Pyr, 2-pyr, 3-Pyr, 3-pyr, Tyr(Ph), tyr(Ph), Phe(3-CN), phe(3-CN), Trp(5-F), trp(5-F), Phe(I), phe(I), Pepa, dPcpa, Hph, dHph, Phg, or dPhg residues (see Table 1 for amino acid abbreviations). For example, in embodiments, each of AA2, AA3, and AA4 present in the compound can each independently comprises Bip, F, R, Bta, Nal, RF, RK, FK, K-Bip, R-Bip, R-Bta, R-Nal, V-Cit, Agp-Bip, Agp-F, Cit-F, EF, FR, R-(2-Pyr), R-(3-Pvr), R-(4-Pyr), R-(Phe(I)), RG, RL, R(m)e-F(me), R-(Phe(3-CN)), R-(Trp(5-F)), R-(Tyr(Ph)), RW, RY, SF, R-Bta-B, KKKRK (SEQ ID NO: 13) KRKR (SEQ ID NO. 28), RF-B, RFR, RPF, RK-Nal, rk-Nal, FGR, (HoArg)-Bip, R-Bip-R, RFK, RGF, R-Nal-R, BRB-Bip (SEQ ID NO: 29), KRK-Nal (SEQ ID NO: 30), kkkr-Nal (SEQ ID NO: 31), KFKF (SEQ ID NO: 32), RFRF (SEQ ID NO: 33), KKRK-Nal (SEQ ID NO: 34), Bip-BRBRB (SEQ ID NO: 35), Nal-BRBRB (SEQ ID NO: 36), KKKRK-Nal (SEQ ID NO: 37), RFE, R-(Phg), R-(Hph), (Pcpa)-F, BR-Bip-RB (SEQ ID NO: 85), RRFF (SEQ ID NO: 86), or FRF.

[0250] In embodiments, AA2 comprises Bip, F, R, Bta, Nal, RF, RK, FK, K-Bip, R-Bip, R-Bta, R-Nal, V-Cit, Agp-Bip, Agp-F Cit-F, EF, FR, R-(2-Pyr), R-(3-Pyr), R-(4-Pyr), R-(Phe(I)), RG, RL, R(me)-F(me), R-(Phe(3-CN)), R-(Trp(5-F)), R-(Tyr(Ph)), RW, RY, SF, R-Bta-B, KKKRK (SEQ ID NO: 13), KRKR (SEQ ID NO: 28), RF-B, RFR, RPF, RK-Nal, rk-Nal, FGR, (HoArg)-Bip, R-Bip-R, RFK, RGF, R-Nal-R, BRB-Bip (SEQ ID NO: 29), KRK-Nal (SEQ ID NO: 30), kkkr-Nal (SEQ ID NO: 31), KFKF (SEQ ID NO: 32), RFRF (SEQ ID NO. 33), KKRK-Nal (SEQ ID NO: 34), Bip-BRBRB (SEQ ID NO: 35), Nal-BRBRB (SEQ ID NO: 36), KKKRK-Nal (SEQ ID NO: 37), RFE, R-(Phg), R-(Hph), (Pcpa)-F, BR-Bip-RB (SEQ ID NO: 85), RRFF (SEQ ID NO: 86), or FRF.

[0251] In embodiments, AA3 comprises Bip, F, R, Bta, Nal, RF, RK, FK, K-Bip, R-Bip, R-Bta, R-Nal, V-Cit, Agp-Bip, Agp-F, Cit-F, EF, FR, R-(2-Pyr), R-(3-Pyr), R-(4-Pyr), R-(Phe(I)), RG, RL, R(me)-F(me), R-(Phe(3-CN)), R-(Trp(5-F)), R-(Tyr(Ph)), RW, RY, SF, R-Bta-B, KKKRK (SEQ ID NO: 13), KRKR (SEQ ID NO: 28), RF-B, RFR, RPF, RK-Nal, rk-Nal, FGR, (HoArg)-Bip, R-Bip-R, RFK, RGF, R-Nal-R, BRB-Bip (SEQ ID NO: 29), KRK-Nal (SEQ ID NO: 30), kkkr-Nal (SEQ ID NO: 31), KFKF (SEQ ID NO: 32), RFRF (SEQ ID NO: 33), KKRK-Nal (SEQ ID NO: 34), Bip-BRBRB (SEQ ID NO: 35), Nal-BRBRB (SEQ ID NO: 36), KKKRK-Nal (SEQ ID NO: 37), RFE, R-(Phg), R-(Hph), (Pcpa)-F, BR-Bip-RB (SEQ ID NO: 85), RRFF (SEQ ID NO: 86), or FRF,

[0252] In embodiments, AA4 comprises Bip, F, R, Bta, Nal, RF, RK, FK, K-Bip, R-Bip, R-Bta, KRKR, R-Nal, V-Cit, Agp-Bip, Agp-F, Cit-F, EF, FR, R-(2-Pyr), R-(3-Pyr), R-(4-Pyr), R-(Phe(I)), RG, RL, R(me)-F(me), R-(Phe(3-CN)), R-(Trp(5-F)), R-(Tyr(Ph)), RW, RY, SF, R-Bta-B, KKKRK (SEQ ID NO: 13), KRKR (SEQ ID NO: 28), RF-B, RFR, RPF, RK-Nal, rk-Nal, FGR, (HoArg)-Bip, R-Bip-R, RFK, RGF, R-Nal-R, BRB-Bip (SEQ ID NO: 29), KRK-Nal (SEQ ID NO: 30), kkkr-Nal (SEQ ID NO: 31), KFKF (SEQ ID NO: 32), RFRF (SEQ ID NO: 33), KKRK-Nal (SEQ ID NO: 34), Bip-BRBRB (SEQ ID NO: 35), Nal-BRBRB (SEQ ID NO: 36), KKKRK-Nal (SEQ ID NO: 37), RFE, R-(Phg), R-(Hph), (Pcpa)-F, BR-Bip-RB (SEQ ID NO: 85), RRFF (SEQ ID NO: 86), FRF.

[0253] In embodiments, each of AA2, AA3, and AA4 present in the compound of is independently selected from one of the following groups:(Group A) KKKRK (SEQ ID NO: 13), RK, RF, or R;(Group B) Bip-BRBRB (SEQ ID NO: 35), Nal-BRBRB (SEQ ID NO: 36), KKKRK-Nal (SEQ ID NO: 37), BRB-Bip (SEQ ID NO: 29), FK, K-Bip, kkkr-Nal (SEQ ID NO: 31), KKRK-Nal (SEQ ID NO: 30), KKRK-Nal (SEQ ID NO: 34), KRK-Nal (SEQ ID NO: 30), Nal, R-Bip, R-Bta, R-Bta-B, RF-B, RFR, RK-Nal, rk-Nal, R-Nal, V-Cit, Cit-R, EF, FGR, FR, (HoArg)-Bip, KRKR (SEQ ID NO: 28), R-(2-Pyr), R-(3-Pyr), R(4-Pyr), R-Bip-R, R-(Phe(I)), RFK, RFRF (SEQ ID NO: 33), RG, RGF, RL, R(rne)-F(me), R-Nal-R, R-(Phe(3-CN)), R-(Trp(5-F), R-(Tyr(Ph), RW, RY, SF, RPF, Agp-Bip, Agp-F, RFE, R-(Phg), R-(Hph), (Pcpa)-F, BR-Bip-RB (SEQ ID NO: 85), RRFF (SEQ ID NO: 86), or FRF; and(Group C) Bip, F, R, Bta, Nal, RF, or F.

[0254] In embodiments, AA2 comprises is KKKRK (SEQ ID NO: 13), RK, or RF. In embodiments, AA2 comprises is KKKRK (SEQ ID NO: 13). In embodiments, AA2 includes or is RK. In embodiments, AA2 comprises is KKKRK (SEQ ID NO: 13). In embodiments, AA2 comprises is RF In embodiments, AA2 comprises R.

[0255] In embodiments, AA3 comprises Bip-BRBRB (SEQ ID NO: 35), Nal-BRBRB (SEQ ID NO: 36), KKKRK-Nal (SEQ ID NO: 37), BRB-Bip (SEQ ID NO: 29), FK, K-Bip, kkkr-Nal (SEQ ID NO: 31), KKRK-Nal (SEQ ID NO: 34), KKRK-Nal (SEQ ID NO: 34), KRK-Nal (SEQ ID NO: 30), Nal, R-Bip, R-Bta, R-Bta-B, RF-B, RFR, RK-Nal, rk-Nal, R-Nal, or V-Cit. In embodiments, AA3 comprises is Bip-BRBRB (SEQ ID NO: 35), Nal-BRBRB (SEQ ID NO: 36), KKKRK-Nal (SEQ ID NO: 37), BRB-Bip (SEQ ID NO: 29), FK, K-Bip, kkkr-Nal (SEQ ID NO: 31), KKRK-Nal (SEQ ID NO: 34), KRK-Nal (SEQ ID NO: 30), Nal, R-Bip, R-Bta, R-Bta-B, RF-B, RFR, RK-Nal, rk-Nal, R-Nal, V-Cit, Cit-R, EF, FGR, FR, (HoArg)-Bip, KRKR (SEQ ID NO: 28), R-(2-Pyr), R-(3-Pyr), R(4-Pyr), R-Bip-R, R-(Phe(I)), RFK, RFRF (SEQ ID NO: 33), RG, RGF, RL, R(me)-F(N-me), R-Nal-R, R-(Phe(3-CN)), R-(Trp(5-F), R-(Tyr(Ph), RW, RY, SF, RPF, Agp-Bip, Agp-F, RFE, R-(Phg), R-(Hph), (Pcpa)-F, BR-Bip-RB (SEQ ID NO: 85), RRFF (SEQ ID NO: 86), or FRF.

[0256] In embodiments, AA3 comprises Bip-BRBRB (SEQ ID NO: 35). In embodiments, AA3 includes or is Nal-BRBRB (SEQ ID NO: 36). In embodiments, AA3 comprises KKKRK-Nal (SEQ ID NO: 37). In embodiments, AA3 includes or is BRB-Bip (SEQ ID NO: 29). In embodiments, AA3 comprises FK. In embodiments, AA3 compriseK-Bip. In embodiments, AA3 comprises kkkr-Nal (SEQ ID NO: 31). In embodiments, AA3 comprises KKRK-Nal (SEQ ID NO: 34). In embodiments, AA3 comprises KRK-Nal (SEQ ID NO: 30). In embodiments, AA3 comprises Nal. In embodiments, AA3 comprises R-Bip. In embodiments, AA3 comprises R-Bta. In embodiments, AA3 comprises R-Bta-B. In embodiments, AA3 comprises RF-B. In embodiments, AA3 comprises RFR. In embodiments, A A3 comprises RK-Nal. In embodiments, AA3 comprises rk-Nal. In embodiments, AA3 comprises R-Nal. In embodiments, AA3 comprises V-Cit. In embodiments, AA3 comprises Cit-R. In embodiments, AA3 comprises EF, In embodiments, AA3 comprises FGR. In embodiments, AA3 comprises FR. In embodiments, AA3 comprises (HoArg)-Bip. In embodiments, AA3 comprises KRKR (SEQ ID NO: 28). In embodiments, A. A3 comprisesR-(2-Pyr). In embodiments, AA3 comprises R-(3-Pyr). In embodiments, AA3 comprises R-(4-Pyr). In embodiments, AA3 comprises R-Bip-R Inembodiments, AA3 comprises R-(Phe(I)). Tn embodiments, AA3 comprises RFK. In embodiments, AA3 comprises RFRF (SEQ ID NO: 33). In embodiments, AA3 comprises RG. In embodiments, AA3 comprises RGF. In embodiments, AA3 comprises RL. In embodiments, AA3 comprises R(me)-F(me). In embodiments, AA3 comprises R-Nal-R. In embodiments, AA3 comprises R-(Phe(3-CN)). In embodiments, AA3 comprises R-(Trp(5-F)). In embodiments, AA3 comprises R-(Tyr(Ph)). In embodiments, AA3 comprises RW. In embodiments, AA3 comprises RY. In embodiments, AA3 comprises SF. In embodiments, AA3 comprises Agp-Bip. In embodiments, AA3 comprises RPF. In embodiments, AA3 comprises Agp-F. In embodiments, AA3 comprises RFE. In embodiments, AA3 comprises R-(Phg). In embodiments, AA3 comprises R-(Hph). In embodiments, AA3 comprises (Pcpa)-F. In embodiments, AA3 comprises R-(Hph). In embodiments, AA3 comprises BR-Bip-RB (SEQ ID NO: 85). In embodiments, AA3 comprises RRFF (SEQ ID NO: 86), In embodiments, A A3 comprises FRF.

[0257] In embodiments, AA4 comprises Bip, F, R, Bta, or Nal. In embodiments, AA4 comprises Bip. In embodiments, AA4 comprises F. In embodiments, AA4 comprises R. In embodiments, AA4 comprises Bta. In embodiments, AA4 comprises Nal. In embodiments, AA4 comprises RF. In embodiments, AA4 comprises F.

[0258] In embodiments where a2 is 0, a3 is I, and a4 is 0, AA3 comprises Bip-BRBRB (SEQ ID NO: 35), Nal-BRBRB (SEQ ID NO: 36), KKKRK-Nal (SEQ ID NO: 37), BRB-Bip (SEQ ID NO: 29), FK, K-Bip, Agp-F, kkkr-Nal (SEQ ID NO: 31), KKRK-Nal (SEQ ID NO: 34), KRK-Nal (SEQ ID NO: 30), Nal, R-Bip, R-Bta, R-Bta-B, RF-B, RFR, RK-Nal, rk-Nal, R-Nal, V-Cit, Cit-R, EF, FGR, FR, (HoArg)-Bip, KRKR (SEQ ID NO: 28), R-(2-Pyr), R-(3-Pyr), R(4-Pyr), R- Bip-R, R-(Phe(I)), RFK, RFRF (SEQ ID NO: 33), RG, RGF, RL, (Rme)-(Fme), R-Nal-R, R- (Phe(3-CN)), R-(Trp(5-F)), R-(Tyr(Ph)), RW, RY, SF, RPF, Agp-Bip, RFE, R-(Phg), R-(Hph), (Pcpa)-F, BR-Bip-RB (SEQ ID NO: 85), RRFF (SEQ ID NO: 86), or FRF.

[0259] In embodiments where a2 is 0, a3 is 1, and a4 is 1, AA3 comprises Bip-BRBRB (SEQ ID NO: 35), Nal-BRBRB (SEQ ID NO: 36), KKKRK-Nal (SEQ ID NO: 37), BRB-Bip (SEQ ID NO: 29), FK, K-Bip, Agp-F, kkkr-Nal (SEQ ID NO. 31), KKRK-Nal (SEQ ID NO: 34), KRK- Nal (SEQ ID NO: 30), Nal, R-Bip, R-Bta, R-Bta-B, RF-B, RFR, RK-Nal, rk-Nal, R-Nal, V-Cit, Cit-R EF, FGR, FR, (HoArg)-Bip, KRKR (SEQ ID NO: 28), R-(2-Pyr), R-(3-Pyr), R(4-Pyr), R-Bip-R, R-(Phe(I)), RFK, RFRF (SEQ ID NO: 33), RG, RGF, RL, (Rme)-(Fme), R-Nal-R, R- (Phe(3-CN)), R-(Trp(5-F)), R-(Tyr(Ph)), RW, RY, SF, RPF, Agp-Bip, RPF, Agp-Bip, RFE, R-(Phg), R-(Hph), (Pcpa)-F, BR-Bip-RB (SEQ ID NO: 85), RRFF (SEQ ID NO: 86), or FRF; and AA4 is comprises Bip, F, R, Bta, Nal, RF, or F.

[0260] In embodiments where a2 is 1, a3 is 0, and a4 is 0, AA2 comprises KKKRK (SEQ ID NO: 13), RK, orRF.

[0261] In embodiments a2 is 1, a3 is 1, and a4 is 0, AA2 comprises KKKRK, RK, RF, or R and AA3 comprises Bip-BRBRB (SEQ ID NO: 35), Nal-BRBRB (SEQ ID NO: 36), KKKRK-Nal (SEQ ID NO: 37), BRB-Bip (SEQ ID NO: 29), FK, K-Bip, Agp-F, kkkr-Nal (SEQ ID NO: 31), KKRK-Nal (SEQ ID NO: 34), KRK-Nal (SEQ ID NO: 30), Nal, R-Bip, R-Bta, R-Bta-B, RF-B, RFR, RK-Nal, rk-Nal, R-Nal, V-Cit, Cit-R, EF, FGR, FR, (HoArg)-Bip, KRKR (SEQ ID NO: 28), R-(2-Pyr), R-(3-Pyr), R(4-Pyr), R-Bip-R, R-(Phe(I)), RFK, RFRF (SEQ ID NO: 33), RG, RGF, RL, R(me)-F(me), R-Nal -R, R-(Phe(3-CN)), R-(Trp(5-F), R-(Tyr(Ph), RW, RY, SF, RPF, Agp-Bip, RPF, Agp-Bip, RFE, R-(Phg), R-(Hph), (Pcpa)-F, BR-Bip-RB (SEQ ID NO: 85), RRFF (SEQ ID NO: 86), or FRF.

[0262] In embodiments where AA3 and AA4 are present, AA3 comprises Bip-BRBRB (SEQ ID NO: 35), Nal-BRBRB (SEQ ID NO: 36), KKKRK-Nal (SEQ ID NO: 37), BRB-Bip (SEQ ID NO: 29), FK, K-Bip, Agp-F, kkkr-Nal (SEQ ID NO: 31), KKRK-Nal (SEQ ID NO: 34), KRK- Nal (SEQ ID NO: 30), Nal, R-Bip, R-Bta, R-Bta-B, RF-B, RFR, RK-Nal, rk-Nal, R-Nal, V-Cit, Cit-R, EF, FGR, FR, (HoArg)-Bip, KRKR (SEQ ID NO: 28), R-(2-Pyr), R-(3-Pyr), R(4-Pyr), R- Bip-R, R-(Phe(I)), RFK, RFRF (SEQ ID NO: 33), RG, RGF, RL, (Rme)-(Fme), R-Nal-R, R-(Phe(3-CN)), R-(Trp(5-F)), R-(Tyr(Ph)), RW, RY, SF, RPF, Agp-Bip, RPF, Agp-Bip, RFE, R-(Phg), R-(Hph), (Pcpa)-F, BR-Bip-RB (SEQ ID NO: 85), RRFF (SEQ ID NO: 86), or FRF; and AA4 comprises Bip, F, R, Bta, or Nal.

[0263] In embodiments, only one of AA2, AA3, and AA4 is present in the compound (e.g., only 1 of a2, a3, and a4 is 1) and is a single hydrophilic amino acid residue. In embodiments, a2 is 1, a3 is 0, a4 is 0, and AA2 is a single hydrophilic amino acid residue. In embodiments, single hydrophilic amino acid residue has an aromatic side chain. In embodiments, the single hydrophilic amino acid residue is D- or L-naphthyl alanine or D- or L-biphenylalanine.

[0264] In embodiments, two of AA2, AA3, and AA4 are present in the compound (e.g., 2 of a2, a3, and a4 are 1) and each of the two AA2, AA3, and AA4 groups present in the compound independently consist of a single hydrophilic amino acid residue. In embodiments, a2 is 1, a3 is 1, a4 is 0, and AA2 and AA3 consist of a single hydrophilic amino acid residue. In embodiments,each of the two single hydrophilic amino acids independently have an aromatic, side chain In embodiments, the two single hydrophilic amino acid residues are each independently D- or L-naphthylalanine or D- or L-biphenylalanine.cCPP (cyclic Cell Penetrating Peptide): R1, R2, R3, R4, Rs, R6, and R7

[0265] delivery constructs and therefore compounds that include a delivery construct include a cyclic cell penetrating peptide (cCPP). The cCPP of is formed from a cCPP bridging amino acid residue and the amino acid residues characterized by the R1, R2, R3, R4, R5, R6, and R7side chains. As such, R1, R2, R3, R4, R5, R6, and R7are each independently the side chain of an amino acid. The cCPP bridging amino acid residue is the amino acid residue connecting the amino acid residue characterized by the R1side chain and the amino acid residue characterized by the R7side chain. The cCPP is designed to facilitate cell membrane penetration of the compound to which it is attached.

[0266] The side chain of the cCPP bridging amino acid residue is covalently attached to the side chain of an exocyclic bridging amino acid residue. The exocyclic bridging amino acid residue is the amino acid residue that has a side chain covalently attached to the cCPP. For example, the coupling between the side chain of the cCPP bridging amino acid residue and the exocyclic' y NMbridging amino acid residue can be visualized as - "" " (a portion of a compound ) where the cCPP bridging amino acid residue is shown as connected to the cCPP (the partial circle), the exocyclic bridging amino acid residue is the amino acid residue having a backbone that is not within the cCPP (the carbonyl is not a part of the cCPP), n is integer from 0 to 3, and y is an integer from 1 to 5. The cCPP bridging amino acid residue can be characterized by n. The exocyclic bridging amino acid residue can be characterized by y. n can be 0. n can be 2. n can be 3. When n is 0, the bridging cCPP amino acid residue is asparagine. When n is i, the bridging cCPP amino acid residue is glutamine, y can be 1. y can be 2. y can be 3. y can be 4. y can be 5.When y is 4, the exocyclic bridging amino acid residue is lysine. In embodiments the bridging cCPP amino acid residue is glutamine (n is 1) and the bridging exocyclic amino acid residue is lysine (y is 4).

[0267] A cCPP connected to the larger compound can be denoted as JA(cyclo[XAXBXcXDXEXfXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with the side chains R1, R2, R3, R4, R5, R6, and R7, respectively; YAis the cCPP bridging amino acid residue; and JAis the exocyclic bridging amino acid residue. For example, XAis the amino acid residue having the side chain of Rl, XBis the amino acid residue having the side chain of R2, Xcis the amino acid residue having the side chain of R3, XDis the amino acid residue having the side chain of R4, XEis the amino acid residue having the side chain of R5, XFis the amino acid residue having the side chain of R6, and XGis the amino acid residue having the side chain of R7. In embodiments where JAis L-or D-lysine (K or k) and YAis L-or D-glutamine (Q or q),the cCPP can be denoted as K / k(cyclo[XAXBXcXDXEXFXGQ / q]).

[0268] In embodiments, though not shown in some Formulae, the amide nitrogen of an amino acid residue in a cCPP can be methylated (-CH3). Such amino acid residues can be described as the N-methylated amino acid name or amino acid shorthand followed by (N-me). For example, the cCPP can include N-methylated phenylalanine ((F(N-me), f(N-me))) or N-methylated glycine (G(N-me)).

[0269] R1, R2, R3, R4, R5, R6, and R7can be any combination of amino acid side chains. Similar to the AA2, AA3, and AA4 groups, the combination of hydrophilic and hydrophobic amino acid residues in the cCPP can influence the efficacy of the compound.

[0270] In embodiments, at least 2 of R1, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophobic amino acid residue. In embodiments, at least 3 of Rl, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophobic amino acid residue. In embodiments, at least 4 of R1, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophobic amino acid residue. In embodiments, at least 4 of R1, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophobic amino acid residue. In embodiments, 2 of R1, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophobic amino acid residue. In embodiments, 3 of R1, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophobic amino acid residue. In embodiments, 4 of R1, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophobic amino acid residue. In embodiments, 5 of R1, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophobic amino acid residue.

[0271] In embodiments, at least 2 of R1, R2, R3, R4, R3, R6, and R ' are the side chain of a hydrophilic amino acid residue In embodiments, at least 3 of R1, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophilic amino acid residue. In embodiments, at least 4 of R1, R2, R3, R4, R5, R6, and R' are the side chain of a hydrophilic amino acid residue. In embodiments, 2 of R1, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophilic amino acid residue. In embodiments, 3 of R1, R2, R3, R4, R5, R6, and R'' are the side chain of a hydrophilic amino acid residue. In embodiments, 4 of R1, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophilic amino acid residue.

[0272] In embodiments 3 of R1, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophobic amino acid residue and 4 of R1, R2, R3, R4, R5, R6, and R' are the side chain of a hydrophilic amino acid residue.

[0273] In embodiments 4 of R1, R2, R3, R4, R5, R”, and R7are the side chain of a hydrophobic amino acid residue and 3 of R1, R2, R5. R4, R5, R6, and R7are the side chain of a hydrophilic amino acid residue.

[0274] In embodiments 5 of R1, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophobic amino acid residue and 2 of R5, R2, R3, R4, R5, R6, and R7are the side chain of a hydrophilic amino acid residue.

[0275] In embodiments, for each R1, R2, R3, R4, R5, R6, and R7that is the side chain of a hydrophobic amino acid residue, the hydrophobic amino acid residue can be an aromatic amino acid residue; an uncharged, not aromatic, hydrocarbon amino acid residue; or an amino acid residue having no side chain. In embodiments, each aromatic amino acid of the cCPP is independently selected from L- or D-phenylalanine, L- or D-naphthylalanine, L- or D-3-benzotheinyl alanine, or L-or D-biphenylalanine. In embodiments, each uncharged, not aromatic, hydrocarbon amino acid residue of the cCPP is independently selected from L- or D-valine or L-or-D leucine. In embodiments, each hydrophobic amino acid residue in the cCPP that has no side chain is glycine.

[0276] In embodiments, for each R1, R2, R3, R4, R5, R6, and R7that is the side chain of a hydrophobic amino acid residue, the hydrophobic amino acid residue can be an aromatic amino acid residue; an uncharged, not aromatic, hydrocarbon amino acid residue; or an amino acid residue having no side chain. In embodiments, each aromatic amino acid of the cCPP is independently selected from L- or D-phenylalanine, L- or D-naphthylalanine, L- or D-3-benzotheinyl alanine, L-or D-biphenylalanine, L- or D-tyrosine, L-or D-2-pyridylalanine, L- or CMD-4-pyridylalanine, L-or D iodophenylalanine, L- or D- 5-tluorotyrptophan, or L- or D-para-chloropheny 1 alanine. In embodiments, when one of R1, R2, R3, R4, R5, R6, and R7is the side chain of phenylalanine, the amino acid is N-methylated phenylalanine. In embodiments, each uncharged, not aromatic, hydrocarbon amino acid residue of the cCPP is independently selected from L- or D-valine, L- or-D leucine, or L- or D-alanine. In embodiments, each hydrophobic amino acid residue in the cCPP that has no side chain is glycine.

[0277] In embodiments, for each R1, R2, R3, R4, R5, R6, and R7that is the side chain of a hydrophilic amino acid, the hydrophilic amino acid can be a charged amino acid residue. In embodiments, each charged amino acid in the cCPP is independently selected from L- or D-arginine or L- or D-histidine.

[0278] In embodiments, for each R!, R2, R3, R4, R5, R6, and R7that is the side chain of a hydrophilic amino acid, the hydrophilic amino acid can be a charged amino acid residue. In embodiments, each charged amino acid in the cCPP is independently selected from L- or D- MH2,. NH A HN NH J XXOHo arginine, L- or D-histidine, L- or D-, L- or D- O, or L- or D-citrulline.

[0279] In embodiments, for each R1, R2, R3, R4, R5, R6, and R7that is the side chain of a hydrophilic amino acid, the hydrophilic amino acid can be a charged amino acid residue. In embodiments, each, uncharged, not aromatic, hydrocarbon amino acid residue of the cCPP is independently selected from L- or D-valine, L- or-D leucine, or L- or D-alanine

[0280] In embodiments,R1, R2, and R are each independently a side chain of a hydrophobic amino acid residue;R5and R7are each independently a side chain of a hydrophilic amino acid residue; andR4and R6are each independently a side chain of a hydrophobic amino acid or the side chain of a hydrophilic amino acid residueIn embodiments,R1, R2, and R3are each independently a side chain of a hydrophobic amino acid residue where at least two of R1, R2, and R3are each independently an aromatic amino acid side chain optionally selected from the side chain of L- or D-phenylalanine or L- or D-3-benzotheinyl alanine;R5and R7are each independently a side chain of a charged amino acid residue, optionally selected from the side chain of L- or D-arginine, L- or D-citrulline, or L- or D-histidine; and R4and R6are each independently a side chain of a hydrophobic amino acid residue or a side chain of a hydrophilic amino acid residue.

[0281] In embodiments,R’, R2, and R3are each independently a side chain of a hydrophobic amino acid residue where at least two of R1, R2, and R3are each independently an aromatic amino acid side chain optionally selected from the side chain of L- or D-phenylalanine, L- or D-naphthylalanine, L- or D-3-benzotheinyl alanine, L-or D-biphenyl alanine, L- or D-tyrosine, L-or D-2-pyridylalanine, L- or CNf £ 1CN r CfHjN0HH2N ' ' rOHD-4-pyridylalanine, L-or D- O, O, iodophenylalanine, L- or D- 5 -fluor otyrp tophan, or L- or D-parachlorophenylalanine;R3and R7are each independently a side chain of a charged amino acid residue, optionally HH2HfC MHH2M^y0Hselected from the side chain of L- or D-arginine, L- or D-citrulline, L- or D-, L- orD-0, orL- or D-histidine; andR4and R6are each independently a side chain of a hydrophobic amino acid residue or a side chain of a hydrophilic amino acid residue,

[0282] In embodiments,R1, R2, and R3are each independently a side chain of a hydrophobic amino acid residue where two of R’, R2, and R3are each independently an aromatic amino acid side chain optionally selected from the side chain of L- or D-phenylalanine or L- or D-3-benzotheinyl alanine and where one of R1, R2, and R4is H;R5and R7are each independently a side chain of a charged amino acid, optionally selected from the side chain of L- or D-arginine, L- or D-citrulline, or L- or D-histidine; andR4and R6are each independently a side chain of a hydrophobic amino acid or a side chain of a hydrophilic amino acid.

[0283] In embodiments,R1, R2, and R3are each independently a side chain of a hydrophobic amino acid residue where two of R!, R2, and R3are each independently an aromatic amino acid side chain optionally selected from L- or D-phenylalanine, L- or D-naphthyl alanine, L- or D-3-benzotheinyl alanine,H2N L-or D-bi phenyl alanine, L- or D-tyrosine, L- or D-4-pyridylalanine, L-or D- b CNOHH2N- L- or D- O L- or D-iodophenylalanine, L- or D- 5-fluorotyrptophan, or L- or D-parachlorophenylalanine, and where one of R1, R2, and R3is H;R5and R7are each independently a side chain of a charged amino acid, optionally selected fromthe side chain of L- or D-arginine, L- or D-citrulline, L- or D-, L- or D-0, or L- or D-histidine; andR4and R6are each independently a side chain of a hydrophobic amino acid or a side chain of a hydrophilic amino acid.

[0284] In embodiments,R1, R2, and R3are each independently a side chain of a hydrophobic amino acid where at least two of R1, R2, and R3are each independently an aromatic amino acid side chain optionally selected from the side chain of L- or D-phenylalanine or L- or D-3-benzotheinyl alanine; R5and R7are each independently a side chain of a charged amino acid, optionally selected from the side chain of L- or D-arginine, L- or D-citrulline, or L- or D-histidine, andR4and R6are each independently a side chain of a charged hydrophilic amino acid optionally selected from L-or D-arginine, L-or D-citrulline, or L-or D-histidine.

[0285] In embodiments,R1, R2, and R3are each independently a side chain of a hydrophobic amino acid where at least two of R1, R2, and R3are each independently an aromatic amino acid side chain optionally selected from the side chain of L- or D-phenylalanine or L- or D-3-benzotheinyl alanine, R5and R7are each independently a side chain of a charged amino acid, optionally selected from the side chain of L- or D-arginine, L- or D-citrulline, or L- or D-histidine, andR4and R6are each independently H or a side chain of a hydrophobic amino acid having a hydrocarbon side chain and no aromatic group, the hydrophobic amino acid optionally selected from L- or D-valine or L-or D-leucine.

[0286] In embodiments,R1, R2, and R3are each independently a side chain of a hydrophobic amino acid where at least two of R1, R2, and R3are each independently an aromatic amino acid side chain optionally selected from the side chain of L- or D-phenylalanine or L- or D-3-benzotheinyl alanine;R5and R7are each independently a side chain of a charged amino acid, optionally selected from the side chain of L- or D-arginine, L- or D-citrulline, or L- or D-histidine, andR4and R6are each H.

[0287] In embodiments,R1, R2, and R3are each independently a side chain of a hydrophobic amino acid where at least two of R1, R2, and R3are each independently an aromatic amino acid side chain optionally selected from the side chain of L- or D-phenylalanine, L- or D-3-benzotheinyl alanine, L- or D-A„. OH H2N |p naphthylalanine, L- or D-4-pyridylalanine, L - or D-tyrosine, L-or D- O, L- orA y OHD- O, or L- or D-parachlorophenylalanine;R5and R7are each independently a side chain of a charged amino acid, optionally selected fromHN A NHX OH HJJN y the side chain of L- or D-arginine, L- or D-citrulline, L- or D-, L- or D- H2IY^NHA OHH2r YO, or L- or D-histidine; andR4and R6are each H.

[0288] In embodiments,R1, R, and R3are each independently a side chain of a hydrophobic amino acid;at least two of R1, R2, and R3are each independently an aromatic amino acid side chain optionally selected from the side chain of L- or D-valine, L- or-D leucine, or L- or D-alanine; one of R1, R2, and R3is H, and one of R1, R2, and R3is an aromatic amino acid side chain optionally selected from the side chain of L- or D-phenylalanine;R3and R7are each independently a side chain of a charged amino acid, optionally selected from J.the side chain of L- or D-arginine, L- or D-citrulline, L- or D- $ L~ or D- H2N^HH1HS2 wN A YO, or L- or D-histidine; andR4and R6are each H.

[0289] In embodiments,R1is H or a side chain or an aromantic amino acid optionally selected from L- or D-phenylalanine orL- or D-3-benzotheinyl alanine;R2is H or a side chain or an aromantic amino acid optionally selected from L- or D-phenylalanine orL- or D-3-benzotheinyl alanine;R3is a side chain of an aromatic amino acid optionally selected from optionally selected from L-or D-phenylalanine orL- or D-3-benzotheinyl alanine;R4is H or a side chain of a non-aromatic amino acid optionally selected from L- or D-valine, L-or D-leucine, or L- or D-arginine;R5is a side chain of a charged amino acid optionally selected from D- or L-arginine or L- or D-histidine;R6is H or ta side chain of a non-aromatic amino acid optionally selected from L- or D-valine, L-or D-leucine, or L- or D-arginine; andR7is a side chain of a charged amino acid optionally selected from D- or L-arginine or L- or D-histidine.

[0290] In embodiments,R1, R3, R5, and R' are each independently a H or a side chain of a hydrophobic amino acid residue; andR2, R4, and R6are each independently a side chain of hydrophilic amino acid residue.

[0291] In embodiments,R1, R, R\ and R' are each independently H or a side chain of a hydrophobic amino acid residue optionally selected from D- or L-phenylalanine; andR2, R4, and R6are each independently a side chain of hydrophilic amino acid residue optionally selected from D- or L-arginine.

[0292] In embodiments,R1, R2, R4, R5, and Rzare each independently H or a side chain of a hydrophobic amino acid residue; andR3and R6are each independently a side chain of hydrophilic amino acid residue.

[0293] In embodiments,R1, R2, R4, R3, and R7are each independently H or a side chain of a hydrophobic amino acid residue optionally selected from D- or L-phenylalanine, andR3and R6are each independently a side chain of hydrophilic amino acid residue optionally selected from D- or L-arginine.

[0294] In embodiments,R1is H or the side chain of L- or D-3-benzotheinyl alanine or L- or D-phenylalanine;R2is H or the side chain of L- or D-3-benzotheinyl alanine or L- or D-phenylalanine;R3is II or the side chain of L- or D-3-benzotheinyl alanine or L- or D-phenylalanine,R4is H or the side chain of L- or D-leucine, L- or D-valine, L- or D-histidine, and L- or D-arginine;R5is the side chain of L- or D-arginine or L- or D-histidine;R6is H or the side chain L- or D-leucine, L- or D-valine, L- or D-histidine, or L- or D-arginine; andR7is the side chain or L- or D-arginine or L- or D-histidine.

[0295] In embodiments.R1is H or the side chain of L- or D-3-benzotheinyl alanine, L- or D-phenylalanine, L- or D-4-pyridylalanine, L- or D-alanine, L- or D or D-parachlorophenylalanine;R2is H or the side chain of L- or D-3-benzotheinyl alanine, L- or D-tyrosine, L- or D-alanine, or L- or D-phenylalanine;R3is H or the side chain of L- or D-3-benzotheinyl alanine, L- or D-phenylalanine, L- or D-tyrosine, L- or D-4-pyridylalanine, L- or D-alanine, L- or D- L- or D- CNO, or L- or D-parachlorophenylalanine;R4is H or the side chain of I - or D-leucine, L- or D-valine, L- or D-histidine, and L- or D-arginine;R5is the side chain of L- or D-arginine, L- or D-histidine, c L- or D-citrulline, L- or D-hlHR6is H or the side chain of L- or D-leucine, L- or D-valine, L- or D-histidine, or L- or D-arginine; andR7is the side chain or L- or D-arginine, L- or D-histidine, L- or D-citrulline, L- or D-HNor L- or D-

[0296] In embodiments,R1is H or the side chain of L- or D-3-benzotheinyl alanine or L- or D-phenylalanine;R2is H or the side chain of L- or D-phenylalanine;R3is the side chain of L- or D-3-benzotheinyl alanine or L- or D-phenylalanine;R'1is H or the side chain of L- or D-leucine, L- or D-arginine, or L- or D-valine;R3is the side chain of L- or D-arginine or L- or D-histidine;R6is H or the side chain of L- or D-leucine, L- or D-valine, or L- or D-arginine; andR7is the side chain or L- or D-arginine or L- or D-histidine.

[0297] In embodiments,R1is H or the side chain of L- or D-3-benzotheinyl alanine, phenylalanine, L- or D-4- CNr Cl CN r Ct.... X / OH A. OH pyridylalanine, L- or D-alanine, L- or D- O, L- or D- O, or Lor D-parachlorophenyl alanine;R2is H or the side chain of L- or D-3-benzotheinyl alanine, L- or D-alanine, L- or D-phenylalanine, L- or D-arginine, L- or D-tyrosine, or L- or D-arginine;R3is H or the side chain of L- or D-3-benzotheinyl alanine, L- or D-alanine, L- or D-phenylalanine, L- or D-4-pyridylalanine, L- or D-alanine, L- or D-tyrosine, L- or D- CN£1 Ct, > OH A. OH naphthylalanine, L- or D- O, L- or D- O, L- or D-parachlorophenylalanine, or L- or D-arginine;R4is H or the side chain of L- or D-leucine, L- or D-valine, L- or D-histidine, and L- or D-arginine;R5is the side chain of L- or D-arginine, L- or D-histidine, L- or D-citrulline, L- or D- NH2A OH HX Y, L- or D- or L- or D-phenylalanine;R6is H or the side chain of L- or D-leucine, L- or D-valine, L- or D-histidine, or L- or D-arginine; andR7is H or the side chain, L- or D-arginine, L- or D-histidine, L- or D-citrulline, L- or D-HN" MHJ X OHY® or L- or D- 0

[0298] In embodiments, R3and R7are the side chain of arginine, R4and R6are H or an amino acid side chain and two of R1, R2, and R3, are, independently the side chain of phenylalanine and one of R1, R2, and R3is I I or R1, R2, and R3are the side chain of phenylalanine.

[0299] In embodiments, the cCPP can have the sequence cyclo[Bta-G-Bta-GRGRQ] (SEQ ID NO: 38), cyclo[FfFGRGRQ] (SEQ ID NO: 39), cyclo[FGFGRGRQ] (SEQ ID NO: 40), cyclofFGFLRLRQ] (SEQ ID NO: 41), cyclo[FGFRHRHQ] (SEQ ID NO: 42), cyclofFGFVRVRQ] (SEQ ID NO: 43), cydofGfFGrGrQ] (SEQ ID NO: 44), cyclo[fGfrrrrQ] (SEQ ID NO: 45), cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ] (SEQ ID NO: 46), cyclofAGFGRGRQ] (SEQ ID NO: 47), cyclo[FFFGRGRQ] (SEQ ID NO: 48), cyclofFFGRRGQ] (SEQ ID NO: 49), cyclofFGAGRGRQ] (SEQ ID NO: 50), cyclo[FGFG-Cit-GRQ] (SEQ ID NO 51), cyclo[FGFGRG-Cit-Q] (SEQ ID NO: 52), cyclofFGFGRrRQ] (SEQ ID NO: 53), cyclo[FRFRFRFQ] (SEQ ID NO: 54), cyclo[G-f(N-me)-FGrGrQ] (SEQ ID NO: 55), cyclo[Gt-Nal-GrGrQ] (SEQ ID NO: 56), cyclo[GFRGFRGQ] (SEQ ID NO: 57), cyclofGyYGrGrQ] (SEQ ID NO: 58), and cyclo[(Phe(4-CN))-G-(Phe(4-CN))-GRGRQ] (SEQ ID NO: 59), cyclo[FGF-G(N-me)-RGRQ] (SEQ ID NO: 60), cyclo[F-G(N-me)-FGRGRQ] (SEQ ID NO: 61),cyclofFAFARGRQ] (SEQ ID NO: 62), cyclo[FGFG-Agp-G-Agp-Q] (SEQ ID NO: 63), cyclo[(Pcpa)-G-(Pcpa)-GRGRQ] (SEQ ID NO: 64), cyclofGFFGRGRQ] (SEQ ID NO: 65), cyclo[GRFGRFGQ] (SEQ ID NO: 66), cyclo[RFGGRFGQ] (SEQ ID NO: 67), cyclo[FGFRRRRQ] (SEQ ID NO: 81), cyclo[fffrrrrQ] (SEQ ID NO: 82), cyclo[fGfGrGrQ] (SEQ ID NO: 83), or cyclofFGRGFGRQ] (SEQ ID NO: 84), where Q is the cCPP bridging amino acid. In embodiments, the cCPP has the sequence cyclo[Bta-G-Bta-GRGRQ] (SEQ ID NO: 38). In embodiments, the cCPP has the sequence cyclo[FfFGRGRQ] (SEQ ID NO: 39). In embodiments, the cCPP has the sequence cyclo[FGFGRGRQ] (SEQ ID NO: 40). In embodiments, the cCPP has the sequence cyclo[FGFLRLRQ] (SEQ ID NO: 41). In embodiments, the cCPP has the sequence cyclo[FGFRHRHQ] (SEQ ID NO: 42). In embodiments, the cCPP has the sequence cyclofFGFVRVRQ] (SEQ ID NO: 43). In embodiments, the cCPP has the sequence cyclo[GfFGrGrQ] (SEQ ID NO: 44). In embodiments, the cCPP has the sequence cyclo[fGfrrrrQ] (SEQ ID NO: 45). In embodiments, the cCPP has the sequence cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ] (SEQ ID NO: 46). In embodiments, the cCPP has the sequence cyclo[AGFGRGRQ] (SEQ ID NO: 47). In embodiments, the cCPP has the sequence cyclofFFFGRGRQ] (SEQ ID NO: 48). In embodiments, the cCPP has the sequence cyclo[FFGRRGQ] (SEQ ID NO: 49). In embodiments, the cCPP has the sequence cyclofFGAGRGRQ] (SEQ ID NO: 50). In embodiments, the cCPP has the sequence cyclo[FGFG-Cit-GRQ] (SEQ ID NO: 51). In embodiments, the cCPP has the sequence cyclo[FGFGRG-Cit-Q] (SEQ ID NO: 52). In embodiments, the cCPP has the sequence cyclofFGFGRrRQ] (SEQ ID NO: 53). In embodiments, the cCPP has the sequence cyclo[FRFRFRFQ] (SEQ ID NO: 54). In embodiments, the cCPP has the sequence cyclo[G-f(N-me)-FGrGrQ] (SEQ ID NO: 55). In embodiments, the cCPP has the sequence cyclo[Gf-Nal-GrGrQ] (SEQ ID NO: 56). In embodiments, the cCPP has the sequence cyclo[GFRGFRGQ] (SEQ ID NO: 57). In embodiments, the cCPP has the sequence cyclo[GyYGrGrQ] (SEQ ID NO: 58). In embodiments, the cCPP has the sequence cyclo[(Phe(4-CN))-G-(Phe(4-CN))-GRGRQ] (SEQ ID NO: 59). In embodiments, the cCPP has the sequence cyclo[FGF-G(N-me)-RGRQ] (SEQ ID NO: 60). In embodiments, the cCPP has the sequence cyclo[F-G(N-me)-FGRGRQ] (SEQ ID NO: 61). In embodiments, the cCPP has the sequence cyclo[FAFARGRQ] (SEQ ID NO: 62). In embodiments, the cCPP has the sequence cyclo[FGFG-Agp-G-Agp-Q] (SEQ ID NO: 63). In embodiments, the cCPP has the sequence cyclo[(Pcpa)-G-(Pcpa)-GRGRQ] (SEQ IDNO: 64). In embodiments, the cCPP has the sequence cyclo[GFFGRGRQ] (SEQ ID NO: 65). In embodiments, the cCPP has the sequence cyclofGRFGRFGQ] (SEQ ID NO: 66), In embodiments, the cCPP has the sequence cyclo[RFGGRFGQ] (SEQ ID NO: 67). In embodiments, the cCPP has the sequence cyclo[FGFRRRRQ] (SEQ ID NO: 81) In embodiments, the cCPP has the sequence cyclo[fffrrrrQ] (SEQ ID NO: 82). In embodiments, the cCPP has the sequence cyclo[fGfGrGrQ] (SEQ ID NO: 83). In embodiments, the cCPP has the sequence cyclo[FGRGFGRQ] (SEQ ID NO: 84).Reactive Handle: M

[0300] In embodiments, a compound including a delivery' construct includes a reactive handle. A compound including a delivery construct and a reactive handle can be conjugated through reaction of the reactive handle with a complementary reactive handle of a cargo to form another compound that includes the delivery construct, sometimes called a delivery construct-cargo conjugate or cargo-conjugate. The reactive handle (M) may be a part of a defined moiety in the compound or the reactive handle may be an additional moiety,

[0301] In embodiments, M is OH. In embodiments when M is OH, the OH may be a part of a carboxylic acid. For example, when a delivery construct includes a terminalH / • ' r ysr® (p and s are defined here), where * indicates the attachment to the rest of the delivery construct, an OH (M) can be appended to the terminal carbonyl. In embodiments, when a delivery construct includes a terminal amino acid residue having a terminal carboxylic acid group, l can be I and M can be denoted as OH where the OH is a part of the terminal carboxylic acid group.

[0302] In embodiments, M is OH. In embodiments when M is OH, the OH may be a part of a carboxylic acid. For example, when a delivery construct includes a terminalH,,*■§ O) <•w(p and s are defined here), where * indicates the attachment to the rest of the delivery construct, an OH (M) can be appended to the terminal carbonyl. In embodiments, when a delivery construct includes a terminal amino acid residue having aterminal carboxylic acid group, m l can be 1 and M can be denoted as OH where the OH is a part of the terminal carboxylic acid group.' HH1

[0303] In embodiments when ml is 1, M comprisesO for example,uorHO, where y" is an integer from 1-4. y" can be 1. y" can be 2. y" can be 3. y" can be 4. When y" is 4, M can be called azidolysine. In embodiments when ml is 1, M can comprises2 where y" is an integer from 1-4. In embodiments when ml is 1, M compriseswhere y" is an integer from 1-4. In embodiments when ml is 1, M comprisesNH2where y" is an integer from 1-4.

[0304] Examples of compounds of Formula III include those listed in Tables 9A-9C and examples of compounds of Formula IV include those listed in Table 9D In Tables 9A-9D, Ac is -C(O)CH3; the cCPP is written as JA(cyclo[XAXBXcXDXEXFXGYA]) where X '. XB, Xc, XD, XE, X1, and XGare amino acid residues with the side chain R1, R2, R3, R4, R5, R6, and R7, respectively, YAis the cCPP bridging amino acid residue, and JAis the bridging exocyclic amino acid residue (see, for example, the cCPP description herein); “miniPEG2” indicates -(CH2-CH2-O)2-CH2-CO-; and “PEG#” indicates --(CH2-CH2-O)#-CH2-CO- or (CH2-CH2-O)#-CH2-CH2- CO- where # indicates to the number of -CH2-CH2-O- units. In Tables 9A-9D when the compound includes a terminal amino acid residue, M is an OH of a carboxylic acid of the terminal amino acid residue. In Tables 9A-9D when the compound includes a terminal “PEG#”, M is an OH appended to the -CO- portion of “PEG#.” In embodiments of the compounds ofTables 9A-9D, each instance of “PEG?.” refers to ~-(CH?-CH?-O)2-CH2-CO- (i.e., “miniPEG?”) and each instance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2. In embodiments of the compounds of Tables 9A-9D, each instance of “PEG2” refers to -(CH?-CH2-O)2-CH2-CH2-CO- and each instance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2.Table 9A.SEQ IDNo. Compound including a delivery constructNOs: Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Bip-BRBRB-M18, 40, LI (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-Bip- 35 BRBRB-M)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal-BRBRB-M18, 40, 1.2 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal- 36 BRBRB-M)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-B-ML3 18, 40 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-B-M) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BRB-Bip-Al 13, 40, L4(Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-BRB-Bip-M) 29 Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG12-BR-Bip-RB-M18, 40, L5 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEG 12-BR-Bip-RB- 85 M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-B-ML6 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-B-M)Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ]> PEGs-RF-ML7 18, 38 (Ac-PKKKRKV-miniPEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-RF-M) Ac-KKKRK-PEG2-K(cyclo[GfFGrGrQ])-PEG8-RF-ML8 13, 44 (Ac-KKKRK-miniPEG2-K(cyclo[GfFGrGrQ])-PEGg-RF-M)Ac-kkkRK-PEG2-K(cyclo[GfFGrGrQ])-PEG8-RF-ML9 11, 44 (Ac-kkkRK-miniPEG2-K(cyclo[GfFGrGrQ])-PEG8-RF-M)Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-MLIO 18, 38 (Ac-PKKKRKV-miniPEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-M)Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-K-Bip-MLil 20, 40 (Ac-RBRRBR-miniPEG2-K(cydo[FGFGRGRQ])-PEG8-K-Bip-M)Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-ML12 12, 40 (Ac-kkkrk-miniPEG₂-K(cyclo[FGFGRGRQ])-PEG8-RF-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-ML13 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-rf-MLI 4 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-rf-M)L15 Ac-RBKKBR-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-M 80, 40SEQ I D No. Compound including a delivery constructNOs: Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FK-ML16 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-FK-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-ML17 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-M)Ac-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])- PEG8-RF-ML18 14, 40 (Ac-K(me)-K(me)-K(me)-R(me)-K(me)-miniPEG2- K(cyclo|FGFGRGRQ])-PEG8-RF-M)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Val-Cit-ML19 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-Val-Cit- 18, 40 M)Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-ML20 21, 40 (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-M)L21 Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG8-Bip-M 20, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-PEG2-ML22 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-PEG2-M) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG2-ML23 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-R-Bta- 13, 40 miniPEG2-M)Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-ML24 20, 40 (Ac-RBRRBR-K(cyclo[FGFGRGRQ])-miniPEG2-KF-PEG4-M)Ac-KKKRK-PEG2-K(cyclo[FGFRHRHQ])-PEG2-RF-PEG4-ML25 (Ac-KKKRK-miniPEG2-K([cyclo[FGFRHRHQ])-miniPEG2-RF-PEG4- 13, 42 M)L25.1 Ac-KKKRK-PEG2-K(cyclo[FGFRHRHQ])-PEG2-RF-PEG4-K(N3)-NH213, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bta-PEG2-ML26 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ)-PEG4-R-Bta- 21, 39 miniPEG2-M)Ac-YArVRRrGPR-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4-ML27 (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FfFGRGRQ])-miniPEG2-RF- 40, 18 PEG4-M)Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEG8-ML28 13, 40 (Ac-K(cyclo[FGFGRGRQ])-miniPEG2-PKKKRKV-PEG8-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-Bip-ML29 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-rf-PEG4- 18, 40 Bip-M)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-F-M18, 40, L30 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 35 PEG4-F-M)Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bta-ML31 (Ac-RBRRBR-miniPEG₂-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 20, 40Bta-M)SEQ I D No. Compound including a delivery constructNOs: Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Nal-ML32 (Ac-KKKRK-miniPEG2-K([cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 13, 40 Nal-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG4-Nal-ML33 (Ac-KKKRK-miniPEG2-K([cyclo[FGFGRGRQ])-PEG8-RF-PEG4-Nal- 13, 40 M)Ac-PKKKRKV-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG2-Nal-ML34 (Ac-PKKKRKV-miniPEG2-K(cyclo[FfFGRGRQ])-miniPEG2-RF- 18, 39 miniPEG2-Nal-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-Bip-ML35 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-KF-PEG4- 13, 40 Bip-M)Ac-KKKRK-PEG2-K(cyclo[FfFGRGRQ])-PEGi2-(2-Nal)-PEG2-(2-Nal)- ML36 13, 39 (Ac-KKKRK-miniPEG2-K(cyclo[FfFGRGRQ])-PEGi2-[2-Nal]- miniPEG2-[2-Nal]-M)Ac-KKKRK-PEG2-K(cyclo[FfFGRGRQ])-PEGl2-Bip-PEG2-Bip-ML37 (Ac-KKKRK-miniPEG2-K(cyclo[FfFGRGRQ])-PEG12-Bip-miniPEG2- 13, 39 Bip-M)Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEG12-Nal-PEG2-Nal-ML38 20, 39 (Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEG12-Nal-miniPEG2-Nal-M)Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-PEG2-Nal-ML39 20, 40 (Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-miniPEG2-Nal-M)L40 Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-M 1, 40 L41 Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-M 12, 40 L42 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-M 13, 40 L43 Ac-TKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 9, 40 L44 Ac-KKTRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 8, 40 L45 Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG4-M 21, 40 L46 Ac-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ])-PEG2-RG-PEG4-M 13, 55 L47 Ac-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ])-PEG2-RF-PEG4-M 13, 55 L48 Ac-KKKRK-PEG2-K(cyclo[Gf-Nal-GrGrQ])-PEG2-RF-PEG4-M 13, 56 L49 Ac-KKKRK-PEG2-K(cyclo[GyYGrGrQ])-PEG2-RF-PEG4-M 13, 58 L50 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-PEG4-M 13, 40 L51 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG2-M 13, 40 L52 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-M 13, 40 L53 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-PEG4-M 13, 40 L54 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFR-PEG4-M 13, 40 L55 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-R-PEG4-M 13, 40L56 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-R-PEG4-M 13, 40SEQ I D No. Compound including a delivery constructNOs: L57 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4-M 13, 40 L58 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEGB-M 13, 40 L59 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-M 13, 40 L60 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ] )-PEG2-R-(3 -Pyr)-PEG4-M 13, 40 L61 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(2-Pyr)-PEG4-M 13, 40 L62 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(4-Pyr)-PEG4-M 13, 40 L63 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phe(3-CN)-PEG4-M 13, 40 L64 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Trp(5-F> PEG4-M 13, 40 L65 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Tyr(Ph)-PEG4-M 13, 40 L66 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-HoArg-Bip-PEG4-M 13, 40 L67 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-rf-PEG4-M 13, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R(me)-F(N-me)- L68 13, 40 PEG4-MAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-(4-Pyr)-PEG4-Nal- L69 13, 40 ML70 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4-F-M 13, 40 Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-RF- L71 13, 46 PEGi-MAc-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-R-Bip- 13, 46 L72PEG4-ML73 Ac-KKKRK-PEG4-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 13, 40 L74 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG4-M 13, 4013, 40, L75 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFRF-PEG4-M33 13, 40, L76 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RRFF-PEG4-M86 L77 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-M 40 L78 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KFKF-PEG4-M 40, 32 L79 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-EF-PEG4-M 13, 40 L80 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-PEG4-M 13, 40 L81 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FGR-PEG4-M 13, 40 Ac-KKKRK-PEG2-K(cyclo[Phe(4-CN)-G-Phe(4-CN)-GRGRQ])-PEG2- L82 13, 59 RF-PEG4-ML83 Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-K-PEG4-M 1, 40 L84 Ac-KKRK-PEG2-K(cyclo[FGFGRrRQ])-PEG2-RF-PEG4-M 1, 53 L85 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ]-PEG2-R-F(I)-PEG4-M 13, 40 L86 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FR-PEG4-M 13, 40 L87 Ac-KKKRKR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-F-PEG4-M 17, 40 L88 Ac-KKKRKF-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG4-M 16, 40L89 Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-M 13, 57SEQ ID No. Compound including a delivery constructNOs: L90 Ac-KKKRK-PEG2-K(cyclo[FFGRRGQ])-PEG2-RF-PEG4-M 13, 49 L91 Ac-KGKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 3, 40 L92 Ac-KKGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 4, 40 L93 Ac-KKKGK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 5, 40 L94 Ac-KKRKG-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 6, 40 L95 Ac-KKRKK-PEG2-K(cyclo[FGFG-Cit-GRQ])-PEG2-RF-PEG4-M 7, 51 L96 Ac-KKRKK-PEG2-K(cyclo[FGFGRG-Cit-Q])-PEG2-RF-PEG4-M 7, 52 L97 Ac-KKRKK-PEG2-K(cyclo[AGFGRGRQ])-PEG2-RF-PEG4-M 7, 47 L98 Ac-KKRKK-PEG2-K(cyclo[FGAGRGRQ])-PEG2-RF-PEG4-M 7, 50 L99 Ac-KKKGK-PEG2-K(cyclo[FtFGRGRQ])-PEG2-RF-PEG4-M 5, 39 L100 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-SF-PEG4-M 13, 40 L101 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RL-PEG4-M 13, 40 L102 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RY-PEG4-M 13, 40 L103 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RW-PEG4-M 13, 40 L104 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Cit-F-PEG4-M 13, 40 L105 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-Bip-M 13, 40 L106 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-R-Bip-PEG8-M 13, 40 L107 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG4-M 13, 40 L108 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG2-M 13, 40 L109 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RPF-PEG4-M 13, 40 LUO Ac-KKKRK-PEG2-K(cyclo[FGF-G(N-me)-RGRQ])-PEG2-RPF-PEG4-M 13, 60 LIU Ac-KKKRK-PEG2-K(cyclo[F-G(N-me)-FGRGRQ])-PEG2-RPF-PEG4-M 13, 61 Lil 2 Ac-KKKRK-PEG2-K(cyclo[FAFARGRQ])-PEG2-RF-PEG4-M 13, 62 L113 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-Bip-PEG4-M 13, 40 L114 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-F-PEG4-M 13, 40Lil 5 Ac-KKKRK-PEG2-K(cyclo[FGFG-Agp-G-Agp-Ql)-PEG2-RF-PEG4-M 13, 63 Table 9B.SEQ IDNo. Compound including a delivery constructNOs: L116 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4-M 13, 40 L117 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG2-M 13, 40 L118 Ac-Kl< KRK-PEG2-K(cyc[o[FGFGRGRQ])-PEG2-R-Phg-PEG4-M 13, 40 LI 19 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFE-M 13, 40 L120 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Hph-PEG4-M 13, 40 L121 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Pcpa-F-PEG4-M 13, 40 L122 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-M 13, 40L123 Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 12, 40SEQ ID No. Compound including a delivery constructNOs: Ac-KKKRK-PEG2-K(cyclo[Pcpa-G-Pcpa-GRGRQ])-PEGi-RF- 13, 64 L124 PEG4-MLI 25 Ac-RFGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4-M 22, 40 Table 9C.SEQ IDNo.Compound including a delivery construct NOs: Ac-KKKHH-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-MLI 26 (Ac-KKKHH-miniPEG2-K(cyclo[FGFGRGRQ])-mitiiPEG2-RF-PEG4-Bip- 15, 40 M)Ac-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])- PEG2-RF-PEG4-Bip-ML127 14, 40 (Ac-K(me)-K(me)-K(me)-R(me)-K(me)-miniPEG2- K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-Bip-M)Ac-KBKBKBRBK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-ML128 (Ac-KBKBKBRBK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 23, 40 PEG4-Bip-M)Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-Bip-ML129 (Ac-KKKRK-miniPEG2-K(cyclo[GFRGFRGQ])-miniPEG2-RF-PEG4-Bip- 13, 57 M)Ac-KKKRK-PEG2-K(cyclo[GRFGRFGQ])-PEG2-RF-PEG4-Bip-ML130 (Ac-KKKRK-miniPEG2-K(cyclo[GRFGRFGQ])-miniPEG2-RF-PEG4-Bip- 13, 66 M)Ac-RFKKRFK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-ML131 (Ac-RFKKRFK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 24, 40 Bip-M)Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-ML132 (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 24, 40 PEG4-M)Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-ML133 (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 21, 40 PEGi-Bip-M)Ac-KKKRK-PEG2-K(cyclo[RFGGRFGQ])-PEG2-RF-PEG4-Bip-ML134 (Ac-KKKRK-miniPEG2-K(cyclo[RFGGRFGQ])-miniPEG2-RF-PEG4-Bip- 13, 67 M)Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-PEG2-K(cyclo[FGFGRGRQ])- PEG2-RF-PEG4-Bip-ML135 25, 40 (Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-miniPEG2- K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-Bip-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-ML136 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-niiniPEG2-RF-PEG4-Bip- 13, 40M)SEQ ID No.Compound including a delivery construct NOs: Ac-(N(Arg))-B-(N(Arg))-(N(Arg))-B-(N(Arg))-K(cyclo[FGFGRGRQ])- PEG2-RF-PEG4-Bip-ML137 26, 40 (Ac-(N(Arg))-B-(N(Arg))-(N(Arg))-B-(N(Arg))-K(cyclo[FGFGRGRQ])- miniPEG2-RF-PEG4-Bip-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FRF-PEG4-Bip-ML138 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-FRF-PEG4- 13, 40 Bip-M)Ac-KKKRK-PEG2-K(cyclo[GFFGRGRQ])-PEG2-RF-PEG4-Bip-ML139 (Ac-KKKRK-miniPEG2-K(cyclo[GFFGRGRQ])-miniPEG2-RF-PEG4-Bip- 13, 65M)Table 9DSEQ IDNo. Compound including a delivery constructNOs: L140 Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEG8-RF-PEG4-M 40, 18 L141 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG2-F-PEG4-M 40, 18 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-PEG4- L142 13, 40M

[0305] In embodiments, a compound comprises a delivery construct selected from L7, L8, or L9, wherein “PEG2” is -(CH2-CH2-O)2-CH2-CH2~CO.

[0306] In embodiments, a compound can be Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta- GRGRQ])-PEGs-M (SEQ ID NOS: 18, 38), wherein PEG2is -(CH2-CH2-O)2-CH2-CH2-CO- or -(CH2-CH2-O)2-CH2-CO-, and PEG? is -(CH2-CH2-O)8-CH2-C(O)- or -(CH2-CH2-O)8-CH2-CH2-CO-.

[0307] FIGS 4C, 5B, 6B, 7B, 8B, 9B, 10B, 11B, 12B, 13B, 14B, 15B, 16B, 17B, 18B, 19B, 20B, 21B, 22B, 23B, 24B, 25B, and 26B show the structures of compounds 904c, 905b, 906b, 907b, 908b, 909b, 910b, 911b, 912b, 913b, 914b, 915b, 916b, 917b, 918b, 919b, 920b, 921b, 922b, 923b, 924b, 925b, and 926b each compound includes a delivery construct.

[0308] Compound 904c (FIG. 4C) is Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-PEG2- Nal-M (e g., see L39 in Table 9A, see also C11(b) in Table 12D), wherein PEG4 is (CH2-CH2- O)4-CH2-CH2-CO- and PEG2 is -(CH2-CH2-O)-CH2-C(O)-. Compound 904c includes the delivery 904a (FIG. 4A), wherein the delivery' construct is covalently attached to an OH.

[0309] Compound 905b (FIG. 5B) is Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEGs-Bip-M (e g., see L21 in Table 9A, see also A17(b) in Table 10C), wherein PEG8 is -(CH2-CH2-O)8-CH2-CHs-CO-. Compound 905b includes the delivery construct 905a (FIG. 5A), wherein the deliver}' construct is covalently attached to an OH.

[0310] Compound 906b (FIG. 6B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Nal-M (e.g., see L32 in Table 9A, see also C2(b) in Table 12A), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is (CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 906b includes the delivery construct 906a (FIG. 6A), wherein the delivery construct is covalently attached to an OH.

[0311] Compound 907b (FIG. 7B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-PEGi-Nal-M (e.g., see L33 in Table 9A, see also C3(b) in Table 12A), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO-, PEG8 is (CH2-CH2-O)8-CH2-CH2-C(O)-, and PEG4is (CH2-CH2-O)4-CH2-CH2-C(O)- Compound 907b includes the delivery construct 907a (FIG. 7A), wherein the delivery construct is covalently attached to an OH.

[0312] Compound 908b (FIG. 8B) is Ac-PKKKRKV-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG2-Nal-M (e.g., see L34 in Table 9A, see also C6(b) in Table 12C), wherein PEG2 is (CH2-CH2-O)2-CH2-CO-. Compound 908b includes the delivery construct 908a (FIG. 8A), wherein the deliver}' construct is covalently attached to an OH.

[0313] Compound 909b (FIG. 9B) is Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-F-M (e.g., see L30 in Table 9A, see also C5(b) in Table 12B), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 909b includes the delivery constmct 909a (FIG. 9A), wherein the delivery construct is covalently attached to an OH.

[0314] Compound 910b (FIG. 10B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bta-PEG2-M (e.g., see L26 in Table 9A, see also B4(b) in Table 11A ), wherein PEG2 is -(CH2-CH2-O)2-CH22-CO- and PEG4is -(CH -CH2-O)4-CFl2-CH2-C(O)-. Compound 910b includes the delivery construct 910a (FIG. 10A), wherein the delivery construct is covalently attached to an OH.

[0315] Compound 911b (FIG. 11B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-Bip-M (e.g., see L29 in Table 9A, see also Cl(b) in Table 12A), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is (CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 911b includes the delivery construct 911a (FIG. 11 A), wherein the delivery construct is covalently attached to an OH.

[0316] Compound 912b (FIG. 12B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFRF-PEG4-M (e.g., see L75 in Table 9A, see also B38(b) in Table 11C), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is “(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 912b includes the delivery construct 912a (FIG. 12A), wherein the delivery construct is covalently attached to an OH.

[0317] Compound 913b (FIG. 13B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFR- PEG4-M (e.g., see L54 in Table 9A, see also B18(b) in Table 11C), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4 is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 913b includes the delivery construct 913a (FIG. 13A), wherein the delivery construct is covalently attached to an OH.

[0318] Compound 914b (FIG. 14B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Tyr( Ph)-PEG4-M (e g., see L65 in Table 9A, see also B29(b) in Table 11C), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 914b includes the delivery construct 914a (FIG. 14A), wherein the delivery construct is covalently attached to an OH.

[0319] Compound 915b (FIG. 15B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-F-PEG4-M (e.g., see L114 in Table 9A, see also B74(b) in Table 11C), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 915b includes the deliver}' construct 915a (FIG. 15A), wherein the deliver}' construct is covalently attached to an OH

[0320] Compound 916b (FIG. 16B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF- PEG4-M (e.g., see L77 in Table 9A, see also B41(b) in Table 11C), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO-. Compound 916b includes the delivery construct 916a (FIG. 16A), wherein the deliver}' construct is covalently attached to an OH.

[0321] Compound 917b (FIG. 17B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG2-M (e.g., see L51 in Table 9A, see also B16(b) in Table 11C), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO-. Compound 917b includes the delivery construct 917a (FIG. 17A), wherein the deliver}' construct is covalently attached to an OH.

[0322] Compound 918b (FIG. 18B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4-M (e.g., see L116 in Table 9B, see also B76(b) in Table 11D), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 918b includes thedelivery construct 918a (FIG. 18A), wherein the deliver}' construct is covalently attached to an OH

[0323] Compound 919b (FIG. 19B) is Ac-KKKRKR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-F-PEG4-M (e.g., see L87 in Table 9A, see also B51(b) in Table 11C), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4 is (CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 919b includes the delivery construct 919a (FIG. 19A), wherein the delivery construct is covalently attached to an OH.

[0324] Compound 920b (FIG. 20B) is Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEGi-M (e.g., see L89 in Table 9A, see also B53(b) in Table 11C), wherein PEG? is -(CH22-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 920b includes the delivery construct 920a (FIG. 20A), wherein the delivery construct is covalently attached to an OH.

[0325] Compound 921b (FIG. 21B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4-M (e.g., see L57 in Table 9A, see also B21(b) in Table 11C), wherein PEG2 is (CH2- CH2-O)2-CH2-CO-, PEG4 is -(CH2-CH2-O)4-CH2-CH2-C(O)-, and PEG8 is -(CH2-CH2-O)s-CH2- CH2-C(O)- Compound 921b includes the delivery construct 921a (FIG. 21A), wherein the delivery construct is covalently attached to an OH.

[0326] Compound 922b (FIG. 22B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RPF-PEG4-M (e.g., see L109 in Table 9A, see also B69(b) in Table 11C), wherein PEG2 is ~(CH2-CH2-O)2-CH2-CO- and PEG4 is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 922b includes the delivery construct 922a (FIG. 22A), wherein the delivery construct is covalently attached to an OH.

[0327] Compound 923b (FIG. 23B) is Ac-KKKRKF-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG4-M (e.g., see L88 in Table 9A, see also B52(b) in Table 11C), wherein PEG2is -(CH2-CH2-O)2-CH2-CO- and PEG4 is -(CH2-CH2-O)4-CH2-CH2-C(O)- Compound 923b includes the delivery construct 923a (FIG. 23A), wherein the delivery construct is covalently attached to an OH.

[0328] Compound 924b (FIG. 24B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FR-PEG4-M (e.g., see L86 in Table 9A, see also B50(b) in Table 11C), wherein PEG2 is (CH2-CH2-O)2-CH2-CO- and PEG4is (CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 924b includes thedelivery construct 924a (FIG. 24A), wherein the deliver}' construct is covalently attached to an OH[03291 Compound 925b (FIG. 25B) is Ac-KKKRK-PEG4-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M (e.g., see L86 in Table 9A, see also B37(b) in Table 11C), wherein PEG2 is -(CH2- CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 925b includes the delivery construct 925a (FIG. 25A), wherein the delivery construct is covalently attached to an OH.[03301 Compound 926b (FIG.26B) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-Bip-M (e g., see L35 in Table 9A, see also C4(a) in Table 12A), wherein PEG2 is -(CH2-CH2-O)2-CH2-CO- and PEG4is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 926b includes the delivery construct 926a (FIG. 26A), wherein the delivery construct is covalently attached to an OH.[03311 In embodiments, a compound includes a delivery construct is selected from compound 904b, 905b, 906b, 907b, 908b, 909b, 910b, 911b, 912b, 913b, 914b, 915b, 91 b, 917b, 918b, 919b, 29b, 921b, 922b, 923b, 924b, 925b, or 926b

[0332] In embodiments, a compound that includes a delivery construct is compound 904c. In embodiments, a compound that includes a delivery construct is compound 905b. In embodiments, a compound that includes a delivery construct is compound 906b. In embodiments, a compound that includes a delivery construct is compound 907b. In embodiments, a compound that includes a delivery construct is compound 908b. In embodiments, a compound that includes a delivery construct is compound 909b. In embodiments, a compound that includes a delivery construct is compound 910b. In embodiments, a compound that includes a delivery construct is compound 911b. In embodiments, a compound that includes a delivery construct is compound 912b. In embodiments, a compound that includes a delivery construct is compound 913b In embodiments, a compound that includes a delivery construct is compound 914b. In embodiments, a compound that includes a delivery construct is compound 915b. In embodiments, a compound that includes a delivery construct is compound 916b. In embodiments, a compound that includes a delivery construct is compound 917b. In embodiments, a compound that includes a delivery construct is compound 918b. In embodiments, a compound that includes a delivery construct is compound 919b. InIllembodiments, a compound that includes a delivery construct is compound 920b. In embodiments, a compound that includes a delivery construct is compound 921b, In embodiments, a compound that includes a delivery construct is compound 922b. In embodiments, a compound that includes a delivery construct is compound 923b. In embodiments, a compound that includes a delivery construct is compound 924b. In embodiments, a compound that includes a delivery construct is compound 925b. In embodiments, a compound that includes a delivery construct is compound 926b,

[0333] In embodiments, the compound of Formula III may be of Formula III(i):Formula III(i)H O H 0 R20(AA2)'NV^nHK- [AA3].,, a3 01. a2 v 9 / x2 *2&li HA "" & (AA4) ml w,l \?yHH w2Jw3 a -AOHo,> HN„r2FK?6' X NH HN" yNr ■«-■< r b0 |^4or a pharmaceutically acceptable salt thereof,wherein:wl, w2, and w3 are each independently 0 or 1;xl, x2, and x3 are each independently an integer from 1 to 14;j 1, j 2, and j3 are each independently an integer from 1 to 4; andR20, AA1, al, y, n, R1, R2, R3, R4, R5, R6, R7, AA2, a2, AA3, a3, AA4, a4, ml, and M are defined herein, where at least one of a2, a3, and a4 is 1 and at least one of w2 and w3 is 1.

[0334] wl, w2, and w3 are each independently 0 or 1. wl can be 0. wl can be 1. w2 can be 0 w2 can be 1. w3 can be 0. w3 can be 1. In embodiments, at least one of w2 and w3 is 1.

[0335] In embodiments, al is 1, a2 is 1, a3 is 0, a4 is 0, wl is 1, w2 is 1, and w3 is 0. In embodiments, al is 0, a2 is 1, a3 is 0, wl is 1, w2 is 1, and w3 is 0. In embodiments, al is 0, a2 is 1, a3 is 0, wl is 0, w2 is 1, and w3 is 0,

[0336] In embodiments, al is 1, a2 is 0, a3 is 1, a4 is 0, wl is 1, w2 is 1, and w3 is 1. In embodiments, al is 0, a2 is 0, wl is 1, w2 is 1, and w3 is 1, In embodiments, al is 0, a2 is 0, wl is 0, w2 is 1, and w3 is 1.

[0337] In embodiments, al is 1, a2 is 0, a3 is 1, a4 is 1, wl is 1, w2 is 1, and w3 is 1. In embodiments, al is 1, a2 is 0, a3 is 1, a4 is 1, wl is 1, w2 is 1, and w3 is 1. In embodiments, al is 1, a2 is 0, a3 is 1, a4 is 1, wl is 0, w2 is 1, and w3 is 1

[0338] In embodiments, al is 1, a2 is 1, a3 is 1, a4 is 0, wl is l,w2 is 1, and w3 is 0. In embodiments, al is 1, a2 is 1, a3 is 1, a4 is 0, wl is 1, w2 is 1, and w3 is 0. In embodiments, al is 1, a2 is 1, a3 is 1, a4 is 0, wl is 0, w2 is 1, and w3 is 0

[0339] In embodiments, al is 1, a2 is 1, a3 is 0, a4 is 0, wl is 1, w2 is 1, and w3 is 0. In embodiments, al is 0, a2 is 1, a.3 is 0, a4 is 0, wl is 1, w2 is 1, and w3 is 0, In embodiments, al is 0, a2 is 1, a3 is 0, a4 is 0, wl is 0, w2 is 1, and w3 is 0.

[0340] xl, x2, and x3 are each independently an integer from 1 to 14. Each of xl, x2, and x3 present in the compound are each independently 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, or 14. In embodiments, tach of xl, x2, and x3 present in the compound are each independently 2, 4, 6, 8, 10, or 12. In embodiments, each of xl, x2, and x3 present in the compound are each independently 2, 4, 8, or 12.

[0341] When wl is 1, xl can be 2, 4, 8, or 12. When wl is 1, xl can be 2. When wl is 1, xl can be 4. When wl is 1, xl can be 8. When wl is 1, xl can be 12.

[0342] When w2 is 1, x2 can be 2, 4, 8, or 12. When w2 is 1, x2 can be 2. When w2 is 1, x2 can be 4. When w2 is 1, x2 can be 8. When w2 is 1, x2 can be 12.

[0343] When w3 is 1, x3 can be 2, 4, 8, or 12. When w3 is 1, x2 can be 2, When w3 is 1, x.3 can be 4. When w3 is 1, x2 can be 8. When w3 is 1, x3 can be 12.

[0344] j 1, j2, and j3 are each independently an integer from 1 to 4. 0. j 1 can be 1. j 1 can be 2. j can be 3. j 1 can be 4. j2 can be 1. j2 can be 2. j2 can be 3. j2 can be 4. j3 can be 1. j3 can be 2. j3 can be 3. j 3 can be 4.

[0345] In embodiments when wl is 1. xl can be 2, 4, 8, or 12, and j 1 can be 1 or 2 In embodiments when wl is 1, xl can be 2 and jl can be 1, In embodiments when wl is 1, xl can be 2 and jl can be 2. In embodiments when wl is 1, xl can be 4 andjl can be 1. In embodiments when wl is 1, xl can be 4 andjl can be 2 In embodiments when wl is 1, xl can be 8 andjl can be 1. In embodiments when wl is 1, xl can be 8 and j 1 can be 2. In embodiments when wl is 1, xl can be 12 and j 1 can be 1. In embodiments when wl is 1, xl can be 12 andjl can be 2.

[0346] In embodiments when w2 is 1, x2 can be 2, 4, 8, or 12, and j2 can be 1 or 2. In embodiments when w2 is I, x2 can be 2 and j2 can be 1. In embodiments when w2 is 1, x2 can be 2 and j2 can be 2. In embodiments when w2 is 1, x2 can be 4 and j2 can be 1. In embodiments when w2 is 1, x2 can be 4 and j2 can be 2. In embodiments when w2 is 1, x2 can be 8 and j2 can be 1, In embodiments when w2 is 1, x2 can be 8 and j2 can be 2 In embodiments when w2 is 1, x2 can be 12 and j2 can be 1. In embodiments when w2 is 1, x2 can be 12 and j2 can be 2

[0347] In embodiments when w3 is 1, x3 can be 2, 4, 8, or 12, and j3 can be 1 or 2. In embodiments when w3 is 1, x3 can be 2 and j3 can be 1. In embodiments when w3 is 1, x3 can be 2 and j3 can be 2. In embodiments when w3 is 1, x3 can be 4 and j3 can be 1. In embodiments when w3 is 1, x3 can be 4 and j3 can be 2. In embodiments when w3 is 1, x3 can be 8 and j3 can be 1. In embodiments when w3 is 1, x3 can be 8 and j3 can be 2. In embodiments when w3 is I, x3 can be 12 and j can be 1, In embodiments when w3 is 1, x3 can be 12 and j3 can be 2.[034S] In embodiments, the compound of Formula III(i) may be of Formula III(A):Formula III(A):or a pharmaceutically acceptable salt thereof,wherein a3 is 1 and R20, AA1, al, xl, j 1, wl, y, n, R1, R2, R3, R4, R5, R6, R7, x2, j2, AA3, ml, and M are defined herein.

[0349] A compound of Formula III(A) can be a compound including a delivery construct of Formula 1(A) wherein the delivery construct of Formula 1(A) is covalently attached to M.

[0350] In embodiments, M is OH. In embodiments, M is OH of the C-terminal end of the C-terminal amino acid residue of AA3.

[0351] Examples of compounds of Formula III(A) include those listed in Tables 10A-10H In Tables 10A-10H, Ac is -C(O)CH3; the cCPP is written as JA(cyclo[XAXBXcXuXEXFXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with the side chain R1, R2, R’, R4, R5, R6, and R7, respectively, YAis the cCPP bridging amino acid residue, and JAis the bridging exocyclic amino acid residue (see, for example, the cCPP description herein); HniriiPECb’ indicates ~(CH2-CH2-O)2-CH2-CO-, and “PEG#” indicates ~(CH2-CH2-O)#-CH2-CO- or -(CH2-CH2-O)#-CH2-CH2-CO- where # indicates to the number of -CH2-CH2-O- units. In Tables 10A-10H, M is the OH of the carboxylic acid of the C -terminal amino acid residue or any M disclosed herein. In embodiments of the compounds of Tables 10A-10C, each instance of “PEG2” refers to -(CH2-CH2-O)2-CH2-CO- (i.e., “miniPEGf’) and each instance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2. In embodiments of the compounds of Tables 10A-10C, each instance of “PEG2” refers to ---(CH2-CH2-O)2-CH2- CH2-CO- and each instance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2.Table 1 OA.SEQ IDNo. Compound including a delivery constructNOs: Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Bip-BRBRB-M 18, 40, Al(b)(Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-Bip-BRBRB-M) 35 Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal-BRBRB-M 18, 40, A2(b)(Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal-BRBRB-M) 36 Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-B-MA3(b) 18, 40 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-B-M)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BR-Bip-RB-M 18, 40, A4(b)Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-BR-Bip-RB-M 85 Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Val-Cit-MA5(b) 18, 40Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-Val-Cit-MTable 1 OB.SEQ IDNo. Compound including a delivery constructNOs: Ac-KKKRK -PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-B-M13, 40 A6(b) (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-B-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BRB-Bip-M13, 40, 29 A7(b) (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQl)-PEGi2-BRB-Bip-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG«-R-Nal-M13, 40 A8(b) (Ac-KKKRK-miniPEG2-K(cyclo|FGFGRGRQ])-PEG8-R-Nal-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-rf-M13, 40 A9(b) Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-rf-MAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])- PEG2-FK-M13, 40 A10(b) (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-FK-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-M13, 40 All(b) (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-M)Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-M12, 40 A 12(b) (Ac-kkkrk-miniPEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-M)A13(c) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-M 13, 40A14(c) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-M 13, 40Table IOC.SEQ IDNo. Compound including a delivery constructNOs: Ac-RBRRB R-PEG2-K (cyclo[FGFGRGRQ])-PEGs-K-Bip-MA 15(b) 20, 40(Ac-RBRRBR-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-K-Bip-M) A16(b) Ac-RBKKBR-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-M 80, 40A17(b) Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG8-Bip-M 20, 40 Table IOD.SEQ IDNo.Compound including a delivery construct NOs: Ac-K(me)-K(nie)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])- PEGs-RF-MA18(b) 14, 40(Ac-K(me)-K(me)-K(me)-R(me)-K(me)-miniPEG2- K(cyclo[FGFGRGRQ])-PEG8-RF-M)Ac-YArVRRrGPR-mimPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-MA19(b) 21, 40(Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-M)Table 1 OE.SEQ IDNo. Compound including a delivery constructNOs Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-RF-MA20(b) (Ac-PKKKRKV-miniPEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-RF- 18, 38M)Table 10F.SEQ IDNo. Compound including a delivery constructNOs: Ac-KKKRK-PEG2-K(cyclo[GfFGrGrQ])-PEG8-RF-MA21(b) 13, 44(Ac-KKKRK-miniPEG2-K(cvclo[GfFGrGrQ])-PEG«-RF-M)Ac-kkkRK-PEG2-K(cyclo[GfFGrGrQ])-PEG8-RF-MA22(b) 11, 44(Ac-kkkRK-miniPEG2-K(cyclo[GfFGrGrQT)-PEGs-RF-M)Table 1 OG.SEQ IDNo. Compound including a delivery constructNOs: A23(b) Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-M 1, 40A24(b) Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-M 12, 40 Table 1 OH.SEQ IDNo. Compound including a delivery constructNOs:A25 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFE-M 13, 40

[0352] In embodiments, a compound including a delivery construct is selected from any one of Tables 10A-10H. In embodiments, a compound including a delivery construct is selected from any one of Tables 10A-10H wherein M is the OH of the C -terminal end of the C-terminal amino acid residue. In embodiments, a compound including a delivery construct is selected from Table 10A. In embodiments, a compound including a delivery construct is selected from Table 10A wherein M is the OH of the C-terminal end of the C-terminal amino acid residue.

[0353] In embodiments, a compound including a delivery construct is selected from Table 10B. In embodiments, a compound including a delivery construct is selected from Table 10B wherein M is the OH of the C-terminal end of the C-terminal amino acid residue.

[0354] In embodiments, a compound including a delivery construct is selected from Table 10C. In embodiments, a compound including a delivery construct is selected from Table 10C wherein M is the OH of the C-terminal end of the C-terminal amino acid residue.

[0355] In embodiments, a compound including a delivery construct is selected from Table 10D. In embodiments, a compound including a delivery construct is selected from Table 10D wherein M is the OH of the C-terminal end of the C-terminal amino acid residue.

[0356] In embodiments, a compound including a delivery construct is selected from Table 10E. In embodiments, a compound including a delivery construct is selected from Table IDE wherein M is the OH of the C-terminal end of the C-terminal amino acid residue.

[0357] In embodiments, a compound including a delivery construct is selected from Table 10F. In embodiments, a compound including a delivery construct is selected from Table 10F wherein M is the OH of the C-terminal end of the C-terminal amino acid residue.

[0358] In embodiments, a compound including a delivery construct is selected from Table 10G. In embodiments, a compound including a delivery construct is selected from Table 10G wherein M is the OH of the C-terminal end of the C-terminal amino acid residue.

[0359] In embodiments, a compound including a delivery construct is selected from Table 10H. In embodiments, a compound including a delivery construct is selected from Table 10H wherein M is the OH of the C-terminal end of the C-terminal amino acid residue.

[0360] In embodiments, the compound of Formula III(i) may be of Formula III(B):Formula III(B):\ M H o TT""'M.r Y A w N' 1A H 6 A H * R S3 W? (1 ^ < N< Ho HN O0;,^HKNH HH ’RsNA”’ <? C o0 R* or a pharmaceutically acceptable salt thereof,wherein a3 is 1, R40is H or CH?, and R20, AA1, al, xl, j 1, wl, y, n, R1, R2, R3, R4, R5, R6, R7, x2, j2, AA3, x3, j3, ml, and M are defined herein.

[0361] In embodiments R40is H. In embodiments R40is CH3. When R40is CH3, the amino acid of the cCPP having the R2side chain can is N-methylated (e.g., N-methylated phenylalanine (f(N-me) or F(N-me)), N-methylated glycine (G(N-me)), and the like).

[0362] A compound of Formula III(B) can be a compound that includes a delivery construct of Formula 1(B) wherein the delivery construct of Formula 1(B) is covalently attached to M In embodiments M is OH.

[0363] Examples of compounds of Formula III(B) include those listed in Tables 11A-I IE. In Tables 11A-11E, Ac is -C(O)CH3;the cCPP is written as JA(cyclo[XAXBXcXDXEXFXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with the side chain R’, R2, R3, R4, R5, R6, and R7, respectively, YAis the cCPP bridging amino acid residue, and JAis the bridging exocyclic amino acid residue (see, for example, the cCPP description herein), “miniPEGf’ indicates -(CH2-CH2-O)2-CH2-CO-; and “PEG#” indicates -(CH2-CH2-O)#-CH2-CO- or -(CH2-CH2-O)#-CH2-CH2-CO- where # indicates to the number of -CH2-CH2-O- units. In Tables 11A-HE, M is OH or any M disclosed herein. In embodiments of the compounds of Tables 11A-11E, each instance of “PEG2” refers to ~(CH2-CH2-O)2-CH2-CO- (i.e “miniPEG2”) and each instance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2. In embodiments of the compounds of Tables 11A-11E, each instance of “PEG2” refers to -(CH2-CH2-O)2-CH2-CH2-CO- and each instance of “PEG#” refers to (CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2.Table 11 A.SEQ IDNo. Compound including a delivery constructNOs: Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-PEG2-MBl(b) 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-PEG2-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG2-MB2(b) (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-R-Bta- 13, 40 miniPEG2-M)Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-MB3(b) 20, 40 (Ac-RBRRBR-K(cyclo[FGFGRGRQl)-miniPEG2-KF-PEG4-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bta-PEG2-MB4(b) (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ)-PEG4-R-Bta-miiuPEG2- 13, 40M)Table 11B.SEQ IDNo. Compound including a delivery constructNOs: Ac-KKKRK-PEG2-K(cyclo[FGFRFIRHQ])-PEG2-RF-PEG4-MB5(b) 13, 42 (Ac-KKKRK-miniPEG2-K(cyclo[FGFRHRHQl)-miniPEG2-RF-PEG4-M)Ac-YArVRRrGPR-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4-MB6(b) (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FfFGRGRQ])-miniPEG2-RF- 21, 39 PEG4-M)AC-K(CVC1O[FGFGRGRQ])-PEG2-PKKKRK. V-PEGB-MB7(b) 40, 18(Ac-K(cvclo[FGFGRGRQ])-miniPEG2-PKKKRKV-PEG8-M)Table 11C.SEQ IDNo. Compound including a delivery constructNOs: B8(b) Ac-TKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 9, 40 B09(b) Ac-KKTRK-PEG2~K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 8, 40 Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-PEG4- B10(b) 21, 40 MAc-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ])-PEG2-RG-PEG4- Bll(b) 13, 55 MAc-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ])-PEG2-RF-PEG4- Bl 2(b) 13, 55MSEQ ID No. Compound including a delivery constructNOs: B13(b) Ac-KKKRK-PEG2-K(cyclo[Gf-Nal-GrGrQ])-PEG2-RF-PEG4-M 13, 56 B14(b) Ac-KKKRK-PEG2-K(cyclo[GyYGrGrQ])-PEG2-RF-PEG4-M 13, 58 B15(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-PEG4-M 13, 40 B16(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG2-M 13, 40 B17(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-PEG4-M 13, 40 B18(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFR-PEG4-M 13, 40 B19(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-R-PEG4-M 13, 40 B20(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-R-PEG4-M 13, 40 B21(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Nal-PEG4-M 13, 40 B22(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG8-M 13, 40 B23(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-M 13, 40Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(3-Pyr)-PEG4- 24(b) 13, 40 MAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(2-Pyr)-PEG4- B25(b) 13, 40MAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(4-Pyr)-PEG4- B26(b) 13, 40MAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phe(3-CN)- B27(b) 13, 40PEG4-MAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Trp(5-F)- B28(b) 13, 40PEG4-MAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Tyr(Ph)-PEG4- B29(b) 13, 40MAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-HoArg-Bip- B30(b) 13, 40 PEG4-MB31(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-rf-PEG4-M 13, 40Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R(me)-F(N-me)- B32(b) 13, 40PEG4-MAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-(4-Pyr)-PEG4- B33(b) 13, 40Nal-MB34(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4-F-M 13, 40Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-RF- B35(b) 13, 46PEG4-MAc-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-R- B36(b) 13, 46Bip-PEG4-MB37(b) Ac-KKKRK-PEG4-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 13, 40 B38(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG4-M 13, 40 B39(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFRF-PEG4-M 13, 40, 33 B40(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RRFF-PEG4-M 13, 40, 86 B41(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-M 40B42(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KFKF-PEG4-M 40, 32SEQ ID No. Compound including a delivery constructNOs: B43(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-EF-PEG4-M 13, 40 B44(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PECn-R-Bip-PEG4-M 13, 40 B45(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FGR-PEG4-M 13, 40Ac-KKKRK-PEG2-K(cyclo[Phe(4-CN)-G-Phe(4-CN)-GRGRQ])- B46(b) 13, 59PEG2-RF-PEG4-MB47(b) Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-K-PEG4-M 1, 40 B48(b) Ac-KKRK-PEG2-K(cyclo[FGFGRrRQ])-PEG2-RF-PEG4-M 1, 53 B49(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ]-PEG2-RF(I)-PEG4-M 13, 40 B50(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FR-PEG4-M 13, 40 B51(b) Ac-KKKRKR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-F-PEG4-M 17, 40 B52(b) Ac-KKKRKF-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG4-M 16, 40 B53(b) Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-M 13, 57 B54(b) Ac-KKKRK-PEG2-K(cyclo[FFGRRGQ])-PEG2-RF-PEG4-M 13, 49 B55(b) Ac-KGKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 3, 40 B56(b) Ac-KKGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 4, 40 B57(b) Ac-KKKGK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 5, 40 B58(b) Ac-KKRKG-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 6, 40 B59(b) Ac-KKRKK-PEG2-K(cyclo[FGFG-Cit-GRQ])-PEG2-RF-PEG4-M 7, 51 B60(b) Ac-KKRKK-PEG2-K(cyclo[FGFGRG-Cit-Q])-PEG2-RF-PEG4-M 7, 52 B61(b) Ac-KKRKK-PEG2-K(cyclo[AGFGRGRQ])-PEG2-RF-PEG4-M 7, 47 B62(b) Ac-KKRKK-PEG2-K(cyclo[FGAGRGRQ])-PEG2-RF-PEG4-M 7, 50 B63(b) Ac-KKKGK-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4-M 5, 39 B64(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-SF-PEG4-M 13, 40 B65(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RL-PEG4-M 13, 40 B66(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RY-PEG4-M 13, 40 B67(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RW-PEG4-M 13, 40 B68(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Cit-F-PEG4-M 13, 40 B69(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RPF-PEG4-M 13, 40Ac-KKKRK-PEG2-K(cyclo[FGF-G(N-me)-RGRQ])-PEG2-RPF- B70(b) 13, 60PEG4- MAc-KKKRK-PEG2-K(cyclo[F-G(N-me)-FGRGRQ])-PEG2-RPF- B71(b) 13, 61PEG4- MB72(b) Ac-KKKRK-PEG2-K(cyclo[FAFARGRQ])-PEG2-RF-PEG4- M 13, 62Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-Bip-PEG4- B73(b) 13, 40MB74(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-F-PEG4-M 13, 40Ac-KKKRK-PEG2-K(cyclo[FGFG-Agp-G-Agp-Q])-PEG2-RF- B75(b) 13, 63PEG4-MTable 11).SEQ IDNo. Compound including a delivery constructNOs: B76(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG1-RF-PEG4-M 13, 40 B77(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG2-M 13, 40 B78(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phg-PEG4-M 13, 40 B79(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Hph-PEG4-M 13, 40 B80(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Pcpa-F-PEG4-M 13, 40 B81(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-M 13, 40 B82(b) Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 12, 40 B83(b) Ac-KKKRK-PEG2-K(cyclo[Pcpa-G-Pcpa-GRGRQ])-PEG2-RF-PEG4-M 13, 64B84(b) Ac-RFGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4-M 22, 40 Table 11E.SEQNo. Compound including a delivery construct ID NOs: Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M 24,B85(b) (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-M) 40

[0364] In embodiments, a compound including a delivery construct is selected from any one of Tables 11A-11E. In embodiments, a compound including a delivery construct is selected from any one of Tables 11A-11E wherein M is OH.

[0365] In embodiments, a compound including a delivery construct is selected from Table 11A. In embodiments, a compound including a delivery' construct is selected form Table 11A wherein M is OH.

[0366] In embodiments, a compound including a delivery construct is selected from Table 11B. In embodiments, a compound including a delivery construct is selected form Table 11 B wherein M is OH.

[0367] In embodiments, a compound including a delivery construct is selected from Table 11C In embodiments, a compound including a delivery construct is selected form Table 11C wherein M is OH.

[0368] In embodiments, a compound including a delivery construct is selected from Table 11D. In embodiments, a compound including a delivery construct is selected form Table 11D wherein M is OH.

[0369] In embodiments, a compound including a delivery construct is selected from Table 11E. In embodiments, a compound including a delivery construct is selected form Table 11E wherein M is OH.

[0370] In embodiments, the compound of Formula III(i) may be of Formula III(C):Formula 111(C).SHor a pharm ceutically acceptable salt thereof,

[0371] wherein a3 and a4 are 1 and R20, AA1, al, xl, j 1, wl, y, n, R1, R2, R3, R4, R5, R6, R7, x2, j2, AA3, x3, j3, AA4, ml, and M are defined herein. A compound of Formula III(C) can be a compound that includes a delivery construct of Formula 1(C) wherein the delivery construct of Formula 1(C) is covalently attached to M.

[0372] In embodiments, M is OH. In embodiments, M is OH of the C-temiinal end of the C-terminal amino acid residue of AA4.

[0373] Examples of compounds of Formula III(A) include those listed in Tables 12A-12E. In Tables 12A-12E, Ac is -C(O)CH3; the cCPP is written as JA(cyclo[XAXBXcXDXEXFXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with the side chain R1, R2, R3, R4, R5, R6, and R7, respectively, YAis the cCPP bridging amino acid residue, and JAis the bridging exocyclic amino acid residue (see, for example, the cCPP description herein): “miniPEG2”indicates --(CH2-CH2-O)2-CH2-CO-; and “PEG / ’ indicates -(CH2-CH2-O)#-CH2-CO- or -(CH2-CH2-O)#-CH2-CH2-CO- where # indicates to the number of -CH2-CH2-O- units. In Tables 12A- 12E, M is the OH of the carboxylic acid of the C -terminal amino acid residue or any M disclosed herein. In embodiments of the compounds of Tables 12A-12E, each instance of “PEG2” refers to --(CH2-CH2-O)2-CH2-CO- (i.e., “miniPEG?”) and each instance of “PEG / ’ refers to --(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2. In embodiments of the compounds of Tables 12A-12E, each instance of “PEG?” refers to (CH2-CH2-O)2-CH2-CH2-CO- and each instance of “PEG / ’ refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2. Table 12 A.SEQ IDNo. Compound including a delivery constructNOs: Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-Bip-MC1(b) (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-rf-PEG4-Bip- 13, 40 M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Nal-MC2(b) (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-Nal- 13, 40 M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG4-Nal-MC3(b) 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG4-Nal-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])- PEG2-KF-PEG4-Bip-MC4(b) (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-KF-PEG4-Bip- 13, 40M)Table 12B.SEQ IDNo. Compound including a delivery constructNOs: Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-F-M18, 40 C5(b) (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-F-M)Table 12C.SEQ IDNo. Compound including a delivery constructNOs: Ac-PKKKRKV-PEG2-K(cyclo[FtFGRGRQ])-PEG2-RF-PEG2-Nal-MC6(b) (Ac-PKKKRKV-miniPEG2-K(cyclo[FfFGRGRQ])-miniPEG2-RF- 18, 39 miniPEG2-Nal-M)Ac-KKKRK-PEG2-K(cyclo[FfFGRGRQ])-PEGi2-(2-Nal)-PEG2-(2-Nal)-MC7(b) (Ac-KKKRK-miniPEG2-K(cyclo[FfFGRGRQ])-PEGi2-(2-Nar)-miniPEG2- 13, 39 (2-Nal)-M)C8(b) Ac-KKKRK-PEG2-K(cyclo[FfFGRGRQ])-PEGi2-Bip-PEG2-Bip-M 13, 39SEQ ID No. Compound including a delivery constructNOs: (Ac-KKKRK-miniPEG2-K(cyclo[FfFGRGRQ])-PEGi2-Bip-miniPEG2-Bip- M)C9(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-Bip-M 13, 40 Table 12D.SEQ IDNo. Compound including a delivery constructNOs: Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bta-M C10(b) (Ac-RBRRBR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 20, 40Bta-M)Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-PEG2-Nal-MC11(b) 20, 39(Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-miniPEG2-Nal-M) Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEGi2-Nal-PEG C12(b)12(b) 20, 40(Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEGi2-Nal-miniPEG2-Nal-M)Table 12E.SEQ IDNo. Compound including a delivery constructNOs: Ac-KKKHH-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M(Ac-KKKHH-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 15, 40 C13(b) Bip-M)Ac-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])- PEG2-RF-PEG4-Bip-M ’14, 40 (Ac-K(me)-K(me)-K(me)-R(me)-K(me)-miniPEG2- C14(b) K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-Bip-M)Ac-KBKBKBRBK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M(Ac-KBKBKBRBK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 23, 40 C15(b) PEG4-Bip-M)Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-Bip-M(Ac-KKKRK-miniPEG2-K(cyclo[GFRGFRGQ])-miniPEG2-RF-PEG4- 13, 57 C16(b) Bip-M)Ac-KKKRK-PEG2-K(cyclo[GRFGRFGQ])-PEG2-RF-PEG4-Bip-M(Ac-KKKRK-miniPEG2-K(cyclo[GRFGRFGQ])-miniPEG2-RF-PEG4- 13, 66 C17(b) Bip-M)Ac-RFKKRFK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M(Ac-RFKKRFK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 24, 40 C18(b) Bip-M)Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M(Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 21, 40 C19(b) PEG4-Bip-M)Ac-KKKRK-PEG2-K(cyclo[RFGGRFGQ])-PEG2-RF-PEG4-Bip-M(Ac-KKKRK-miniPEG2-K(cyclo[RFGGRFGQ])-miniPEG2-RF-PEG4- 13, 67C20(b) Bip-M)SEQ I D No. Compound including a delivery constructNOs: Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-PEG2-K(cyclo[FGFGRGRQ])- PEG2-RF-PEG4-Bip-M25, 40 (Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-miniPEG2- C21(b) K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-Bip-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M(Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 13, 40 C22(b) Bip-M)Ac-(N(Arg))-B-(N(Arg))-(N(Arg))-B-(N(Arg))- K(cyclo[FGFGRGRQ])- PEG2-RF-PEG4-Bip-M26, 40 (Ac-(N(Arg))-B-(N(Arg))-(N(Arg))-B-(N(Arg))-K(cyclo[FGFGRGRQ])- C23(b) mini PEG2-RF-PEG4-Bip-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FRF-PEG4-Bip-M(Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-FRF-PEG4- 13, 40 C24(b) Bip-M)Ac-KKKRK-PEG2-K(cyclo[GFFGRGRQ])-PEG2-RF-PEG4-Bip-M(Ac-KKKRK-miniPEG2-K(cyclo[GFFGRGRQ])-miniPEG2-RF-PEG4- 13, 65C25(b) Bip-M)

[0374] In embodiments, the compound of Formula III(i) may be of Formula III(D):Formula III(D):or a pharmaceutically acceptable salt thereof,wherein a2 and a3 are 1 and R20, AA 1, al, xl, j 1, wl, y, n, R1, R2, R3, R4, R5, R6, R7x2, j2, A A3, ml, and M are defined herein.

[0375] In embodiments, the compound of Formula III(i) may be of Formula III(E):Formula III(E):or a pharmaceutically acceptable salt thereof,wherein a2 is 1 and R20, AA1, al, xl, j 1, wl, y, n, R1, R2, R3, R4, R5, R6, R7, AA2, x2, j2, ml, and M are defined herein,

[0376] A compound of Formula III(E) can be a compound that includes a delivery construct of Formula 1(E) wherein the delivery construct of Formula 1(E) is covalently attached to M. In embodiments M is OH.

[0377] Examples of compounds of Formula III(E) include those listed in Table 13, In Table 13, Ac is -C(O)CH3; the cCPP is written as JA(cyclo[XAXBXcXDXEXFXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with the side chain R1, R2, R3, R4, R5, R6, and R7,respectively, YAis the cCPP bridging amino acid residue, and JAis the bridging exocyclic amino acid residue (see, for example, the cCPP description herein); “miniPEG2” indicates -(CH2-CH2-O)2-CH2-CO-; and “PEG#” indicates -(CH2-CH2-O)#-CH2-CO- or -(CH2-CH2-O)#-CH2-CH2-CO- where # indicates to the number of -CH2-CH2-O- units. In Table 13, M is OH or any M disclosed herein. In embodiments of the compounds of Table 13, each instance of “PEG2” refers to -(CH2-CH2-O)2-CH2-CO- (i.e., “miniPEGs”) and each instance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2. In embodiments of the compounds of Table 13, each instance of “PEGz” refers to -(CH2-CH2-O)2-CH2-CH2-CO- and each instance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2.Table 13.SEQ IDNo, Compound including a delivery constructNOs El(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-R-Bip-PEG8-M 13, 40 E2(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG4-M 13, 40E3(b) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG2-M 13, 40

[0378] In embodiments, a compound that includes a delivery construct is selected from any one of Table 13. In embodiments, a compound that includes a delivery construct is selected from Table 13 wherein M is OH.

[0379] In embodiments, the compound of Formula III(i) may be of Formula III(F):Formula IV(F):0a1 f a H • -x4or a pharmaceutically acceptable salt thereof,wherein x4 is an integer from 1 to 14, j4 is integer from 1 to 4; R40is H or CH3; and R20, AAl, al, xl, j 1, wl, y, n, R1, R2, R, R4, R~, R6, R7, x2, j2, AA3, x3, j3, AA4, ml, and XI are defined herein.

[0380] A compound of Formula IV (F) can be a compound that includes a delivery construct of Formula 11(F) wherein the delivery construct of Formula 11(F) is covalently attached to M. In embodiments M is OH.

[0381] x4 is an integer from 1 to 14. x4 can be 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, or 14. x4 can be 2, 4, 6, 8, 10, or 12. x4 can be 2, 4, 8, or 12. x4 can be 2. x4 can be 4. x4 can be 6 x4 can be 8. x4 can be 12.

[0382] j4 can be integer from 1 to 4. 0. j4 can be 1. j4 can be 2. j4 can be 3. j4 can be 4.

[0383] Examples of compounds of Formula IV(F) include those listed in Table 14. In Table 14, Ac is -C(O)CH3, the cCPP is written as JA(cyclo[XAXBXcXDXEXFXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with the side chain R1, R, R3, R4, R5, R6, and R7, respectively, YAis the cCPP bridging amino acid residue, and JAis the bridging exocyclic amino acid residue (see, for example, the cCPP description herein), “miniPEG2” indicates -(CH2-CH2-O)2-CH2-CO-; and ‘TEG*’’ indicates -(CH2-CH2-O)*-CH2-CO- or -(CH2-CH2-O)#-CH2-CH2- CO- where # indicates to the number of -CH2-CH2-O- units. In Table 14, M is OH or any Mdisclosed herein. In embodiments of the compounds of Table 14, each instance of “PEG2” refers to -(CH2-CH2-O)2-CH2-CO- (i.e., “miniPEG2”) and each instance of “PEG#” refers to -(CH₂-CH₂-O)#-CH₂-CH₂-CO- where # is an integer greater than 2. In embodiments of the compounds of Table 14, each instance of “PEG?” refers to -(CH2-CH2-O) -CH2-CH2-CO- and each instance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2.Table 14.SEQ IDNo. Compound including a delivery constructNOs: F1(b) Ac-K(cyclo|FGFGRGRQ])-PEG2-PKKKRKV-PEG8-RF-PEG4-M 40, 18 F2(b) Ac-KKkRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG2-F-PEG4-M 13, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-PEG4- F3(b) 13, 40M

[0384] In embodiments, a compound including a delivery construct is selected from any one of Table 14 In embodiments, a compound including a delivery construct is selected from Table 14 wherein M is OH.Delivery construct-cargo conjugates

[0385] A compound that includes a delivery construct can include a cargo and a delivery construct can be called a delivery construct-cargo conjugate, or cargo conjugate A delivery construct or a compound that includes a delivery construct (e.g,, compounds that include a reactive handle) can be conjugated to a cargo to provide a delivery construct-cargo conjugate, otherwise termed a cargo conjugate. A cargo conjugate includes a delivery construct of the present disclosure and a cargo that is a therapeutic moiety or therapeutic agent. The therapeutic moiety may be any suitable therapeutic moiety for treating a disease. As used herein, the terms “therapeutic moiety” or “therapeutic agent” refer to any molecule (e.g., polypeptide, small molecule, oligonucleotide, gene editing machinery, or combination thereof) that is designed to have and / or has prophylactic or other biological activity. In embodiments, the therapeutic moiety selectively binds to a target molecule associated with a disease. In embodiments, the target molecule is a macromolecule implicated in a disease or pathology. In embodiments, the target molecule is a polypeptide or protein. In embodiments, the target molecule is an oligonucleotide. In embodiments, the oligonucleotide target comprises DNA, In embodiments, the oligonucleotide target comprises genomic DNA. In embodiments, the oligonucleotide target comprises RNA. In embodiments, theoligonucleotide target comprises mRNA. In embodiments, the target molecule is associated with a di sease. In embodiments, selective binding of the therapeutic moiety with the target molecule is useful for the treatment of a disease, pathology or other abnormal state or condition. In embodiments, selective binding of the therapeutic moiety to the target molecule upregulates expression or activity of the target molecule. In embodiments, selective binding of the therapeutic moiety to the target molecule downregulates expression or activity of the target molecule.

[0386] In embodiments, the therapeutic moiety comprises a therapeutic oligonucleotide. In embodiments, the therapeutic moiety comprises a polypeptide. In embodiments, the therapeutic moiety comprises a small molecule. In embodiments, the therapeutic moiety includes one or more components of gene editing machinery.

[0387] In embodiments, the therapeutic moiety is designed to treat a neuromuscular disease. Examples of neuromuscular disease include, but are not limited to various muscular dystrophies including Duchenne muscular dystrophy, Becker muscular dystrophy, Emery-Dreifuss muscular dystrophy, congenital muscular dystrophy, limb-girdle muscular dystrophy, oculopharayngeal muscular dystrophy, mytonic dystrophy, facioscapulohumeral muscular dystrophy, and the like.

[0388] In embodiments, the therapeutic moiety comprises a therapeutic oligonucleotide designed to treat a neuromuscular disease. In embodiments, the therapeutic moiety comprises a polypeptide designed to treat a neuromuscular disease. In embodiments, the therapeutic moiety comprises includes one or more components of gene editing machinery designed to treat a neuromuscular disease.Therapeutic Oligonucleotides

[0389] In embodiments, the therapeutic moiety comprises a therapeutic oligonucleotide. In embodiments, the therapeutic oligonucleotide comprises an antisense oligonucleotide (ASO). In embodiments, the therapeutic oligonucleotide comprises siRNA, RNAi, microRNA, antagomir, an aptamer, a ribozyme, an immunostimulatory oligonucleotide, a decoy oligonucleotide, a supermir, a miRNA mimic, a miRNA inhibitor, or a combination thereof (See, for example, Chery, J., “RNA therapeutics: RNAi and antisense mechanisms and clinical applications,” Postdoc J, July 2016, 4(7):35-50, and Zhu, et al., “RNA-based therapeutics: an overview and prospectus,: Cell Death & Disease, 23 July 2022, 12(644) (doi: 10.1038 / s41419-022-05075-2).

[0390] In embodiments, therapeutic oligonucleotides are provided that include from about 5 to about 100 nucleic acids. In embodiments, the therapeutic oligonucleotide is from about 5 to about50, about 8 to about 40, about 10 to about 30, about 15 to about 30, or about 20 to about 30 nucleotides in length. In embodiments, the therapeutic oligonucleotide includes one or more modified nucleosides, one or more modified internucleoside linkages, one or more conjugate groups, or combinations thereof.Antisense Oligonucleotides (ASO)

[0391] In embodiments, the therapeutic oligonucleotide is an antisense oligonucleotide (ASO) directed to a target gene or a target transcript associated with a disease. The ASO may be directed to and bind to a target nucleotide sequence located within a target gene or a target transcript. In embodiments, the target nucleotide sequence is within a target gene and / or target transcript associated with a disease.

[0392] The term “antisense oligonucleotide” refers to an oligonucleotide that is at least partially complementary to a target sequence within a target polynucleotide. An antisense oligonucleotide (ASO) is a single stranded molecule that contains DNA, RNA, or combinations or modifications thereof that are at least partially complementary to a chosen sequence, e.g., a target nucleotide sequence within a target gene or target transcript.

[0393] An ASO may modulate one or more aspects of gene expression and / or protein function via hybridization of the ASO with a target nucleotide sequence. The ASO may modulate one or more aspects of gene expression and / or protein function through various mechanisms. For example, hybridization of an ASO to a target nucleotide sequence of a target transcript may modulate splicing of a target transcript such as, for example, via exon skipping; exon inclusion; alternative splicing; prevent polyadenylation of the target transcript; increase the target transcript stability; induce target transcript degradation; prevent translation of the target transcript; or any combination thereof ASOs have been demonstrated to be effective and targeted inhibitors of protein synthesis, and, consequently, can be used to modulate gene expression of a targeted gene.

[0394] In embodiments, the ASO hybridizes with a target sequence of a target gene or target transcript having a sequence from about 5 to about 50 nucleotides in length, which can also be referred to as the length of the ASO. In embodiments, the ASO is from about 5 to about 50, about 8 to about 40, about 10 to about 30, about 15 to about 30, or about 20 to about 30 nucleotides in length. In embodiments, the ASO is at least about 5, about 6, about 7, about 8, about 9, about 10, about 11, about 12, about 13, about 14, or about 15, and up to about 16, about 17, about 18, about 19, about 20, about 21, about 22, about 23, about 24, about 25, about 26, about 27, about 28, about29, about 30, about 31, about 32, about 33, about 34, about 35, about 36, about 37, about 38, about 39, about 40, about 41, about 42, about 43, about 44, about 45, about 46, about 47, about 48, about 49, or about 50 nucleotides in length. In embodiments, the ASO is about 15 nucleotides in length. In embodiments, the ASO is about 16 nucleotides in length. In embodiments, the ASO is about 17 nucleotides in length. In embodiments, the ASO is about 18 nucleotides in length. In embodiments, the ASO is about 19 nucleotides in length. In embodiments, the ASO is about 20 nucleotides in length. In embodiments, the ASO is about 21 nucleotides in length. In embodiments, the ASO is about 22 nucleotides in length. In embodiments, the ASO is about 23 nucleotides in length. In embodiments, the ASO is about 24 nucleotides in length. In embodiments, the ASO is about 25 nucleotides in length. In embodiments, the ASO is about 26 nucleotides in length. In embodiments, the ASO is about 27 nucleotides in length. In embodiments, the ASO is about 28 nucleotides in length. In embodiments, the ASO is about 29 nucleotides in length. In embodiments, the ASO is about 30 nucleotides in length.

[0395] In embodiments, the ASO may be less than about 100 percent complementary to a target nucleotide sequence. As used herein, the term ‘‘percent complementarity” refers to the number of nucleobases of an ASO that have nucleobase complementarity with a corresponding nucleobase of target nucleotide sequence by the total length (number of nucleobases) of the ASO. One skilled in the art recognizes that the inclusion of mismatches is possible without eliminating the activity of the antisense compound. In embodiments, the ASOs contain no more than about 15%, no more than about 10%, no more than 5%, or no mismatches. In embodiments, the ASOs are at least about 80 ), at least about 85%, at least about 90%, at least about 95%, at least about 96%), at least about 97%, at least about 98%, at least about 99%, about 100%, or 100% complementary' to a target nucleic acid. Percent complementarity of an oligonucleotide is calculated by dividing the number of complementary' nucleobases by the total number of nucleobases of the oligonucleotide. Percent complementarity of a region of an oligonucleotide is calculated by dividing the number of complementary nucleobases in the region by the total number of nucleobases region.

[0396] In embodiments, incorporation of nucleotide affinity modifications allows for a greater number of mismatches compared to an unmodified compound. Similarly, certain oligonucleotide sequences may be more tolerant to mismatches than other oligonucleotide sequences. One of ordinary skill in the art is capable of determining an appropriate number of mismatches between a an ASO and a target nucleotide sequence, such as by determining melting temperature (Tm). Tmor change in Tm (ATm) can be calculated by techniques that are familiar to one of ordinary skill in the art. For example, techniques described in Freier et al. (Nucleic Acids Research, 1997, 25, 22: 4429-4443) allow one of ordinary skill in the art to evaluate nucleotide modifications for their ability to increase the melting temperature of an RNA: DNA duplex.Therapeutic oligonucleotides design

[0397] Design of a therapeutic oligonucleotides (e.g., an ASO) will depend upon the target gene. Targeting a therapeutic oligonucleotide to a particular target nucleotide sequence can be a multistep process. The process usually begins with the identification of gene of interest. The transcript of the gene of interest is analyzed and a target nucleotide sequence is identified. In embodiments, the target gene is a gene associated with a disease.

[0398] One of skill in the art will be able to design, synthesize, and screen therapeutic oli onucleotides of different nucleobase sequences to identify a sequence that results in antisense activity For example, a therapeutic oligonucleotide can be designed that inhibits expression of a target gene. Methods for designing, synthesizing, and screening therapeutic nucleotides for antisense activity against a preselected target nucleic acid and / or target gene can be found, for example in " Antisense Drug Technology, Principles, Strategies, and Applications" Edited by Stanley T. Crooke, CRC Press, Boca Raton, Florida, which is incorporated by reference in its entirety for any purpose.

[0399] The efficacy of a therapeutic oligonucleotide (e.g., an ASO) may be assessed by evaluating the antisense activity effected by their administration. As used herein, the term "antisense activity" refers to any detectable and / or measurable activity attributable to the hybridization of a therapeutic oligonucleotide to its target nucleotide sequence. Such detection and / or measuring may be direct or indirect. In embodiments, antisense activity is assessed by detecting and or measuring the amount of target protein in a cell or population of cells before and after administration of the therapeutic oligonucleotide to the cell or population of cells. In embodiments, antisense activity is assessed by detecting and / or measuring the amount of target transcript in a cell or population of cells.Therapeutic Oligonucleotides Structure

[0400] Therapeutic oligonucleotides (e.g., ASOs) are nucleosides linked through internucleoside linkages. Nucleosides include a pentose sugar (e.g., ribose or deoxyribose) a sugar substitute, or a modified sugar and a nitrogenous base (nucleobase) covalently attached to sugar, sugarsubstitute, or modified sugar. The naturally occurring nucleobases found in DNA and / or RNA are adenine (A), guanine (G), thymine (T), cytosine (C), and uracil (U). The naturally occurring sugars found in DNA and / or RNA are deoxyribose (DNA) and ribose (RNA). The naturally occurring internucleoside linkage is a phosphodiester. In embodiments, the ASO may have all natural sugars, natural bases, and natural internucleoside linkages.

[0401] Chemically modified nucleosides and / or modified intemucleoside linkages can be incorporated into therapeutic oligonucleotides. Such modifications can enhance one or more properties, such as nuclease resistance, pharmacokinetics or affinity for a target gene or target transcript. Non-limiting examples of modified nucleosides and modified intemucleoside linkages are shown in FIG. 1.

[0402] In general, a nucleobase is any group that contains one or more atoms or groups of atoms capable of hydrogen bonding to a base of another nucleic acid. In addition to natural nucleobases, many modified nucleobases or nucleobase mimetics known to those skilled in the art are amenable with the compounds described herein. The terms modified nucleobase and nucleobase mimetic can overlap but generally a modified nucleobase refers to a nucleobase that is fairly similar in structure to the parent nucleobase, whereas a nucleobase mimetic generally includes more complicated structures Examples of modified nucleobases include 2 -thiodeoxythymine (see structure 4 in FIG. 1) 7-deaza purine 5-mehtyl cytosine, G-clamp. An example of a nucleobase mimetic is tricyclic phenoxazine nucleobase mimetic. Methods for preparation of the above noted modified nucleobases are well known to those skilled in the art.

[0403] In embodiments, a therapeutic oligonucleotide includes one or more modified nucleosides having a modified sugar moiety. The furanosyl sugar ring of a natural nucleoside can be modified. A furanosyl sugar ring may be modified in any suitable manner, including, but not limited to, addition of a substituent group, bridging of two non-geminal ring atoms to form a bicyclic nucleic acid (BNA), and substitution of an atom or group such as -S-, -N(R)- or -C(R’)(R2) for the ring oxygen at the eposition. Modified sugar moieties are well known and can be used to alter, typically increase, the affinity of the ASO for its target and / or increase nuclease resistance. A representative list of modified sugars includes but is not limited to non-bicyclic substituted sugars, especially non-bicyclic ^'-substituted sugars having a 2'-F, 2'-OCH3 or a 2-O(CH2)2-OCH3 substituent group (see structures 5 to 8 of FIG. 1 for examples); and 4'-thio modified sugars. The ring of a sugar can be opened, for example between the 2' and 3' position.to result in an unlocked nucleotide (see structure 14 of FIG. 1). Sugars can also be replaced with a sugar mimetic group, for example, a morpholino ring, or a methylenemorpholine (FIG. 2, structure 1) ring, among others.

[0404] In embodiments, a therapeutic oligonucleotide may include one or more bicyclic modified sugars (BNA's), such as, for example, LNA (4'-(CH2)-O-2' bridge, see structure 9 of FIG. 1), 2r-thio-LNA (4'-(CH2)-S-2rbridge), tricyclo DNA (see structure 11 of FIG. 1) 2'-amino-LNA (4'-(CH2)-NR-2' bridge), ENA (4'-(CH2)2-O-2' bridge), 4'-(CH2)3-2' bridged BNA, 4'-(CH2CH(CH3))-2' bridged BN; cEt (4'-(CH(CH3)-O-2' bridge, see structure 10 or FIG. 1), and cMOE BNAs (4'-(CH(CH2OCH3)-O-2' bridge).

[0405] In embodiments, a therapeutic oligonucleotide may include one or more locked nucleic acids (LNAs) in which the 2'-hydroxyl group of the ribosyl sugar ring is linked to the 4' carbon atom of the sugar ring thereby forming a 2'-C,4'-C-oxymethylene linkage resulting in a bicyclic sugar moiety. The synthesis and preparation of the LNA monomers adenine, cytosine, guanine, 5 -methyl -cytosine, thymine and uracil, along with their oligomerization, and nucleic acid recognition properties have been described (Koshkin et al., Tetrahedron, 1998, 54, 3607-3630). LNAs and preparation thereof are also described in WO 98 / 39352 and WO 99 / 14226.

[0406] In embodiments, a therapeutic oligonucleotide has one or more modified internucleoside linkages. Internucleoside linking groups link the nucleosides (natural or modified) monomer units of an oligonucleotide together. The two main classes of internucleoside linking groups are defined by the presence or absence of a phosphorus atom Representative phosphorus containing internucleoside linkages include, but are not limited to, phosphodiesters, phosphotriesters, vinyl phosphonates (see structure 15 of FIG. 1), alkyphosphonates (see structure 16 of FIG. 1), phosphorami date, phosphorodiamidate (see structure 3 of FIG. 1), and phosphorothioates (see structures 1, 17, and 18 of FIG. 1). Representative non-phosphorus containing internucleoside linking groups include, but are not limited to, methylenemethylimino (-CH2-N(CH3)-O-CH2-), thiodiester (-O-C(O)-S-), thionocarbamate (-O-C(O)(NH)-S-); siloxane (-O-Si(H)2-O-); and N, N'-dimethylhydrazine (-CH2-N(CIL)-N(CH3)-). ASOs having non-phosphorus internucleoside linking groups are referred to as oligonucleosides. Modified internucleoside linkages, compared to natural phosphodiester linkages, can be used to alter, typically increase, nuclease resistance of the oligonucleotides. Internucleoside linkages having a chiral atom can be prepared racemic, chiral, or as a mixture. Representative chiral internucleoside linkages include, but are not limitedto, alkylphosphonates and phosphorothioates. Methods of preparation of phosphorous-containing and non-phosphorous-containing linkages are well known to those skilled in the art.

[0407] In embodiments, a phosphate group can be linked to the 2', 3 ', or 5' (or 6', for a 6 membered ring, such as a methylenemorpholine ring) hydroxyl moiety of the sugar (or modified sugar). In forming oligonucleotides, the phosphate groups covalently link adjacent nucleosides to one another to form a linear polymeric compound. Within oligonucleotides, the phosphate groups are commonly referred to as forming the internucleoside backbone of the oligonucleotide. The natural linkage of an RNA or DNA backbone is a 3' to 5' phosphodiester linkage. In this linkage, a 5' phosphate group of a nucleotide is linked to the 3' hydroxy of the adjacent 5' nucleotide in a phosphodiester bond.

[0408] In embodiments, a therapeutic oligonucleotide is a phosphorodiamidate morpholino oligomer (PMO). A PMO has nucleosides that include a methylene morpholine ring conjugated to nucleobase (see structure 1 of FIG. 2). The PMO nucleoside monomers units are coupled through phosphorodiamidate internucleoside linkages (see structure 2 of FIG. 2). The 5' terminal nucleotide of a PMO may lack a 5' phosphate group. For example, the 5' terminal nucleotide of a PMO may have 5' hydroxyl group, FIG. 2, structure 2, shows a three nucleotide PMO, The 5' nucleotide has a terminal 5' hydroxyl group. The 3' nucleotide has 3' terminal NH group. PMOs are uncharged nucleic acid analogs that bind to a target nucleic acid through base paring. As uncharged, or net neutral charged, oligonucleotides, PMOs are particularly effective for intracellular delivery when conjugated to a delivery construct of the present disclosure.

[0001] In embodiments, the ASO is a peptide nucleic acid (PNA). PNAs have a backbone of N-(2-aminoethyl) glycine monomers conjugated via amide bonds. Each N-(2-aminoethyl) glycine monomer includes a nucleobase attached via a methyl carbonyl linker. FIG. 3 shows a PNA structure. The PNA includes an N-terminus and an N-terminal nucleobase (Bn). The N-terminus of a PNA can also be described as the 5' end of a PNA. The PNA includes a C-terminus and a C-terminal nucleobase (Bc). The C-terminus of a PNA can also be described as the 3' end of a PNA. Between the N-terminus and the C-terminus, the PNA includes one or more nucleobases (Bn-Bc) each nucleobase attached to a N-(2-aminoethyl) glycine repeat monomer.

[0002] In one or more embodiments, the ASO is a PNA. In one or more embodiments, the ASO is a PNA and includes any ASO sequence disclosed herein. In one or more embodiments, the ASO is a PNA such as any ASO sequence disclosed herein.Gene-Editing Machinery

[0003] In embodiments, the therapeutic moiety comprises one or more component of gene-editing machinery. As used herein, "‘gene-editing machinery” refers to protein, nucleic acids, or combinations thereof, which may be used to edit a genome. Non-limiting examples of gene-editing machinery include guide RNAs (gRNAs), nucleases, nuclease inhibitors, and combinations and complexes thereof.

[0004] The gene editing machinery may be used to repair a mutated gene or to introduce a mutation into a gene. The gene may be a gene associated with a disease.

[0005] In embodiments, a linker conjugates the delivery construct to the one or more components of gene-editing machinery. Any linker described in this disclosure or that is known to a person of skill in the art may be utilized.gRNA

[0006] In embodiments, the therapeutic moiety includes a guide RNA (gRNA). A gRNA targets a genomic loci in a prokaryotic or eukaryotic cell.

[0007] In embodiments, the gRNA is a single-molecule guide RNA (sgRNA). A sgRNA includes a spacer sequence and a scaffold sequence. A spacer sequence is a short nucleic acid sequence used to target a nuclease (e.g., a Cas9 nuclease) to a specific nucleotide region of interest (e.g., a genomic DNA sequence to be cleaved). In embodiments, the spacer may be about 17-24 bases in length, such as about 20 bases in length.

[0008] In embodiments, the spacer targets a site that immediately precedes a 5' protospacer adjacent motif (PAM). The PAM sequence may be selected based on the desired nuclease. For example, the PAM sequence may be any one of the PAM sequences shown in Table 14 below, wherein N refers to any nucleic acid, R refers to A or G, Y refers to C or T, W refers to A or T, and V refers to A or C or G.Table 14. Nucleases and PAM sequencesPAM sequence (5' to 3') Nuclease Isolated fromNGG SpCas9 Streptococcus pyogenes NGRRT or NGRRN SaCas9 Staphylococcus aureus NNNN GA TT NmeCas9 Neisseria meningitidis NNNNRYAC CjCas9 Campylobacter j ejuniPAM sequence (5' to 3') Nuclease Isolated fromNNAGAAW StCas9 S treptococcus th ermophil e s TTTV LbCpfl Lachnospiraceae bacterium TTTV AsCpfl Acidaminococcus sp.

[0009] In embodiments, a spacer may target a sequence of a mammalian gene, such as a human gene. In embodiments, the spacer may target a mutant gene. In embodiments, the spacer may target a coding sequence. In embodiments, the spacer may target an exonic sequence. In embodiments, the spacer may target a polyadenylation site (PS). In embodiments, the spacer may target a sequence element of a PS, In embodiments, the spacer may target a polyadenylation signal (PAS), an intervening sequence (IS), a cleavage site (CS), a downstream element (DES), or a portion or combination thereof. In embodiments, a spacer may target a splicing element (SE) or a cis-splicing regulatory element (SRE).

[0010] The scaffold sequence is the sequence within the sgRNA that is responsible for nuclease (e.g, Cas9) binding. The scaffold sequence does not include the spacer / targeting sequence. In embodiments, the scaffold may be about 10 to about 150 nucleotides in length, or about 50 to about 100 nucleotides in length.

[0011] In embodiments, the gRNA is single guide RNA molecule comprising the spacer and the scaffold. In embodiments, the gRNA comprises two molecules that hybridize to form the gRNA. An example of a gRNA that includes two molecules is a gRNA comprising a crRNA and tracrRNA. In embodiments, the gRNA or one or more components thereof may further include a poly(A) tail.

[0012] In embodiments, a compound that includes a CPP is conjugated to a nucleic acid that includes a gRNA or a component thereof. In embodiments, the nucleic acid includes about 1, about 2, about 3, about 4, about 5, about 6, about 7, about 8, about 9, about 10, about 11, about 12, about 13, about 14, about 15, about 16, about 17, about 18, about 19, or about 20 gRNAs or components thereof In embodiments, the gRNAs recognize the same target. In embodiments, the gRNAs recognize different targets.

[0013] In embodiments, a compound that includes a CPP is conjugated to a nucleic acid designed to express the gRNA within a cell. The nucleic acid may include a promoter sequence to drive expression of the gRNA,Nuclease

[0014] In embodiments, the therapeutic moiety includes a nuclease. In embodiments, the nuclease is a Type II, Type V-A, Type V-B, Type VC, Type V-U, Type VI -B nuclease. In embodiments, the nuclease is a transcription, activator-like effector nuclease (TALEN), a meganuclease, or a zine-finger nuclease or a modified form or variant thereof. In embodiments, the nuclease is a Cas9, Casl2a (Cpfl), Casl2b, Casl2c, Tnp-B like, Casl3a (C2c2), Casl3b, or Casl4 nuclease or a modified form or variant thereof. For example, in embodiments, the nuclease is a Cas9 nuclease or a Cpfl nuclease.

[0015] In embodiments, the delivery construct is conjugated to a nucleic acid encoding a nuclease. In embodiments, the nucleic acid encoding a nuclease includes a sequence encoding a promoter, wherein the promoter drives expression of the nuclease.gRNA Mid Nuclease Combinations

[0016] In embodiments, the therapeutic moiety includes a ribonucleoprotein (RNP) that includes a gRNA and a nuclease. A RNP is a complex of a gRNA bound to a nuclease. The gRNA, the nuclease, or both may be covalently attached to a delivery construct to form a cargo conjugate having an RNP therapeutic moiety.

[0017] In embodiments, a composition that includes: (a) a cargo conjugate comprising a delivery' construct conjugated to a gRNA and (b) a nuclease is delivered to a cell. In embodiments, a composition that includes: (a) a cargo conjugate comprising a delivery construct conjugated to a nuclease and (b) an gRNA is delivered to a cell. In embodiments, a composition that includes: (a) a first cargo conjugate comprising a first delivery construct conjugated to a gRNA and (b) a second cargo conjugate comprising a second delivery construct conjugated to a nuclease is delivered to a cell. In embodiments, the first delivery construct and the second delivery construct are the same. In embodiments, the first delivery construct and the second delivery construct are different.

[0018] In embodiments, a cargo conjugate comprises a delivery constaict conjugated to a nucleic acid encoding a gRNA and / or a nuclease. In embodiments, the nucleic acid encoding a nuclease and a gRNA includes a sequence encoding a promoter, wherein the promoter drives expression of the nuclease and the gRNA. In embodiments, the nucleic acid encoding a nuclease and a gRNA includes two promoters, wherein a first promoter controls expression of the nuclease and a second promoter controls expression of the gRNA. In embodiments, the nucleic acid encoding a gRNA and a nuclease encodes from about 1 to about 20 gRNAs, or from about 1, about 2, about 3, about4, about 5, about 6, about 7, about 8, about 9, about 10, about 11, about 12, about 13, about 14, about 15, about 16, about 17, about 18, or about 19, and up to about 20 gRNAs. In embodiments, the gRNAs recognize different targets. In embodiments, the gRNAs recognize the same target.Nuclease Inhibitors

[0019] In embodiments, the therapeutic moiety includes a nuclease inhibitor. A limitation of gene editing is potential off-target editing. The delivery of a nuclease inhibitor may limit off-target editing. In embodiments, the nuclease inhibitor is a polypeptide, polynucleotide, or small molecule.Therapeutic polypeptides

[0020] In embodiments, the therapeutic moiety includes a therapeutic polypeptide. In embodiments, the therapeutic polypeptide includes a peptide inhibitor. In embodiments, the peptide inhibitor inhibits a protein associated with a disease. In embodiments, the therapeutic polypeptide includes a peptide replacement therapy to functionally replace an aberrantly expressed protein associated with a disease.

[0021] In embodiments, the therapeutic moiety includes a protein or a fragment thereof. In embodiments, the therapeutic moiety includes an RNA binding protein or an RNA binding fragment thereof. In embodiments, the therapeutic moiety includes an enzyme In embodiments, the therapeutic moiety includes an RNA-cleaving enzyme or an active fragment thereof.Antibodies

[0022] In embodiments, the therapeutic moiety includes an antibody or an antigen-binding fragment. Antibodies and antigen-binding fragments can be derived from any suitable source, including human, mouse, camelid (e.g., camel, alpaca, llama), rat, ungulates, or non-human primates (e.g., monkey, rhesus macaque).

[0023] The term “antibody” includes intact polyclonal or monoclonal antibodies and antigen¬ binding fragments thereof. For example, a native immunoglobulin molecule includes two heavy chain polypeptides and two light chain polypeptides. Each of the heavy chain polypeptides associate with a light chain polypeptide by virtue of interchain disulfide bonds between the heavy and light chain polypeptides to form two heterodimeric proteins or polypeptides (i.e., a protein that includes two heterologous polypeptide chains). The two heterodimeric proteins then associate byvirtue of additional interchain disulfide bonds between the heavy chain polypeptides to form an immunoglobulin protein or polypeptide.

[0024] In embodiments, the therapeutic moiety is an antigen-binding fragment that binds to a target protein associated with a disease. An antibody may modulate the activity of the target protein to which it binds. In embodiments, the therapeutic moiety is an antigen-binding fragment that binds to a target transcript of a protein (Ye et al., PNAS (2008), 105(1 ):82-87; and Jung et al., RNA (2014), 20(6): 805-814). In embodiments, an antigen-binding fragment that binds to a target protein includes 1, 2, 3, 4, 5, or all 6 CDRs of a variable heavy chain (VH) and / or a variable light chain (VL) sequence from an antibody that specifically binds to the target protein. In embodiments, the antigen binding fragment includes 1, 2, or 3 of the CDRs of a camelid single domain antibody such as the VHH region. In embodiments, the antigen-binding fragment that binds to a target protein is a portion of a full-length antibody, such as Fab, F(ab’)2, Fab’, Fv fragments, minibodies, diabodies, single domain antibody (dAb), single-chain variable fragments (scFv), multispecific antibodies formed from antibody fragments, or any other modified configuration of the immunoglobulin molecule that includes an antigen-binding site or fragment of the appropriate specificity.

[0025] In embodiments, the therapeutic moiety includes a bispecific antibody. Bispecific antibodies (BsAbs) are antibodies that can simultaneously bind two separate and unique antigens (or different epitopes of the same antigen). In embodiments, the therapeutic moiety includes a bi specific antibody that can simultaneously bind to a target protein associated with a disease and another target protein. Non-limiting examples include scFv (single-chain variable fragment), BsDb (bispecific diabody), scBsDb (single-chain bispecific diabody), scBsTaFv (single-chain bispecific tandem variable domain), DNL-(Fab)3 (dock-and-lock trivalent Fab), sdAb (single-domain antibody), and BssdAb (bispecific single-domain antibody).

[0026] BsAbs with an Fc region are useful for carrying out Fc mediated effector functions such as antibody-dependent cell-mediated cytotoxicity and complement-dependent cytotoxicity. They have the half-life of normal IgG. On the other hand, BsAbs without the Fc region (bispecific fragments) rely solely on their antigen-binding capacity for carrying out therapeutic activity. Due to their smaller size, these fragments have better solid-tumor penetration rates. BsAb fragments do not require glycosylation, and they may be produced in bacterial cells. The size, valency, flexibility and half-life of BsAbs to suit the application

[0027] In embodiments, the therapeutic moiety includes a “diabody.” The term diabody refers to a bispecific antigen-binding antibody fragment in which VH and X domains are expressed in a single polypeptide chain using a linker that is too short to allow for pairing between the two domains on the same chain, thereby forcing the domains to pair with complementary domains of another chain and creating two antigen-binding sites (see, e.g., Holliger et al., Proc. Natl. Acad. Sei. USA 90:6444-48 (1993) and Poljak et al., Structure 2:1121- 23 (1994)). Diabodies may be designed to bind to two distinct antigens and are bi-specific antigen binding constructs.

[0028] In embodiments, the therapeutic moiety includes a “nanobody” or a “single domain antibody” (which can also be referred to herein as sdAbs or VHH). Single domain antibody refers to an antigen-binding fragment that includes a single monomeric variable antibody domain comprising one variable domain (VH) of a heavy-chain antibody. In embodiments, the variable chain is the VHH of a camelid single chain antibody.

[0029] In embodiments, the therapeutic moiety includes a minibody.

[0030] In embodiments, the therapeutic moiety’ is an antibody mimetic. Antibody mimetics are compounds that, like antibodies, can specifically bind antigens, but that are not structurally related to antibodies. They are usually artificial peptides or proteins with a molar mass of about 3 to 20 kD (compared to the molar mass of antibodies at -150 kDa ). Examples of antibody mimetics include affibody molecules affilins, affiraers, affitins, alphabodies anticalins, avimers, D. ARPins, fynomers Kunitz domain peptides and monobodies.Other Peptides

[0031] In embodiments, the therapeutic moiety includes a peptide. In embodiments, the peptide acts as an agonist, increasing the activity of a target protein. In embodiments, the peptide acts as an antagonist, decreasing the activity of a target protein. In embodiments, the peptide is configured to inhibit protein-protein interaction (PPI). Protein-protein interactions (PPIs) are important in many biochemical processes, including transcription of nucleic acid and various post-translational modifications of translated proteins. PPIs can be experimentally determined by biophysical techniques such as X-ray crystallography, NMR spectroscopy, surface plasma resonance (SPR), bio-layer interferometry (BLI), isothermal titration calorimetry (ITC), radio-ligand binding, spectrophotometric assays and fluorescence spectroscopy. Peptides that inhibit protein-protein interaction can be referred to as peptide inhibitors.

[0032] In embodiments, the therapeutic moiety includes a peptide inhibitor. Tn embodiments, the peptide inhibitor includes from about 5 to about 100 amino acids, from about 5 to about 50 amino acids; from about 15 to about 30 amino acids; or from about 20 to about 40 amino acids. In embodiments, the peptide inhibitor includes one or more chemical modifications, for example, to reduce proteolytic degradation and / or to improve in vivo half-life. In embodiments, the peptide inhibitor includes one or more synthetic amino acids and / or a backbone modification. In embodiments, the peptide inhibitor has an cx-helical structure.

[0033] In embodiments, the peptide inhibitor is configured to disrupt one or more function of a protein associated with a disease. In embodiments, the peptide inhibitor is configured to disrupt formation of protein complexes. In embodiments, binding of the peptide inhibitor to the protein blocks dimer formation.Small Molecules

[0034] In embodiments, the therapeutic moiety includes a small molecule for treating a disease. In embodiments, the small molecule does not readily gain access to an intracellular compartment of a cell when delivered by itself (not conjugated to a delivery construct).

[0035] In embodiments, a cargo-conjugate is of Formula V:Formula V,, o H RW-(AA1)S-(L1£,NY' f '< k / y'HH O^zA t y 'n < O o yy R» R{_ y N UN — ^. Q o^NHHN2R6'A"-< NH HN0O^^y-NH ^_ / ''R3R5 / W" %0 ^4 pharmaceutically acceptable salt thereof,wherein:m* is 0 or 1:M' is a coupling group; andR20, AA1, al, LI, bl, y, n, AA2, a2, L2, b2, AA3, a3, L3, b3, AA4, and cargo are defined herein.

[0036] Cargo-conjugates of Formula V can be formed from compounds of Formula III. For example, a compound of Formula III can be reacted with cargo to form a cargo-conjugate of Formula V.

[0037] Compounds including a delivery construct of Formula I can be cargo-conjugates of Formula V when the delivery construct of Formula I is covalently attached to a cargo directly (m* is 0) or through a coupling group (M'j.

[0038] In embodiments, a cargo-conjugate is of FormulaVI:Formula VI,, 0 H HN 1..— (AA1 ' '(L2) — (AA3) — (L3) — (AA4) — (L4J — (l$5^™c«argo / h v V NOwherin:m* is 0 or 1;M is a coupling group; andR20, AA1, al, LI, bl, y, n, a2, L2, b2, AA3, a3, L3, b3, AA4, and cargo are defined herein.

[0039] Cargo-conjugates of Formula VI can be formed from compounds of Formula IV. For example, a compound of Formula IV can be reacted with a cargo to form a cargo-conjugate of Formula VI.

[0040] Compounds that include a delivery construct of Formula II can be cargo-conjugates of Formula VI when the delivery construct of Formula II is covalently attached to a cargo directly (m* is 0) or through a bonding group (M').

[0041] In embodiments, the cargo is an oligonucleotide In embodiments, the oligonucleotide is an antisense oligonucleotide. In embodiments, the oligonucleotide is a phosphorodiamidate morpholino oligonucleotide (PMO). In embodiments, the cargo is an ASO designed to treat a muscle disease In embodiments, a cargo is an PMO designed to treat a muscle disease.Coupling Group: M'

[0042] A compound including a delivery construct can include a terminal reactive handle that reacts with a complementary reactive handle on the cargo to form the delivery construct-cargo conjugate. In embodiments, post conjugation, the cargo is directly coupled to the delivery construct. In other embodiments, post conjugation, the cargo is coupled to the delivery construct through a coupling group M'. In embodiments when M' is present in the compound, M' can include at least a portion of the reaction product of the two reactive handles and, optionally, one or more additional atoms or groups.

[0043] m* can be 0 or 1. In embodiments, m* is 0. In embodiments m* is 1.

[0044] When m* is 0, the delivery construct is directly attached to the cargo. For example, in embodiments when the cargo is a PMO and m* is 0, the delivery' construct is covalently bonded to the free secondary' amine of the morpholino ring of the 3' terminal end of a PMO. For example, in embodiments when m* is 0 and the cargo is a PMO, the connection between the, O., B1.T-yPMO cargo and the deliver}' construct canbe ** where B1is the 3' terminal nucleobase of the PMO cargo, * indicates the point of attachment to the remaining PMO cargo, and ** indicates the point of attachment to delivery construct.

[0045] In embodiments when the cargo is a PNA and m* is 0, the delivery’ construct can be covalently bonded to the free amine of the N-terminus of a PNA. For example, in embodiment when m* is 0 and the cargo is a PNA, the connection between the PNA cargo and the deliveryconstruct can bewhere Bnis the N-terminal nucleobase of the PNA cargo, indicates the point of attachment to the remaining PNA cargo, and ** indicates the point of attachment to delivery construct,

[0046] In embodiments when m* is 1, the compound comprises M' In embodiments, when m* is 1, the cargo is coupled to the larger delivery construct through M'.

[0047] M' can be covalently bound to any suitable location on the cargo. For example, M' can be covalently bound to the 3' end or 5' end of an ASO cargo.o

[0048] M' can include -NH-,' 't ', or a heteroaryl where t is an integer from 0 to 10. t can be an integer from 0 to 5. t can be an integer from 0 to 3.

[0049] In embodiments, M' is a bond to the cargo.

[0050] In embodiments, M' can include or be -NH- O

[0051] In embodiments, M' can includeor be ' 't ' where t is an integer from 0 to 5.

[0052] In embodiments, M' can include a heteroaryl. The heteroaryl may include the reaction product between an azide and cyclooctyne. For example, M' can be or includethereof where y" is an integer from 1 to 4. In embodiment when y" is 4, the heteroaryl containing group is the reaction product between azidolysine and cyclooctyne.

[0053] M' can be covalently bound to 3' end or the 5' end of an ASO cargo. In embodiments M' is covalently bound to the 3' end of the ASO cargo. In embodiments M' is covalently bound to the 5' end of an ASO cargo. In embodiments where the cargo is a PMO, M' can form a bond to the free hydroxyl of the of the 5' terminal nucleotide of an PMO.

[0054] In embodiments when the cargo is a PMO, M' is a bond to the free secondary' amine of the morpholino ring of the 3' terminal nucleotide of the PMO.

[0055] In embodiments, the M' may include a heteroaryl and one or more -CH2CH2O- units. For example, in embodiments, M' can include or beo cO''’xS '13W H#1 L. A, NH§ H VH AOwhere #1 is the M' point of attachment to the delivery construct, #2 is the point of attachment to the cargo, y" is an integer from 1 to 4, x3 is an integer from 1 to 4, and j3 is an integer from 1 to 4. In embodiment when y” is 4, the heteroaryl containing group is the reaction product between azidolysine and cyclooctyne. In embodiments, x3 is 2. In embodiments, x3 is 4. In embodiments, j 3 is 1. In embodiments, j 3 is 2. In embodiments, j is 3. In embodiments, j is 4. In embodiments, y" is 4, x3 is 4, and j3 is 1. In embodiments, j3 is 2. In embodiments, y", x3 is 4, and j3 is 2. In embodiments when the cargo isO / oA N t A / yN -'XA" HH:a PMO,0is directly attached to the free secondary amine of the morpholino ring of the 3' terminal nucleotide of a PMO.

[0056] In embodiments when m* is 0 or 1 and the compound comprises a C-terminal amino acid residue that has a side chain with a reactive moiety (e.g., lysine, glutamic acid, and the like), the compound may be coupled to the ASO through the C-terminal carboxylic acid (COOH) of the amino acid or through the side chain of the C-terminal amino acid. For example, when the compound comprises glutamic acid as a C-terminal amino acid, the ASO may be conjugated to the larger compound through the side chain of glutamic acid or through the C-terminal carboxylic acid of glutamic acid. In embodiments when the ASO is attached to the larger compound through the side chain a C-terminal amino acid residue, the C-terminal carboxylic acid may be modified or protected with a group other than a carboxylic acid. In embodiments when the ASO is attached to the larger compound through the C-terminal carboxylic acid of anamino acid residue having a side chain that comprises a reactive moiety, the reactive moiety of the side chain may be modified or protected

[0057] Examples of compounds (cargo-conjugates) of Formula V include those listed in Table 15A-15C and examples of cargo-conjugates of Formula VI include those listed in Table 15D In Tables 15A-15D, Ac is -C(O)CH3; the cCPP is written as JA(cyclo[XAXBXcXDXEXFXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with the side chain R1, R2, R3, R4, R5, R6, and R7, respectively, YAis the cCPP bridging amino acid residue, and JAis the bridging exocyclic amino acid residue; “miniPEG2” indicates ~-(CH2-CH2-O)2-CH2-CO-; “PEG#” indicates ~(CH2-CH2-O)#-CH2-CO- or-(CH2-CH2-O)#-CH2-CH2-CO- where # indicates to the number of -CH2-CH2O- units; M' can be absent (i.e., m* is 0) or any M' described herein (i.e., m* is 1); and cargo is any cargo described herein. In embodiments of the compounds of Tables 15A-15D,, each instance of “PEG#” refers to --(CH2-CH2-O)2-CH2-CO- (i.e., “miniPEG2”) and each instance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2. In embodiments of the compounds of Tables 15A-15D,,, each instance of “PEG2” refers to -(CH2-CH -O)2-CH2-CH2-CO- and each instance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2.Table 15 A.SEQ IDNo. Cargo-conjugateNOs: Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Bip-BRBRB-M'- cargo 18, 40, Ml(Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-Bip-BRBRB- 35 M'-cargo)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal-BRBRB-M'- cargo 18, 40, M2(Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal-BRBRB- 36 M'-cargo)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bta-B-M'-cargoM3 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-B-M'- 18, 40 cargo)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BRB-Bip-M'-cargo13, 40, M4 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-BRB-Bip-M'- 29 cargo)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BR-Bip-RB-M'- cargo 18, 40, MS(Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-BR-Bip-RB- 85M'-cargo)SEQ I D No. Cargo-conjugateNOs: Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-B-M'-cargoM6 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-B-M'-cargo)Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEGs-RF-M'-cargoM7 (Ac-PKKKRKV-miniPEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-RF-M'- 18, 38 cargo)Ac-KKKRK-PEG2-K(cyclo[GfFGrGrQ])-PEGs-RF-M'-cargoMS 13, 44 (Ac-KKKRK-miniPEG2-K(cyclo[GfFGrGrQ])-PECre-RF-M'-cargo)Ac-kkkRK-PEG2-K(cyclo[GfFGrGrQ])-PEGs-RF-M'-cargoM9 11, 44 (Ac-kkkRK-miniPEG2-K(cyclo[GtFGrGrQ])-PEG8-RF-M'-cargo)Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-M'-cargoMIO 18, 38 (Ac-PKKKRKV-miniPEG2-k('cyclo[Bta-G-Bta-GRGRQ])-PECh-M’-cargo)Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-K-Bip-M'-cargoMil 20, 40 (Ac-RBRRBR-miniPEG2-K(cyclo[FGFGRGRQ])-PEGs-K-Bip-M'-cargo)Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-M' -cargoM12 12, 40 (Ac-kkkrk-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-M’-cargo)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-M'-cargoM13 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-M'-cargo)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-rf-M'-cargoM14 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-rf-M'-cargo)M15 Ac-RBKKBR-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-M'-cargo 80, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FK-M'-cargoM16 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-FK-M'-cargo)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-M'-cargoM17 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bta-M'-cargo)Ac-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])- PEGs-RF -M'-cargoM18 14, 40 (Ac-K(me)-K(me)-K(me)-R(me)-K(me)-miniPEG2- K(cyclo[FGFGRGRQ])-PEG8-RF-M'-cargo)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Val-Cit-M'-cargoM19 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQJ)-rainiPEG2-Val-Cit-M'- 18, 40 cargo)Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-M'-cargoM20 (Ac-YAiYRRrGPR-mmiPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-M'- 21, 40 cargo)M21 Ac-RBRRBR-K(cYclo[FGFGRGRQl)-PEG8-Bip-M'-cargo 20, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-PEG2-M’-cargoM22 (Ac-KKKRK-mimPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-PEG2-M'- 13, 40cargo)SEQ I D No. Cargo-conjugateNOs: Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG2-M'-cargoM23 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-R-Bta- 13, 40 mimPEG2-M'-cargo)Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-M'-cargoM24 20, 40 (Ac-RBRRBR-K(cyclo[FGFGRGRQ])-miniPEG2-KF-PEG4-M'-cargo)Ac-KKKRK-PEG2-K(cyclo[FGFRHRHQ])-PEG2-RF-PEG4-MM25 13, 42 (Ac-KKKRK-miniPEG2-K(cyclo[FGFRHRHQ])-miniPEG2-RF-PEG4-M)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bta-PEG2-M'-cargoM26 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ)-PEG4-R-Bta-miniPEG2- 13, 40 M'-cargo)Ac-YArVRRrGPR-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4-M'-cargo M27 (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FfFGRGRQ])-mmiPEG2-RF- 21, 39 PEGi-M'-cargo)Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEG8-M,-cargoM28 40, 18 (Ac-K(cyclo[FGFGRGRQ])-miniPEG2-PKKKRKV-PEG8-M'-cargo)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-Bip-M'-cargoM29 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-rf-PEG4-Bip- 13, 40 M'-cargo)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-F-M'-cargo M30 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 18, 40 F-M’-cargo)Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bta-M'-cargo M31 (Ac-RBRRBR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 20, 40 Bta-M'-cargo)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Nal-M'-cargo M32 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-Nal- 13, 40 M'-cargo)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG4-Nal-M'-cargo M33 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG4-Nal-M'- 13, 40 cargo)Ac-PKKKRKV-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG2-Nal-M'- cargoM34 18, 39 (Ac-PKKKRKV-miniPEG2-K(cyclo[FfFGRGRQ])-miniPEG2-RF- miniPEG2-Nal-M'-cargo)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-Bip-M'-cargo M35 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-KF-PEG4-Bip- 13, 40 M'-cargo)Ac-KKKRK-PEG2-K(cyc1o[FffGRGRQ])-PEGi2-(2-Nal)-PEG2-(2-Nal)- M'-cargoM36 13, 39 (Ac-KKKRK-miniPEG2-K(cyclo[FfFGRGRQ])-PEGi2-(2-Nal)-miniPEG2-(2-Nal)-M'-cargo)SEQ I D No. Cargo-conjugateNOs:Ac-KKKRK-PEG2-K(cyclo[FfFGRGRQ])-PEGi2-Bip-PEG2-Bip-M'-cargo M37 (Ac-KKKRK-miniPEG2-K(cyclo[FfFGRGRQ])-PEGi2-Bip-miniPEG2-Bip- 20, 39 M'-cargo)'Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEGi2-Nal-PEG2-Nal-M'-cargoM38 20, 40 (Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEGj2-Nal-miniPEG2-Nal-M'-cargo) Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-PEG2-Nal-M'-cargoM39 (Ac-RBRRBR-K(cyclo[FGFGRGRQD-PEG4-Nal-miniPEG2-Nal-M'- 1, 40 cargo)M40 Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-M'-cargo 12, 40 M41 Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-M'-cargo 13, 40 M42 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-M'-cargo 9, 40 M43 Ac-TKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo 8, 40 M44 Ac-KKTRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo 21, 40 Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG4-M'- M45 13, 55 cargoAc-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ])-PEG2-RG-PEG4-M'- M46 13, 55 cargoAc-KKKRK-PEG2-K(cyclo[G-ij(N-me)-FGTGrQ])-PEG2-RF-PEG4-M'- M47 13, 56 cargoM48 Ac-KKKRK-PEG2-K(cyclo[Gf-Nal-GrGrQ])-PEG2-RF-PEG4-M'-cargo 13, 58 M49 Ac-KKKRK-PEG2-K(cyclo[GyYGrGrQ])-PEG2-RF-PEG4-M’-cargo 13, 40 M50 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQj)-PEG4-R-Bip-PEG4-M,-cargo 13, 40 M51 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG2-M'-cargo 13, 40 M52 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-M'-cargo 13, 40 M53 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-PEG4-M'-cargo 13, 39 M54 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFR-PEG4-M'-cargo 13, 40 M55 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-R-PEG4-M'-cargo 13, 40 M56 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-R-PEG4-M'-cargo 13, 40 M57 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Nal-PEG4-M'-cargo 13, 40 M58 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEGs-M'-cargo 13, 40 M59 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-M'-cargo 13, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(3-Pyr)-PEG4-M'- M60 13, 40 cargoAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(2-Pyr)-PEG4-M'- M61 13, 40 cargoAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(4-Pyr)-PEG4-M'- M62 13, 40 cargoAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phe(3-CN)-PEG4-M'- M63 13, 40 cargoAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Trp(5-F)-PEG4-M!- M64 13, 40cargoSEQ I D No. Cargo-conjugateNOs:Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Tyr(Ph)-PEG4-M'- M65 13, 40 cargoAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-HoArg-Bip-PEG4-M'- M66 13, 40 cargoM67 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-rf-PEG4-M'-cargo 13, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R(me)-F(N-me)-PEG4- M68 13, 40 M'-cargoAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-(4-Pyr)-PEG4-Na3-M'- M69 13, 40 cargoM70 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4-F-M'-cargo 13, 40 Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-RF-PEG4- M71 13, 46 M'-cargoAc-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-R-Bip- M72 13, 46 PEG4-M1-cargoM73 Ac-KKKRK-PEG4-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo 13, 40 M74 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG4-M'-cargo 13, 4013, 40, M75 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFRF-PEG4-M’-cargo33 13, 40, M76 Ac-KK KRK-PEG2-K (cy cl ofFGFGR GRQ] )-PEG2-RRF F-P EG4-M'-cargo86 M77 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-M'-cargo 40 M78 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KFKF-PEG4-M'-cargo 40, 32 M79 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-EF-PEG4-M'-cargo 13, 40 M80 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-PEG4-M'-cargo 13, 40 M81 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FGR-PEG4-M'-cargo 13, 40 Ac-KKKRK-PEG2-K(cyclo[Phe(4-CN)-G-Phe(4-CN)-GRGRQ])-PEG2- M82 13, 59 RF -PEGi-M'-cargoM83 Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-K-PEG4-M'-cargo 1, 40 M84 Ac-KKRK-PEG2-K(cyclo[FGFGRrRQ])-PEG2-RF-PEG4-M,-cargo 1, 53 M85 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ]-PEG2-R-F(I)-PEG4-M'-cargo 13, 40 M86 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FR-PEG4-M'-cargo 13, 40 M87 Ac-KKKRKR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-F-PEG4-M'-cargo 17, 40 M88 Ac-KKKRKF-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG4-M'-cargo 16, 40 M89 Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-M’-cargo 13, 57 M90 Ac-KKKRK-PEG2-K(cyclo[FFGRRGQ])-PEG2-RF-PEG4-M’-cargo 13, 49 M91 Ac-KGKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo 3, 40 M92 Ac-KKGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo 4, 40 M93 Ac-KKKGK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo 5, 40 M94 Ac-KKRKG-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo 6, 40 M95 Ac-KKRKK-PEG2-K(cyclo[FGFG-Cit-GRQ])-PEG2-RF-PEG4-M'-cargo 7, 51M96 Ac-KKRKK-PEG2-K(cyclo[FGFGRG-Cit-Q])-PEG2-RF-PEG4-M'-cargo 7, 52SEQ ID No. Cargo-conjugateNOs: M97 Ac-KKRKK-PEG2-K(cyclo[AGFGRGRQ])-PEG2-RF-PEG4-M'-cargo 7, 47 M98 Ac-KKRKK-PEG2-K(cyclo[FGAGRGRQ])-PEG2-RF-PEG4-M’-cargo 7, 50 M99 Ac-KKKGK-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4-M'-cargo 5, 39 M100 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-SF-PEG4-M'-cargo 13, 40 Ml 01 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RL-PEG4-M’-cargo 13, 40 Ml 02 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RY-PEG4-M'-cargo 13, 40 Ml 03 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RW-PEG4-M'-cargo 13, 40 Ml 04 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Cit-F-PEG4-M'-cargo 13, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-Bip-M'- Ml 05 13, 40 cargoM106 Ac-KKKRK-PEG2-K(cyclo[EGFGRGRQ])-R-Bip-PEGs-M'-cargo 13, 40 Ml 07 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG4-M'-cargo 13, 40 Ml 08 Ac-KKKRK-PEG2-K(cycloFFGFGRGRQ])-RF-PEG2-M!-cargo 13, 40 Ml 09 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RPF-PEG4-M'-cargo 13, 40 Ac-KKKRK-PEG2-K(cyclo[FGF-G(N-me)-RGRQ])-PEG2-RPF-PEG4-M'- MHO 13, 60 cargoAc-KKKRK-PEG2-K(cyclo[F-G(N-me)-FGRGRQ])-PEG2-RPF-PEG4-M’- Mill 13, 61 cargoMl 12 Ac-KKKRK-PEG2-K(cyclo[FAFARGRQ])-PEG2-RF-PEG4-M'-cargo 13, 62 Ml 13 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-Bip-PEG4-M'-cargo 13, 40 Ml 14 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-F-PEG4-M-'-cargo 13, 40 Ac-KKKRK-PEG2-K(cyclo[FGFG-Agp-G-Agp-Q])-PEG2-RF-PEG4-M'- Ml 15 13, 63cargoTable I SB.SEQ IDNo. Cargo-conjugateNOs: Ml 16 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQl)-PEG4-RF-PEG4-M'-cargo 13, 40 Ml 17 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG2-M'-cargo 13, 40 Ml 18 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phg-PEG4-M'-cargo 13, 40 Ml 19 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFE-M'-cargo 13, 40 Ml 20 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Hph-PEG4-M'-cargo 13, 40 Ml 21 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Pcpa-F-PEG4-M'-cargo 13, 40 Ml 22 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-M'-cargo 13, 40 M123 Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo 12, 40 Ac-KKKRK-PEG2-K(cyclo[Pcpa-G-Pcpa-GRGRQ])-PEG2-RF-PEG4-M'- M124 13, 64 cargoMl 25 Ac-RFGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4-M'-cargo 22, 40Table 15C.SEQ IDNo. Cargo-conjugateNOs: Ac-K. KK. HH-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M'- M126 15, 40 cargoAc-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])- M127 14, 40PEG2-RF-PEG4-Bip-M'-cargoAc-KBKBKBRBK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- M128 23, 40M'-cargoAc-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-Bip-M'- M129 13, 57 cargoAc-KKKRK-PEG2-K(cyclo[GRFGRFGQ])-PEG2-RF-PEG4-Bip-M'- M130 13, 66 cargoAc-RFKKRFK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M'- M131 24, 40 cargoAc-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'- M132 24, 40 cargoAc-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- M133 21, 40M'-cargoAc-KKKRK-PEG2-K(cyclo[RFGGRFGQ])-PEG2-RF-PEG4-Bip-M'- M134 13, 67 cargoAc-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-PEG2- K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M'-cargoM135 25, 40(Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-miniPEG2- K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-Bip-M'-cargo)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M'- M136 13, 40 cargoAc-(N(Arg))-B-(N(Arg))-(N(Arg))-B-(N(Arg))-K(cyclo[FGFGRGRQ])- M137 26, 40PEG2-RF-PEGi-Bip-M '-cargoAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FRF-PEG4-Bip-M'- M138 13, 40 cargoAc-KK. KRK-PEG2-K(cyclo[GFFGRGRQ])-PEG2-RF-PEG4-Bip-M'- M139 13, 65cargoTable 15D.SEQ IDNo. Cargo-conjugateNOs: Ml 40 Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEG8-RF-PEG4-M'-cargo 40, 18 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG2-F-PEG4-M'- Ml 41 40, 18 cargoAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-PEG4-M'- Ml 42 13, 40cargo

[0058] In embodiments, a compound that includes a delivery construct can be selected from M7, M8, or M9, wherein “PEG2” is -(CH2-CH2-O)2-CH2-CH2-CO.

[0059] In embodiments, a compound that includes a delivery- construct can be Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEGS-M'-cargo (SEQ ID NOS: 18, 38), wherein PEG2is -(CH2-CH2-O)2-CH2-CH2-CO- or (CH2-CH2-O)2-CH2-CO-, and PEGs is (CH2-CH2-O)8-CH2- C(O)- or -(CH2-CH2-O)8-CH2-CH2-CO-.

[0060] FIGS 4D, 5C, 6C, 7C, 8C, 9C, 10C, 11C, I2C. 13C, 14C, 15C, 16C, 17C, 18C, 19C, 20C, 21C, 22C, 23C, 24C, 25C, and 26C show the structures of compounds (cargo-conjugates) 904d, 905c, 906c, 907c, 908c, 909c, 910c, 911c, 912c, 913c, 914c, 915c, 916c, 917c, 918c, 919c, 920c, 921c, 922c, 923c, 924c, 925c, and 926c each compound including a delivery construct.

[0061] Compound (cargo-conjugate) 904d (FIG. 4D) is Ac-RBRRBR-K(cyclo[FGFGRGRQ])- PEG4-Nal-PEG2-Nal-M'-cargo (e.g., see M39 in Table 15A, see also Cll(c) in Table 19D), wherein M' is present (m* is 1) or absent (m* is 0), PEG4 is -(CH2-CH2-O)4-CH2-CH2-CO-, and PEG2is (CH2-CH2-O)-CH2-C(O)-. Compound 904d includes the delivery 904a (FIG. 4D), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 904d can be formed, for example, through reaction of compound 904c (FIG. 4C) with a cargo.

[0062] Compound (cargo-conjugate) 905c (FIG. 5C) is Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEGs-Bip-M'-cargo (e.g,, see M21 in Table 15A, see also A17(c) in Table 17C), wherein M' is present (m* is 1) or absent and PEGs is ~(CH2-CH2-O)8-CH2-CH2-CO-. Compound 905c includes the delivery construct 905a (FIG. 5A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 905c can be formed, for example, through reaction of compound 905b (FIG. 5B) with a cargo.

[0063] Compound (cargo-conjugate) 906c (FIG. 6C) is Ac-KKKRK-PEG2- K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Nal-M'-cargo (e.g., see M32 in Table ISA, see also C2(c) in Table 19A), wherein M' is present (m* is 1) or absent, PEG2 is -(CH2-CFI2-O)2-CH2-CO-, and PEG4 is ~(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 906c includes the delivery construct 906a (FIG. 6A), wherein the delivery7construct is covalently attached to an OH.Compound 906c can be formed, for example, through reaction of compound 906b (FIG. 6B) with a cargo.

[0064] Compound (cargo-conjugate) 907c (FIG. 7C) is Ac-KKKRK-PECh-K(cyclo[FGFGRGRQ])-PEGg-RF-PEG4-Nal -M'-cargo (e.g., see M33 in Table 15A, see alsoC3(c) in Table 19A), wherein M' is present (m* is 1) or absent, PEG?, is ~(CH2-CH?-O)?-CH2-CO-, PEG8 is -(CH2-Ctl2-O)8-CH2-CH2-C(O)-, and PEGt is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 907c includes the delivery construct 907a (FIG. 7A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 907c can be formed, for example, through reaction of compound 907b (FIG. 7B) with a cargo.

[0065] Compound (cargo-conjugate) 908c (FIG. 8C) is Ac-PKKKRKV-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG2-Nal-M'-cargo (e.g., see M34 in Table 15A, see also C6(c) in Table 19C), wherein M’ is present (m* is 1) or absent and PEG2is ~(CH2-CH2-O)2-CH2-CO-. Compound 908c includes the delivery construct 908a (FIG. 8A), wherein the delivery construct is covalently to M'-cargo or cargo. Compound 908c can be formed, for example, through reaction of compound 908b (FIG. 8B) with a cargo.

[0066] Compound (cargo-conjugate) 909c (FIG. 9C) is Ac-PKKKRKV-PEG2- K(cyclo[F GF GRGRQ])-PEG2-RF-PEG4-F -M'-cargo (e.g., see M30 in Table ISA, see also C5(c) in Table 19B), wherein M' is present (m* is 1) or absent, PEG? is (CH2-CH2-O)2-CH2- CO-, and PEG4 is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 909c includes the delivery¬ construct 909a (FIG. 9A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 909c can be formed, for example, through reaction of compound 909b (FIG.9B) with a cargo.

[0067] Compound (car o-conjugate) 910c (FIG. 10C) is Ac-KKKRK-PEG?-K(cyclo[FGFGRGRQ])-PEG4-R-Bta-PEG2-M'-cargo (e.g, see M26 in Table 15A, see also B4(c) in Table 18A), wherein M' is present (m* is 1) or absent, PEG? is (CH2-CH2-O)2-CH2- CO-, and PEG4 is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 910c includes the delivery construct 910a (FIG. 10A), w7herein the delivery construct is covalently attached to M'-cargo or cargo. Compound 910c can be formed, for example, through reaction of compound 910b (FIG, 10B) with a cargo.

[0068] Compound (cargo-conjugate) 911c (FIG. 11C) is Ac-KKKRK-PEGz-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-Bip M'-cargo (e.g., see M29 in Table 15A, see also Cl(c) in Table 19A), wherein M' is present (m* is 1) or absent, PEG? is ~(CH2-CH2-O)?-CH2-CO-, and PEG4 is (CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 911c includes the deliveryconstruct 911a (FIG. 11 A), wherein the delivery construct is covalently attached to M'-cargo orcargo. Compound 911c can be formed, for example, through reaction of compound 911b (FIG.11 B) with a cargo,

[0069] Compound (cargo-conjugate) 912c (FIG. 12C) is Ac-KKKRK-PEC -K(cyclo[FGFGRGRQ])-PEG2-RFRF-PEG4-M'-cargo (e g., see M75 in Table 15A, see also B38(c in Table 18C), wherein M' is present (m* is 1) or absent, PEG2 is (CH2-CH2-O)2-CH2-CO-, and PEG4 is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 912c includes the delivery¬ construct 912a (FIG. 1 A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 912c can be formed, for example, through reaction of compound 912b (FIG.12B) with a cargo.

[0070] Compound (cargo-conjugate) 913c (FIG. 13C) is AC-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFR-PEG4-M'-cargo (e g, see M54 in Table 15A, see also B18(c) in Table 18C), wherein M' is present (m* is 1) or absent, PEG2 is ---(CH2-CH2-O)2-CH2- CO-, and PEG4 is -(CH2-CH2-O) -CH2-CH2-C(O)- Compound 913c includes the delivery construct 913a (FIG. 13A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 913c can be formed, for example, through reaction of compound 913b (FIG, 13B) with a cargo,

[0071] Compound (cargo-conjugate) 914c (FIG. 14C) is AC-KKKRK-PEG2- K(cy clo[F GF GRGRQ])-PEG2-R-Tyr(Ph)-PEG -M '-cargo (e g., see M65 in Table 15A, see also B29(c) in Table 18C), wherein M' is present (m* is 1) or absent, PEG2 is -(CH2-CH2-O) -CH2-CO-, and PEGi is -(CH2-CH2-O)i-CH2-CH2-C(O)- Compound 914c includes the deliveryconstruct 914a (FIG. 14A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 914c can be formed, for example, through reaction of compound 914b (FIG.14B) with a cargo.

[0072] Compound (cargo-conjugate) 915c (FIG. 15C) is AC-KKKRK-PEG2- K(cyclo[FGFGRGRQ])-PEG2-Agp-F-PEG4-PEG4-M'-cargo (e.g., see M114 in Table ISA, see also B74(c) in Table 18C), wherein M' is present (m* is 1) or absent, PEG2 is ~-(CH2-CH2-O)2-CH2-CO-, and PEG4 is ~(CF1 -CH2-O)4-CH2-CH2-C(O)-. Compound 915c includes the delivery' construct 915a (FIG. 15A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 915c can be formed, for example, through reaction of compound 915b (FIG, 15B) with a cargo.

[0073] Compound (cargo-conjugate) 916c (FIG. 16C) is Ac-KKKRK-PEG?-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-PEG4-M'-cargo (e.g., see M77 in Table 15A, see also B41(c) in Table 18C), wherein M' is present (m* is 1) or absent and PEG2 is ~(CH2-CH2-O)2-CH2-CO-. Compound 916c includes the delivery' construct 916a (FIG. 16A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 916c can be formed, for example, through reaction of compound 916b (FIG. 16B) with a cargo.

[0074] Compound (cargo-conjugate) 917c (FIG. 17C) is Ac-KKKRK-PEGz-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG2-PEG4-M'-cargo (e.g., see M51 in Table 15A, see also B16(c) in Table 18C), wherein M' is present (m* is 1) or absent and PEG2 is -(CH2-CH2-O)2- CH2-CO-. Compound 917b includes the delivery construct 917a (FIG. 17 / 1), wherein the delivery construct is covalently attached to an OH. Compound 917c includes the delivery construct 917a (FIG. 17A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 917c can be formed, for example, through reaction of compound 917b (FIG.17B) with a cargo.

[0075] Compound (cargo-conjugate) 918c (FIG. 18C) is Ac-KKKRK-PEG?-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG (e.g., see M116 in Table 15B, see also B76(c) in Table 18D), wherein M' is present (m* is 1) or absent, PEG is -(CH2-CH2-O)?-CH2-CO-, and PEG4 is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 918c includes the delivery construct 918a (FIG.18A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 918c can be formed, for example, through reaction of compound 918b (FIG. 18B) with a cargo

[0076] Compound (cargo-conjugate) 919c (FIG. 19C) is Ac-KKKRKR-PEGz- K(cyclo[FGFGRGRQ])-PEG2-F-PEG4-PEG4-M'-cargo (e.g., see M87 in Table 15A, see also B51(c) in Table 18C), wherein M' is present (m* is 1) or absent, PEG2 is -(CH2-CH2-O)2-CH2-CO-, and PEG4 is -(CH2-CIl2-O)4-CFl -CH2-C(O)-. Compound 919c includes the delivery¬ construct 919a (FIG. 19A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 919c can be formed, for example, through reaction of compound 919b (FIG.19B) with a cargo.

[0077] Compound (cargo-conjugate) 920c (FIG. 20C) is Ac-KKKRK-PEG?-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-PEG4-M'-cargo (e.g., see M89 in Table 15A, see also B53(c) in Table 18C), wherein M' is present (m* is 1) or absent, PEG2 is (CH2-CH2-O)2-CH2- CO-, and PEG4 is -(CH2-CH2-O)4-CH2-CH2-C(O)- Compound 920c includes the deliveryconstruct 920a (FIG. 20A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 920c can be formed, for example, through reaction of compound 920b (FIG.20B) with a cargo.

[0078] Compound (cargo-conjugate) 921c (FIG. 21C) is Ac-KKKRK-PEGz- K(cyclo[FGFGRGRQ])-PEGs-R.-Nal-PEG4-PECi4-M'-cargo (e.g., see M57 in Table ISA, see also B21(c) in Table ISC), wherein M' is present (m* is 1) or absent, PEG2 is -(CFE-CFE-O)?-CH2-CO-, PEG4 is (CH2-CH2-O)4-CH2-CH2-C(O)-, and PEGs is (CH2-CH2-O)s-CH2-CH2- C(O)-. Compound 921c includes the delivery construct 921a (FIG. 21A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 921c can be formed, for example, through reaction of compound 921b (FIG. 2 IB) with a cargo.

[0079] Compound (cargo-conjugate) 922c (FIG. 22C) is Ac-KKKRK-PEG?-K(cyclo[FGFGRGRQ])-PEG2-RPF-PEG4-PEG4-M'-cargo (e.g., see M109 in Table 15A, see also B69(c) in Table 18C), wherein M' is present (m* is 1) or absent, PEG? is -(CH2-CH2-O)2-CH2-CO-, and PEG is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 922c includes the delivery construct 922a (FIG. 22A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 922c can be formed, for example, through reaction of compound 922b (FIG.22B) with a cargo.

[0080] Compound (cargo-conjugate) 923c (FIG. 23C) is Ac-KKKRKF-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG4-PEG4-M'-cargo (e.g., see M88 in Table 15A, see also B52(c) in Table 18C), wherein M' is present (m* is 1) or absent, PEG2 is ~(CH2-C i2-O)2-CH2-CO-, and PEG4 is (CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 923c includes the delivery construct 923a (FIG. 23A), wherein the delivery' construct is covalently attached to M'-cargo or cargo. Compound 923c can be formed, for example, through reaction of compound 923b (FIG.23B) with a cargo.

[0081] Compound (cargo-conjugate) 924c (FIG. 24C) is Ac-KKKRK-PEG?-K(cyclo[FGFGRGRQ])-PEG2-FR-PEG4-PEG4-M'-cargo (e.g., see M86 in Table 15A, see also B50(c) in Table 18C), wherein M' is present (m* is 1) or absent, PEG? is -(CFI2-CH2-O)2-C PECO-, and PEG4is -(CH?-CH2-O)4-CH2-CH2-C(O)-. Compound 924c includes the delivery' construct 924a (FIG. 24A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 924c can be formed, for example, through reaction of compound 924b ( FIG.24B) with a cargo.

[0082] Compound (cargo-conjugate) 925c (FTG. 25C) is Ac-KKKRK-PEG4-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG<i-PEG4-M'-cargo (e g., see M86 in Table 15 A, see also B37(c) in Table 18C), wherein M' is present (m* is 1) or absent, PEG2 is ~(CH2-CH2-O)2-CH?-CO-, and PEG4 is -(CH2-CH2-O)4-CH2-CH2-C(O)-. Compound 925c includes the delivery construct 925a (FIG. 25A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 925c can be formed, for example, through reaction of compound 925b (FIG.25B) with a cargo,

[0083] Compound (cargo-conjugate) 926c (FIG. 26C) is Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-Bip-PEG4-M'-cargo (e g., see M35 in Table 15A, see also C4(c) in Table 12 / ), wherein M' is present (m* is 1) or absent, PEG2 is (CH2-CH2-O)2-CH2-CO-, and PEGi is -(CH2-CIl2-O)4-CIl2-CH2-C(O)-. Compound 926c includes the delivery construct 926a (FIG. 26A), wherein the delivery construct is covalently attached to M'-cargo or cargo. Compound 926c can be formed, for example, through reaction of compound 926b (FIG.26B) with a cargo.

[0084] In embodiments, a compound that includes a delivery construct is selected from compound (cargo-conjugate) 904d, 905c, 906c, 907c, 908c, 909c, 910c, 911c, 912c, 913c, 914c, 915c, 916c, 917c, 918c, 919c, 920c, 921c, 922c, 923c, 924c, 925c, or 926c.

[0085] In embodiments, a compound that includes a delivery construct is compound (cargoconjugate) 904d. In embodiments, a compound that includes a delivery construct is compound (cargo-conjugate) 905c. In embodiments, a compound that includes a delivery construct is compound (cargo-conjugate) 906c. In embodiments, a compound that includes a delivery construct is compound (cargo-conjugate) 907c. In embodiments, a compound that includes a delivery construct is compound (cargo-conjugate) 908c. In embodiments, a compound that includes a delivery construct is compound (cargo-conjugate) 909c. In embodiments, a compound that includes a delivery construct is compound (cargo-conj gate) 910c. In embodiments, a compound that includes a delivery construct is compound (car o-conjug te) 911c. In embodiments, a compound that includes a delivery construct is compound (cargo-conjugate) 912c. In embodiments, a compound that includes a delivery construct is compound (cargoconjugate) 913c. In embodiments, a compound that includes a delivery construct is compound (car o-conjugate) 914c. In embodiments, a compound that includes a delivery construct is compound (cargo-conjugate) 915c. In embodiments, a compound that includes a deliveryconstruct is compound (cargo-conjugate) 916c In embodiments, a compound that includes a delivery construct is compound (cargo-conjugate) 917c. In embodiments, a compound that includes a delivery construct is compound (cargo-conjugate) 918c. In embodiments, a compound that includes a delivery' construct is compound (cargo-conjugate) 919c. In embodiments, a compound that includes a delivery' construct is compound (cargo-conjugate) 920c. In embodiments, a compound that includes a delivery construct is compound (cargo-conjugate) 921c. In embodiments, a compound that includes a delivery construct is compound (cargoconjugate) 922c. In embodiments, a compound that includes a delivery construct is compound (cargo-conjugate) 923c In embodiments, a compound that includes a delivery construct is compound (cargo-conjugate) 924c. In embodiments, a compound that includes a delivery' construct is compound (cargo-conjugate) 925c. In embodiments, a compound that includes a delivery construct is compound (cargo-conjugate) 926c.

[0086] Further examples of compounds (cargo-conjugates) of Formula V include those listed in Table 16A-16C and examples of cargo-conjugates of Formula VI include those listed in Table 16D In Tables 16A-16D, Ac is -C(O)CH3; the cCPP is written as JA(cyclo[XAXRXcXDXRXFXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with the side chain R1, R2, R3, R4, R5, R6, and R7, respectively, YAis the cCPP bridging amino acid residue, and JAis the bridging exocyclic amino acid residue; “miniPEG2” indicates -(CH2-CH2-O)2-CH2-CO-; “PEG#” indicates -(CH2-CH2-O)#-CH2-CO- or ~-(CH2-CH2-O)#-CH2- CH2-CO- where # indicates to the number of -CH2-CH2O- units; and cargo is a PMC) In embodiments of the compounds of Table 16A-16C, each instance of “PEG2” refers to (CH2- CH2-O)2-CH2-CO- (i.e., “miniPEG2”) and each instance of “PEG#” refers to -(CH2-CH2-O)#-CH2-CH2-CO- where # is an integer greater than 2, In embodiments of the compounds of Table 16A-16C, each instance of “PEG2” refers to -(CIl2-CH2-O)2-CIl2-CH2-CO- and each instance of “PEG#” refers to ”(CIl2-CH2-O)f-CH2-CH2-CO- where # is an integer greater than 2.Table 16A.SEQ IDNo. Cargo-conjugateNOs: Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Bip-BRBRB- PMO 18, 40, N1(Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-Bip- 35BRBRB-PMO)SEQ ID No. Cargo-conjugateNOs:Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal-BRBRB- PMO 18, 40, N2(Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal- 36 BRBRB-PMO)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-B-PMON3 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bta-B- 18, 40 PMO)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BRB-Bip-PMO 13, 40, N4(Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEGi2-BRB-Bip-PMO) 29 Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BR-Bip-RB-PMO18, 40, N5 (Ac-PKKKRKV-mmiPEG2-K(cyclo[FGFGRGRQ])-PEGi2-BR-Bjp-RB- 85 PMO)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-B-PMON6 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-B-PMO) Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-RF-PMO N7 (Ac-PKKKRKV-miniPEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-RF- 18, 38 PMO)Ac-KKKRK-PEG2-K(cyclo[GfFGrGrQ])-PEG8-RF-PMON8 13, 44 (Ac-KKKRK-miniPEG2-K(cyclo[GfFGrGrQj)-PEG8-RF-PMO)Ac-kkkRK-PEG2-K(cyclo[GfFGrGrQ])-PEGs-RF-PMON9 11, 44 (Ac-kkkRK-miniPEG2-K(cyclo[GfFGrGrQ])-PEG8-RF-PMO)Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG*-PMON10 18, 38 (Ac-PKKKRKV-miniPEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-PMO) Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG«-K-Bip-PMONil 20, 40 (Ac-RBRRBR-miniPEG2-K(cyclo[FGFGRGRQ])-PEGs-K-Bip-PMO) Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PMON12 12, 40 (Ac-kkkrk-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PMO)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PMON13 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PMO) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-rf-PMON14 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-rf-PMO)N15 Ac-RBKKBR-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-PMO 80, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FK-PMON16 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-FK-PMO) Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-PMON17 13, 40 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-PMO) Ac-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])- PEGs-RF-PMON18 14, 40 (Ac-K(me)-K('me)-K(me)-R(me)-K(me)-miniPEG2-K(cyclo|FGFGRGRQ])-PEG8-RF-PMO)SEQ ID No. Cargo-conjugateNOs: Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Val-Cit-PMON19 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-Val-Cit- 18, 40 PMO)Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PMON20 21, 40 (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQJ)-PEG8-RF-PMO) N21 Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG8-Bip-PMO 20, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-PEG2-PMO N22 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-PEG2- 13, 40 PMO)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG2-PMO N23 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-R-Bta- 13, 40 miniPEG2-PMO)Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-PMON24 20, 40 (Ac-RBRRBR-K(cyclo[FGFGRGRQ])-miniPEG2-KF-PEG4-PMO)Ac-KKKRK-PEG2-K(cyclo[FGFRHRHQ])-PEG2-RF-PEG4-PMON25 (Ac-KKKRK-miniPEG2-K(cyclo[FGFRH]< HQ])-miniPEG2-RF-PEG4- 13, 42 PMO)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bta-PEG2-PMO N26 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ)-PEG4-R-Bta-miniPEG2- 13, 40 PMO)Ac-YArVRRrGPR-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4-PMO N27 (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FfFGRGRQ])-miniPEG2-RF- 21, 39 PEG4-PMO)Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEG8-PMON28 40, 18 (Ac-K(cyclo[FGFGRGRQ])-miniPEG2-PKKKRKV-PEGs-PMO)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-Bip-PMO N29 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-rf-PEG4- 13, 40 Bip-PMO)Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-F-PMO N30 (Ac-PKKKRKV-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 18, 40 PEG4-F-PMO)Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bta-PMO N31 (Ac-RBRRBR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 20, 40 Bta-PMO)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Nal-PMO N32 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 13, 40 Nal-PMO)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RE-PEG4-Nal-PMO N33 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG4-Nal- 13, 40 PMO)Ac-PKKKRKV-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG2-Nal-PMO N34 (Ac-PKKKRKV-miniPEG2-K(cyclo[FfFGRGRQ])-miniPEG2-RF- 18, 39miniPEG2-Nal-PMO)SEQ ID No. Cargo-conjugateNOs: Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-Bip-PMO N35 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-KF-PEG4- 13, 40 Bip-PMO)Ac-KKKRK-PEG2-K(cyclo[FffGRGRQ])-PEGi2-(2-Nal)-PEG2-(2-Nal)- PMON36 13, 39 (Ac-KKKRK-miniPEG2-K(cyclo[FfFGRGRQ])-PEGi2-(2-Nal)- miniPEG2-(2-Nal)-PMO)Ac-KKKRK-PEG2-K(cyclo[FEFGRGRQ])-PEG12-Bip-PEG2-Bip-PMO N37 (Ac-KKKRK-miniPEG2-K(cyclo[FfFGRGRQ])-PEG 12-Bip-miniPEG2- 13, 39 Bip-PMO)Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEG 12-Nal-PEG2-Nal-PMON38 20, 39 (Ac-RBRRBR-K(cyclo[FlFGRGRQ])-PEG12-Nal-miniPEG2-Nal-PMO) Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-PEG2-Nal-PMON39 20, 40 (Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-miniPEG2-Nal-PMO) N40 Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-PMO 1, 40 N41 Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-PMO 12, 40 N42 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PMO 13, 40 N43 Ac-TKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-PMO 9, 40 N44 Ac-KKTRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-PMO 8, 40 N45 Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-PEG4-PMO 21, 40 Ac-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ])-PEG2-RG-PEG4- N46 13, 55 PMOAc-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ])-PEG2-RF-PEG4- N47 13, 55 PMON48 Ac-KKKRK-PEG2-K(cyclo[Gf-Nal-GrGrQ])-PEG2-RF-PEG4-PMO 13, 56 N49 Ac-KKKRK-PEG2-K(cyclo[GyYGrGrQ])-PEG2-RF-PEG4-PMO 13, 58 N50 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-PEG4-PMO 13, 40 N51 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG2-PMO 13, 40 N52 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-PMO 13, 40 N53 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-PEG4-PMO 13, 40 N54 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFR-PEG4-PMO 13, 40 N55 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-R-PEG4-PMO 13, 40 N56 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-R-PEG4-PMO 13, 40 N57 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4-PMO 13, 40 N58 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG8-PMO 13, 40 N59 Ac-KKKRK-PE. G2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-PMO 13, 40 N60 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(3-Pyr)-PEG4-PMO 13, 40 N61 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(2-Pyr)-PEG4-PMO 13, 40N62 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(4-Pyr)-PEG4-PMO 13, 40SEQ ID No. Cargo-conjugateNOs: Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phe(3-CN)-PEG4- N63 13. 40 PMOAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Trp(5-F)-PEG4- N64 13, 40 PMOAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Tyr(Ph)-PEG4- N65 13, 40 PMOAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-HoArg-Bip-PEG4- N66 13, 40 PMON67 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-rf-PEG4-PMO 13, 40 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R(nie)-F(N-me)- N68 13, 40 PEG4-PMOAc-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-(4-Pyr)-PEG4-Nal- N69 13, 40 PMON70 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Nal-PEG4-F-PMO 13, 40 Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-RF- N71 13, 46 PEG4-PMOAc-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-R-Bip- 13, 46 N72PEG4-PMON73 Ac-KKKRK-PEG4-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-PMO 13, 40 N74 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG4-PMO 13, 4013, 40, N75 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFRF-PEG4-PMO33 13, 40, N76 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RRFF-PEG4-PMO86 N77 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-PMO 40 N78 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KFKF-PEG4-PMO 40, 32 N79 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-EF-PEG4-PMO 13, 40 N80 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-PEG4-PMO 13, 40 N81 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FGR-PEG4-PMO 13, 40 Ac-KKKRK-PEG2-K(cyclo[Phe(4-CN)-G-Phe(4-CN)-GRGRQ])-PEG2- N82 13, 59 RF-PEG4-PMON83 Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-K-PEG4-PMO 1, 40 N84 Ac-KKRK-PEG2-K(cyclo[FGFGRrRQ])-PEG2-RF-PEG4-PMO 1, 53 N85 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ]-PEG2-RF(I)-PEG4-PMO 13, 40 N86 Ac-KKKRK.-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FR-PEG4-PMO 13, 40 N87 Ac-KKKRKR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-F-PEG4-PMO 17, 40 N88 Ac-KKKRKF-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG4-PMO 16, 40 N89 Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-PMO 13, 57 N90 Ac-KKKRK-PEG2-K(cyclo[FFGRRGQ])-PEG2-RF-PEG4-PMO 13, 49 N91 Ac-KGKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-PMO 3, 40N92 Ac-KKGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-PMO 4, 40SEQ ID No. Cargo-conjugateNOs: N93 Ac-KKKGK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-PMO 5, 40 N94 Ac-KKRKG-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-PMO 6, 40 N95 Ac-KKRKK-PEG2-K(cyclo[FGFG-Cit-GRQ])-PEG2-RF-PEG4-PMO 7, 51 N96 Ac-KKRKK-PEG2-K(cyclo[FGFGRG-Cit-Q])-PEG2-RF-PEG4-PMO 7, 52 N97 Ac-KKRKK-PEG2-K(cyclo[AGFGRGRQ])-PEG2-RF-PEG4-PMO 7, 47 N98 Ac-KKRKK-PEG2-K(cyclo[FGAGRGRQ])-PEG2-RF-PEG4-PMO 7, 50 N99 Ac-KKKGK-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4-PMO 5, 39 N100 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-SF-PEG4-PMO 13, 40 N101 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RL-PEG4-PMO 13, 40 N102 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RY-PEG4-PMO 13, 40 N103 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RW-PEG4-PMO 13, 40 N104 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Cit-F-PEG4-PMO 13, 40 N105 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-Bip-PMO 13, 40 N106 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-R-Bip-PEG8-PMO 13, 40 N107 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG4-PMO 13, 40 N108 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG2-PMO 13, 40 N109 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RPF-PEG4-PMO 13, 40 Ac-KKKRK-PEG2-K(cyclo[FGF-G(N-me)-RGRQ])-PEG2-RPF-PEG4- N110 13, 60 PMOAc-KKKRK-PEG2-K(cyclo[F-G(N-me)-FGRGRQ])-PEG2-RPF-PEG4- N111 13, 61 PMON112 Ac-KKKRK-PEG2-K(cyclo[FAFARGRQ])-PEG2-RF-PEG4-PMO 13, 62 N113 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-Bip-PEG4-PMO 13, 40 N114 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-F-PEG4-PMO 13, 40 Ac-KKKRK-PEG2-K(cyclo[FGFG-Agp-G-Agp-Qj)-PEG2-RF-PEG4- N115 13, 63PMOTable 16B.SEQ IDNo. Cargo-conjugateNOs: N116 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4-PMO 13, 40 N117 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG2-PMO 13, 40 N118 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phg-PEG4-PMO 13, 40 N119 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFE-PMO 13, 40 N120 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Hph-PEG4-PMO 13, 40Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Pcpa-F-PEG4- N121 13, 40PMON122 Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-PMO 13, 40N123 Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-PMO 12, 40SEQ ID No. Cargo-conjugateNOs: Ac-KKKRK-PEG2-K(cyclo[Pcpa-G-Pcpa-GRGRQ])-PEG2-RF- N124 13, 64PEG4-PMON125 Ac-RFGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4-PMO 22, 40 Table 16C.SEQ IDNo. Cargo-conjugateNOs: Ac-KKKHH-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-F-PEG4-Bip-PMO N126 (Ac-KKKHH-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 15, 40 Bip-PMOAc-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])- PEG2-RF-PEG4-Bip-PMON127 14, 40 (Ac-K(me)-K(me)-K(me)-R(me)-K(me)-miniPEG2- K(cyc!o[FGFGRGRQ])-miniPEG2-RF-PEG4-Bip-PMO)Ac-KBKBKBRBK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- PMON128 23, 40 (Ac-KBKBKBRBK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- PEG4-Bip-PMO)Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-Bip-PMON129 (Ac-KKKRK-miniPEG2-K(cyclo[GFRGFRGQ])-miniPEG2-RF-PEG4- 13, 57 Bip-PMO)Ac-KKKRK-PEG2-K(cyclo[GRFGRFGQ])-PEG2-RF-PEG4-Bip-PMON130 (Ac-KKKRK-miniPEG2-K(cyc]o[GRFGRFGQ])-tniniPEG2-RF-PEG4- 13, 66 Bip-PMO)Ac-RFKKRFK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- PMON131 24, 40 (Ac-RFKKRFK-miniPEG2-K(cvclo[FGFGRGRQ])-miniPEG2-RF- PEG4-Bip-PMO)Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-PMO N132 (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF- 24, 40 PEG4-PMO)Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip- PMON133 21, 40 (Ac-YArVRRrGPR-miniPEG2-K(cyclo[FGFGRGRQ])-niiniPEG2-RF- PEG4-Bip-PMO)Ac-KKKRK-PEG2-K(cycio[RFGGRFGQ])-PEG2-RF-PEG4-Bip-PMON134 (Ac-KKKRK-miniPEG2-K(cyclo[RFGGRFGQ])-miniPEG2-RF-PEG4- 13, 67 Bip-PMO)Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-PEGz- K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-PMON135 25, 40 (Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-miniPEG2- K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4-Bip-PMO)SEQ ID No. Cargo-conjugateNOs: Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-PMON136 ( Ac-KKKRK-mini PEG2-K(cycl o[FGFGRGRQ] )-miniPEG2-RF-PEG4- 13, 40 Bip-PMO)Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-PNAN136.1 (Ac-KKKRK-miniPEG2-K(cyclo[FGFGRGRQ])-miniPEG2-RF-PEG4- 13, 40 Bip-PNA)Ac-(N(Arg))-B-(N(Arg))-(N(Arg))-B-(N(Arg))-K(cyclo[FGFGRGRQ])- PEG2-RF-PEG4-Bip-PMON137 26, 40 ( Ac-( N (Arg))-B -(N(Arg))-(N(...

Claims

1. CLAIMS2.What is claimed is.

1. A compound comprising a deliven' construct of Formula IA;4.R20-~(AA1}~6. 8.or a phar aceutically acceptable salt thereof,9.wherein:10.wl is 0 or 1;11.al is 0 or 1;12.a3 is 1;13.AA1 is an amino acid residue or a peptide comprising 2 to 10 amino acid residues; AA3 is an amino acid residue or a peptide comprising 1 to 6 amino acids residues comprising a hydrophobic amino acid residue, a hydrophilic amino acid residue, or both; j 1 and j2 are each independently an integer from 1 to 4;14.x l and x2 are each independently an integer from 1 to 14;15.n is an integer from 0 to 3;16.y is an integer from 1 to 5; R1, R2, R3, R4, R3, R6, and R7are each independently the side chain an amino acid residue of a cyclic cell penetrating peptide (cCCP) of the formula cyclo[XAXBXtXDXEXI'XGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with side chains R\ R2, R3, R, R3, R6, and R7, respectively, and YAis a cCPP bridging amino acid residue characterized by n;17.provided that:18.(a) AA1 comprises a sequence selected from: K(me)-K(me)-K(me)-R(me)- K(me), RBKKBR, RBRRBR, and YArVRRrGPR;19.(b) the cCPP is cyclo[Bta-G-Bta-GRGRQ] or cyclo[GfFGrGrQ];20.(c) AA3 comprises a sequence selected from: Bip-BRBRB, BRB-Bip, BR-Bip- RB, FK, K-Bip, Nal-BRBRB, R-Bta, R-Bta-B, rf, RFB, RFE, R-Nal, and V- Cit;21.(d) xl is 2 and x2 is 4;22.(e) xl is 0 and x2 is 2, 4, or 8;23.(f) AA1 comprises kkkrk and AA2 comprises R-Bip; or24.(g) AA1 consists of KKRK and AA2 comprises R-Bip.

2. The compound of claim 1, wherein AA1 comprises a sequence selected from: K(me)- K(me)-K(me)-R(me)-K(me), RBKKBR, RBRRBR, and YArVRRrGPR..

3. The compound of claim 1, wherein AAi consists of a sequence selected from: K(me)- K(me)-K(me)-R(me)-K(me), RBKKBR, RBRRBR, and YArVRRrGPR..

4. The compound of any one of claims 1 to 3, wherein the cCPP is cyclo[Bta-G-Bta-GRGRQ] or cyclo[GfFGrGrQ],5. The compound of any one of claims I to 4, wherein / XA3 comprises a sequence selected from: Bip-BRBRB, BRB-Bip, BR-Bip-RB, FK, K-Bip, Nal-BRBRB, R-Bta, R-Bta-B, rf, RFB, RFE, R-Nal, and V-Cit,6. The compound of any one of claims 1 to 4, wherein AA3 consists of a sequence selected from: Bip-BRBRB, BRB-Bip, BR-Bip-RB, FK, K-Bip, Nal-BRBRB, R-Bta, R-Bta-B, rf, RFB, RFE, R-Nal, and V-Cit.

7. The compound of any one of claims 1 to 6, wherein xl is 2 and x2 is 4.

8. The compound of any one of claims 1 to 6, wherein xl is 0 and x2 is 2, 4, or 8.

9. The compound of claim 8, wherein x2 is 2.

10. The compound of claim 8, wdherein x2 is 4.33.11 The compound of claim 8, wdherein x2 is 8.

12. The compound of any one of claims I to 4 or 7 to 10, wherein AA1 comprises kkkrk and AA3 comprises R-Bip.

13. The compound of any one of claims 1 to 4 or 7 to 10, wherein AA1 consists of kkkrk and AA3 comprises R-Bip.

14. The compound of any one of claims 1 to 4 or 7 to 10, wherein AA1 comprises kkkrk and AA3 consists of R-Bip.

15. The compound of any one of claims 1 to 4 or 7 to 10, wherein AA1 consists of KKRK and AA3 comprises R-Bip.38.16 The compound of any one of claims 1 to 4 or 7 to 10, wherein AA1 consists of KKRK and AA3 consists of R-Bip.

17. The compound of any one of claims I to 3, or 5 to 16, wherein the cCPP is cyclofFGF GRGRQ].

18. The compound of any one of claims 1 or 4 to 17, w'herein AA1 comprises KKKRK.

19. The compound of any one of claims 1 or 4 to 17, wherein AA1 consists of KKKRK.

20. The compound of any one of claims 1 to 4 or 7 to 19, wherein AA3 comprises RF.

21. The compound of any one of claims 1 to 4 or 7 to 19, wherein AA3 consists of RF.

22. The compound of any one of claims 1 to 21, wherein xl is 2, 4, 8, or 12.23 The compound of any one of claims 1 to 22, wherein xl is 2.

24. The compound of any one of claims 1 to 22, wherein xl is 4.

25. The compound of any one of claims 1 to 22, wherein xl is 8.

26. The compound of any one of claims 1 to 22, wherein xl is 12.48.27 The compound of any one of claims 1 to 26, wherein x2 is 12.

28. The compound of any one of claims 1 to 27 wherein y is 4.

29. The compound of any one of claims 1 to 28, wherein n is 1.

30. The compound of any one of claims 1 to 29, wherein j 1 is 1.

31. The compound of any one of claims 1 to 30, wherein j 1 is 2.

32. The compound of any one of claims 1 to 31, wherein j 2 is 1,33. The compound of any one of claims 1 to 31, wherein j2 is 2,34. The compound of claim 1 wherein the delivery' construct is selected from:56.Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Bip-BRBRB-; Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal-BRBRB-; Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bta-B-;57.Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi z-BR-Bip-RB-; and Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Val-Cit-, wherein:58.PEG12 is -(CH2-CH2-O)i2-CH2-CO- or -(CH2-CH2-O)i2-CH2-CH2-CO-; PEG8 is -(CH2-CH2-O)s-CH2-CO- or ~-(CH2-CH2-O)8-CH2-CH2-CO-; and PEG2is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-;35. The compound of claim 34, wherein:60.PEG2is (CH2-CH2-O)2-CH2-CO-;61.PEGx is CH2-CH2-O CH2-CH2-CO-; and PEGn is ~-(CH2-CH2-O)I2-CH2-CH2-CO-36. The compound of claim 1 wherein the delivery construct is selected from:63.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-B-;64.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BRB-Bip-;65.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-;66.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-rf-;67.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])- PEG2-FK-;68.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-;69.Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-;70.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-; and71.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-,72.wherein:73.PEG12 is (CH2-CH2-O)i2-CH2-CO- or (CH2-CH2-O)i2-CH2-CH2-CO-; PEG8 is -(CH2-CH2-O)S-CH2-CO- or -(CH2-CH2-O)8-CH2-CH2-CO-; PEG4is -(CH2-CH2-O)4-CH2-CO- or (CH2-CH2-O)4-CH2-CH2-CO-; and PEG2is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-.

37. The compound of claim 37, wherein:75.PEGi2is-(Cl{2-C {2-O)i2-CH2-CH2-CO-;76.PEG8 is -(CH2-CH2-O)8-CH2-CH2-CO-;77.PEG4 is-(CEi2-CH2-O)4-CFI2-CFl2-CO-; and78.PEG2is (CH2-CH2-O)2-CH2-CO-.

38. The compound of claim 1, wherein the delivery construct is selected from:80.Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEGs-K-Bip-;81.Ac-RBKKBR-K(cyclo[FGFGRGRQ])-PEG8-R-Bip-; and82.Ac-RBRRBR-K(cyclo[FGFGRGRQ]> PEGs-Bip-;83.wherein:84.PEG8 is -(CH2-CH2-O)s-CH2-CH2-CO- or -(CH2-CH2-O)s-CH2-CO-; and PEG2is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CI I2-O)2-CH2-CH2-CO-39. The compound of claim 38, wherein:PEGs is ”(CH2-CH2-O)s-CH2-CH2-CO-; and86.PEG2is -(CEI2-CH2-O)2-CH2-CO-.

40. The compound of claim 1, wherein the delivery construct is selected from:88.Ac-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-; and Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-,89.wherein:90.PEG8 is -(CH2-CH2-O)8-CH2-CO- or -(CH2-CH2-O)s-CH2-CH2-CO-, and PEG2is -(CH22-CH2-O)2-CH2-CO- or -(Clfc-CIh-O^-CFh-Cfh-CO-.

41. The compound of claim 40, wherein:92.PEG8 is -(CH2-CH2-O)8-CH2-CH2-CO-; and93.PEGi is -(CH2-CH2-O)2-CH2-CO-.

42. The compound of claim 1, wherein the delivery' construct is selected from:95.Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-RF-,96.wherein:97.PEGs is (CH2-CH2-O)s-CH2-CO- or (CH2-CH2-O)8-CH2-CH2-CO-; and PEG2is -(CH2-CH2-O)2-CH2-CO- or ~-(CH2-CH2-O)2-CH2-CH2-CO-43. The compound of claim 42, wherein:99.PEG8 is -(CH2-CH2-O)8-CE12-CH2-CO-; and100.PEG2is ~-(CH2-CH2-O)2-CH2-CO-44. The compound of claim 1, wherein the delivery construct is selected from:102.Ac-KKKRK-PEG2-K(cyclo[GfFGrGrQ])-PEGs-RF-; and103.Ac-kkkRK-PEG2-K(cyclo[GfFGrGrQ])-PEG8-RF- wherein:104.PEGs is (CH2-CH2-O)8-CH2-CO- or (CH2-CH2-O)8-CH2-CH2-CO-; and PEG2is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-.

45. The compound of claim 44, wherein:106.PEGs is -(CH22-CH2-O)8-CH22-CH2-CO-; and107.PEG2is (CH2-CH2-O)2-CH2-CO-. 46 The compound of claim 1, wherein the delivery construct is selected from:108.Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bip- Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-;109.wherein:110.PEGs is (CH2-CH2-O)s-CH2-CO- or (CH2-CH2-O)s-CH2-CH2-CO-; and111.PEG2is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-47. The compound of claim 46, wherein:113.PEGs is -(CIl2-CH2-O)8-CIl2-CH2-CO-; and114.PEG is (CH2-CH2-O)2-CH2-CO-.

48. The compound of claim 1, wherein the delivery construct is Ac-KKKRK-PEG2- K(cyclo[FGFGRGRQ])-PEG2-RFE-, wherein PEG2is “(CH2-CH2-O)2-CH2-CO- or -(CH2- CH2-O)2-CH2-CH2-CO-.

49. The compound of claim 48, wherein PEG2is (CH2-CH2-O)2-CH2-CO-.50 The compound of any one of claims 1 to 34, wherein the delivery construct is covalently attached to a reactive handle M and the compound is of Formula III(A):117.(M) mt119.

120. wherein ml is 1 and M is a reactive handle.

51. The compound of claim 50, wherein M is OH.122.W123.A 4 ' NH252. The compound of claim 50, wherein M125.

126. is O, wherein y” is an integer from 1 to 4.

53. The compound of any one of claims 50 to 52, wherein the compound is selected from:128.Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Bip-BRBRB-M;129.Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal-BRBRB-M;130.Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGx-R-Bta-B-M;131.Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BR-Bip-RB-M; and132.Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Val-Cit-M, wherein:133.PEG12 is -(CH2-CEh-O)i2-CH2-CO- or -(CH2-CH2-O)i2-CH2-CEb-CO-;134.PEG8 is -(CH2-CH2-O)s-CH2-CO- or ~-(CH2-CH2-O)8-CH2-CH2-CO-; and PEG2 is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-;54. The compound of claim 53, wherein:136.PEG? is (CH2-CH2-O)2-CH2-CO-;137.PEG8 is -(CH2-CH2-O)s-CH2-CH2-CO-;138.PEG12 is -(CEI2-CEl2-O)i2-CH2-CH2-CO-; and139.M is the OH of the carboxylic acid of the C-temiinal amino acid.

55. The compound of any one of claims 50 to 52, wherein the compound is selected from:141.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-B-M;142.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BRB-Bip-M;143.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Nal-M,144.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-rf-M;145.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FK-M;146.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Bta-M;147.Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-M;148.Ac-KK KRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-M, and149.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-M,150.wherein:151.PEG12 is (CH2-CH2-O)i2-CH2-CO- or (CH2-CH2-O)i2-CH2-CH2-CO-;152.PEG8 is -(CH2-CH2-O)8-CH2-CO- or -(CH2-CH2-O)8-CH2-CH2-CO-,153.PEG4is (CH2-CH2-O)4-CH2-CO- or (CH2-CH2-O)4-CH2-CH2-CO-; and PEG? is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-.

56. The compound of claim 55, wherein:155.PEG12 is (CH2-CH2-O)I2-CH2-CH2-CO-;156.PEG8 is -(CH2-CH2-O)8-CH2-CH2-CO-;157.PEG4is -(CH2-CH2-O)4-CH2-CH2-CO-;158.PEG? is (CH2-CH2-O)2-CH2-CO-, and M is the OH of the carboxylic acid of the C-terminal amino acid.

57. The compound of any one of claims 50 to 52, wherein the compound is selected from:160.Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG«-K-Bip-M;161.Ac-RBKKBR-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-M; and162.Ac-RBRRBR-K(cyclo[FGFGRGRQ]> PEG8-Bip-M;163.wherein:164.PEG8 is -(CH2-CH2-O)8-CH2-CO- or -(CH2-CH2-O)s-CH2-CH2-CO-, and165.PEG2is -(CFl2-CH2-O)2-CH2-CO- or -(CFfc-CIh-O^-CFh-Cfh-CO-.

58. The compound of claim 57, wherein:167.PEG8 is -(CH2-CH2-O)s-CH2-CH2-CO-;168.PEG2 is -(CH2-CH2-O)2-CH2-CO-; and169.M is the OH of the carboxylic acid of the C-terminal amino acid.

59. The compound of any one of claims 50 to 52, wherein the compound is selected from:171.Ac-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-M; and Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-M,172.wherein:173.PEG8 is -(CH2-CH2-O)s-CH2-CO- or -(CH2-CH2-O)s-CH2-CH2-CO-; and174.PEG2is ~(CH2-CH2-O)2-CH2-CO- or ~(CH2-CH2-O)2-CH2-CH2-CO-60. The compound of claim 59, wherein:176.PEGs is -(CFI2-CH2-O)8-CH2-CH2-CO-;177.PEGz is (CH2-CH2-O)2-CH2-CO-, and178.M is the OH of the carboxylic acid of the C-terminal amino acid.

61. The compound of any one of claims 50 to 52, wherein the compound is selected from:180.Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-RF-M,181.wherein:182.PEG8 is -(CH2-CH2-O)s-CH2-CO- or -(CH2-CH2-O)s-CH2-CH2-CO-; and183.PEGE is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-62. The compound of claim 61, wherein:PEGs is ~(CH2-CH2-O)S-CH2-CH2-CO-;185.PEG2 is -(CH2-CH2-O)2-CH2-CO-; and186.M is the OH of the carboxylic acid of the C-terminal amino acid.

63. The compound of any one of claims 50 to 52, wherein the compound is selected from:188.Ac-KKKRK-PEG2-K(cyclo[GfFGrGrQ])-PEGs-RF-M; and189.Ac-kkkRK-PEG2-K(cyclo[GfFGrGrQ])-PEGs-RF-M,190.wherein:191.PEGs is -(CIl2-CH2-O)s-CH2-CO- or -(CH2-CH2-O)s-CH2-CH2-CO-; and192.PEG2 is (CH2-CH2-O)2-CH2-CO- or (CH2-CH2-O)2-CH2-CH2-CO-.

64. The compound of claim 63, wherein:194.PEG8 is -(CH2-CH2-O)s-CH2-CH2-CO-;195.PEGs is (CH2-CH2-O)2-CH2-CO-; and196.M is the OH of the carboxylic acid of the C-terminal amino acid.

65. The compound of any one of claims 50 to 52, wherein the compound is selected from:198.Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-M; and199.Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-M;200.wh erein:201.PEGs is ~(CH2-CH2-O)S-CH2-CO- or ~(CH2-CH2-O)s-CH2-CH2-CO-; and202.PEG2is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-.

66. The compound of claim 65, wherein:204.PEGs is (CH2-CH2-O)s-CH2-CH2-CO-;205.PEG2is -(CH2-CH2-O)2-CH2-CO-; and206.M is the OH of the carboxylic acid of the C-terminal amino acid.

67. The compound of any one of claims 50 to 52, wherein the compound is Ac-KKKRK-PEGz- K(cyclo[FGFGRGRQ])-PEG2-RFE-M, wherein PEG? is -(CH2-CH2-O)2-CH2-CO- or - (CH2-CH2-O)2-CH2-CH2-CO-.

68. The compound of claim 67, wherein PEG2is -(CH2-CH2-O)2-CH2-CO- and M is the OH of the carboxylic acid of the C-terminal amino acid.69 The compound of any one of claims 1 to 33, wherein the delivery construct is covalently attached to a cargo or a coupling group (M ') and the compound is of Formula V(A):209.H210.at (M'H cargo212.

213. wherein m* is 0 or 1; and214.O215.M' comprises -NH-,216.

217. , or a heteroaryl wherein t is an integer from 0 to 10.

70. The compound of claim 69, wherein m* is 0.

71. The compound of claim 69, wherein m* is 1.

72. The compound of arty one of claims 69 to 71, wherein the compound is selected from:221.Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Bip-BRBRB-M'-cargo;222.Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-Nal-BRBRB-M'-cargo, Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PECre-R-Bta-B-M '-cargo;223.Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BR-Bip-RB-M'-cargo; and Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Val-Cit-M'-cargo, wherein:224.PEG12 is -(CIl2-CH2-O)i2-CH2-CO- or -(CH2-CH2-O)i2-CFl2-CFl2-CO-; PEGs is ~(CH2-CH2-O)S-CH2-CO- or -(CH2-CH2-O)s-CH2-CH2-CO-;225.PEG2is -(CH2-CH2-O)2-CH2-CO- or -(CM2-CH2-O)2-CFI2-CH2-CO-; and226.M' is present or absent.

73. The compound of claim 72, wherein:228.PEG2is -(CH2-CH2-O)2-CH2-CO-;229.PEGs is (CH2-CH2-O)s-CH2-CH2-CO-;230.PEGn is -(CH2-CH2-O)I2-CH2-CH2-CO-, and231.M' is absent.

74. The compound of any one of claims 69 to 71, wherein the compound is selected from:233.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-B-M'-cargo;234.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGi2-BRB-Bip-M'-cargo;235.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-M'-cargo236.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-rf-M'-cargo;237.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FK-M '-cargo;238.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bta-M'-cargo;239.Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-M'-cargo;240.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-M'-cargo; and241.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-M'-cargo,242.wherein:243.PEGn is -(CH2-CIl2-O)i2-CFI2-CO- or -(CFI2-CH2-O)i2-CH2-CH2-CO-;244.PEGs is (CH2-CH2-O)s-CH2-CO- or (CH2-CH2-O)s-CH2-CH2-CO-;245.PEG4is -(CH2-CH2-O)4-CH2-CO- or -(CH2-CH2-O)4-CH2-CH2-CO-,246.PEG2is (CH2-CH2-O)2-CH2-CO- or (CH2-CH2-O)2-CH2-CH2-CO-; and247.NF is present or absent.

75. The compound of claim 74, wherein:249.PEGn is (CH2-CH2-O)i2-CH2-CH2-CO-;250.PEGs is ~(CH2-CH2-O)s-CH2-CH2-CO-;251.PEG4 i S-(CFI2-CH2-O)4-CH2-CH2-CO-;252.PEG? is (CH2-CH2-O)2-CH2-CO-, and M' is absent.

76. The compound of any one of claims 69 to 71, wherein the compound is selected from:254.Ac-RBRRBR-PEG2-K(cyclo[FGFGRGR. Q])-PEG8-K-Bip-M,-cargo;255.Ac-RBKKBR-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-M'-cargo; and256.Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG8-Bip-M'-cargo;257.wherein:258.PEG8 is -(CH2-CH2-O)s-CH2-CH2-CO-;259.PEG2is -(CH2-CH2-O)2-CH2-CO-, and260.M' is present or absent.

77. The compound of claim 76, wherein:262.PEG8 is -(CH2-CH2-O)S-CH2-CH2-CO-;263.PEG2 is (CH2-CH2-O)2-CH2-CO-; and264.M' is absent.

78. The compound of any one of claims 69 to 71, wherein the compound is selected from:266.Ac-K(me)-K(me)-K(me)-R(me)-K(nie)-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-M'-cargo; and267.Ac-YArVRRiGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-M'-cargo, wherein:268.PEG8 is -(CH2-CH2-O)s-CH22-CO- or -(CH2-CH2-O)8-CFI2-CE12-CO-;269.PEG2is -(CH2-CH2-O)2-CH2-CO- or ~-(CH2-CH2-O)2-CH2-CH2-CO-; and270.\F is present or absent.

79. The compound of claim 78, wherein:272.PEGs is -< CH2-CH2-O)8-CH2-CH2-CO-;273.PEG2is -(CH2-CH2-O)2-CH2-CO-, and274.M' is absent.

80. The compound of any one of claims 69 to 71, wherein the compound is selected from:276.Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEG8-RF-M'-cargo, wherein: PEGs is CH2-CH2-O CH2-CO- or -(CH2-CH2-O)S-CH2-CH2-CO-;277.PEG2 is -(CFI2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CFI2-CH2-CO-; and278.M' is present or absent.

81. The compound of claim 80, wherein:280.PEG8 is -(CH2-CH2-O)8-CH2-CH2-CO-;281.PEG2 is (CH2-CH2-O)2-CH2-CO-; and282.M' is absent.

82. The compound of any one of claims 69 to 71, wherein the compound is selected from:284.Ac-KKKRK-PEG2-K(cyclo[GtFGrGrQ])-PEG8-RF-M'-cargo; and285.Ac-kkkRK-PEG2-K(cyclo[GfFGrGrQ])-PEG8-RF-M'-cargo,286.wherein:287.PEGs is (CH2-CH2-O)s-CH2-CO- or -(CH2-CH2-O)s-CH2-CH2-CO-;288.PEG2is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-; and289.M’ is present or absent.

83. The compound of claim 82, wherein:291.PEG8 is -(CH2-CH2-O)s-CH2-CH2-CO-;292.PEG2 is -(CH2-CH2-O)2-CH2-CO-; and293.M' is absent.

84. The compound of any one of claims 69 to 71, wherein the compound is selected from:295.Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-M'-cargo; and296.Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-M'-cargo;297.wherein:298.PEGs is (CH2-CH2-O)S-CH2-CO- or (CH2-CH2-O)8-CH2-CH2-CO-;299.PEG2 is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-; and300.M' is present or absent.

85. The compound of claim 84, wherein:302.PEG8 is -(CH2-CH2-O)S-CH2-CH2-CO-;303.PEG2is -(CH2-CH2-O)2-CH2-CO-; and M' is absent.

86. The compound of any one of claims 69 to 71, wherein the compound is AC-KKKRK-PEG2- K(cyclo[FGFGRGRQ])-PEG2-RFE-M'-cargo, wherein PEG2 is ~(CH2-CIh-O) -CH2-CO- or (CH2-CH2-O)2-CH2-CH2-CO- and M' is present or absent.

87. The compound of claim 86, wherein PEG2 is (CH2-CH2-O)2-CH2-CO- and M' is absent.

88. A compound comprising a delivery construct of Formula 1(B):

308. 310.or a pharmaceutically acceptable salt thereof;311.wherein:312.O313.R20is H or314.R40is H or CH3;316.

317. wl is 0 or 1;318.al is 0 or 1,319.a3 is 1;320.AA1 is an amino acid residue or a peptide comprising 2 to 10 amino acid residues;321.AA3 is an amino acid residue or a peptide comprising 1 to 6 amino acids residues comprising a hydrophobic amino acid residue, a hydrophilic amino acid residue, or both;322.j 1, j2, and j3 are each independently an integer from 1 to 4;323.l, x2, and x3 are each independently an integer from 1 to 14;324.n is an integer from 0 to 3;325.y is an integer from 1 to 5,326.R1, R2, R3, R4, R R6, and R7are each independently the side chain an amino acid residue of a cyclic cell penetrating peptide (cCCP) of the formula cyclo[XAXBXcXDXtXFXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with side chains R1, R2, R, R4, R’, R6, and R7, respectively, YAis a cCPP bridging amino acid residue characterized by n,327.provided that:328.(a) A A1 comprises a sequence selected from: KGKRK, KKGRK, KKKGK, kkkrk, KKKRKF, KKKRKR, KKRKG, KKRKK, KKRKK, KKTRK, RBRRBR, RFGRK, TKKRK, and YArVRRrGPR;329.(b) the cCCP is cyclofFGFGRrRQ], cyclo[4-Pyr-G-4-Pyr-GRGRQ], cyclo[FAFARGRQ], cyclo[AGFGRGRQ], cyclo[F-G(N-me)-FGRGRQ], cyclo[FGAGRGRQ], cycl o[FGF-G(N -me)-RGRQ], cyclo[FGFG-Agp-G- Agp-Q], cyclo[FGFRHRHQ], cyclo[G-f(N-me)-FGrGrQ], cyclo[Gf-Nal- GrGrQ], cyclo[GFRGFRGQ], cyclo[GyYGrGrQ], cyclo[Pcpa-G-Pcpa- GRGRQ], cyclo[Phe(4-CN)-G-Phe(4-CN)GRGRQ];330.(c) AA3 comprises a sequence selected from: Agp-Bip, Agp-F, Cit-F, EF, FGR, FR, HoAr-Bip, KE, KRKR, Pcpa-F, PKKKRKV, R(me)-F(N-me), R-2-Pyr, R-3-Pyr, R-4-Pyr, R-Bip, R-Bip-R, R-Bta, rf, R-F(I), RFK, RFRF, RGF, R- Hph, RL, R-Nal, R-Nal-R, RPF, R-Phe(3-CN), R-Phg, RRFF, R-Trp(5-F), R- Tyr(Ph), RW, RY, and SF; (d) AA3 consists ofF orR;331.(e) l is 0 or 4;332.(f) x2 is 8;333.(g) xl is 2 and x2 is 2; or334.(h) xl is 2, x2 is 2, and x3 is 2.335.89 The compound of claim 88, wherein AA1 comprises a sequence selected from: KGKRK, KKGRK, KKKGK, kkkrk, KKKRKF, KKKRKR, KKRKG, KKRKK, KKRKK, KKTRK, RBRRBR, RFGRK, TKKRK, and YArVRRrGPR.

90. The compound of claim 88, wherein A Al consists of a sequence selected from: KGKRK, KKGRK, KKKGK, kkkrk, KKKRKF, KKKRKR, KKRKG, KKRKK, KKRKK, KKTRK, RBRRBR, RFGRK, TKKRK, and YArVRRrGPR.

91. The compound of any one of claims 88 to 90, wherein the cCPP is selected from:338.cyclo[FGFGRrRQ], cyclo[4-Pyr-G-4-Pyr-GRGRQ], cyclo[FAFARGRQ], cyclo[AGFGRGRQ], cyclo[F-G(N-me)-FGRGRQ], cyclo[FGAGRGRQ], cyclo[FGF-G(N- me)-RGRQ], cyclo[FGFG-Agp-G-Agp-Q], cyclo[FGFRHRHQ], cyclo[G-f(N-me)- FGrGrQ], cyclo[Gf-Nal-GrGrQ], cyclo[GFRGFRGQ], cyclo[GyYGrGrQ], cyclo[Pcpa-G- Pcpa-GRGRQ], and cyclo[Phe(4-CN)-G-Phe(4-CN)GRGRQ]92. The compound of any one of claims 88 to 91, wherein AA3 comprises a sequence selected from: Agp-Bip, Agp-F, Cit-F, EF, FGR, FR, HoAr-Bip, KE, KRKR, Pcpa-F, PKKKRKV, R(me)-F(N-me), R-2-Pyr, R-3-Pyr, R-4-Pyr, R-Bip, R-Bip-R, R-Bta, rf, R-F(I), RFK, RFRF, RGF, R-Hph, RL, R-Nal, R-Nal-R, RPF, R-Phe(3-CN), R-Phg, RRFF, R-Trp(5-F), R-Tyr(Ph), RW, RY, and SF.

93. The compound of any one of claims 88 to 91, wherein AA3 consists of sequence selected from: Agp-Bip, Agp-F, Cit-F, EF, FGR, FR, HoAr-Bip, KE, KRKR, Pcpa-F, PKKKRKV, R(me)-F(N-me), R-2-Pyr, R-3-Pyr, R-4-Pyr, R-Bip, R-Bip-R, R-Bta, rf, R-F(I), RFK, RFRF, RGF, R-Hph, RL, R-Nal, R-Nal-R, RPF, R-Phe(3-CN), R-Phg, RRFF, R-Trp(5-F), R-Tyr(Ph), RW, RY, or SF.

94. The compound of any one of claims 88 to 91, wherein AA3 consists of F or R95 The compound of any one of claims 88 to 91, wherein xl is 2 and x2 is 2.

96. The compound of any one of claims 88 to 91, wherein xl is 2, x2 is2, and x3 is 2.

97. The compound of any one of claims 88 to 90 or 92 to 95, wherein the cCPP is cyclo[FGFGRGRQ],98. The compound of any one of claims 88 or 91 to 97, wherein AA1 comprises KKKRK.

99. The compound of any one of claims 88 or 91 to 97, wherein AA1 consists of KKKRK.

100. The compound of any one of claims 88 to 91 or 94 to 99, wherein AA3 comprises RF.

101. The compound of any one of claims 88 to 91 or 94 to 99, wherein AA3 consists of RF.

102. The compound of any one of claims 88 to 94 or 97 to 101, wherein xl is 2, 4, 8, or 12.

103. The compound of any one of claims 88 to 94 or 97 to 101, wherein x2 is 2, 4, 8, or 12.

104. The compound of any one of claims 88 to 95 or 97 to 101, wherein x3 is 2, 4, 8, or 12.

105. The compound of any one of claims 88 to 94 or 97 to 103, wherein xl is 2.

106. The compound of any one of claims 88 to 94 or 97 to 103, wherein xl is 4.

107. The compound of any one of claims 88 to 94 or 97 to 103, wherein xl is 8.

108. The compound of any one of claims 88 to 94 or 97 to 103, wherein xl is 12.355.109 The compound of any one of claims 88 to 94 or 97 to 103, wherein x2 is 2.356.110 The compound of any one of claims 88 to 94 or 97 to 103, wherein x2 is 4.357.111 The compound of any one of claims 88 to 94 or 97 to 103, wherein x2 is 8.358.112 The compound of any one of claims 88 to 94 or 97 to 103, wherein x2 is 12.

113. The compound of any one of claims 88 to 95 or 97 to 112, wherein x3 is 2.

114. The compound of any one of claims 88 to 95 or 97 to 112, wherein x3 is 4115. The compound of any one of claims 88 to 95 or 97 to 112, wherein x3 is 8.

116. The compound of any one of claims 88 to 95 or 97 to 112, wherein x3 is 12.

117. The compound of any one of claims 88 to 116, wherein y is 4.

118. The compound of any one of claims 88 to 117, wherein n is 1.

119. The compound of any one of claims 88 to 118, wherein j 1 is 1.

120. The compound of any one of claims 88 to 118, wherein j 1 is 2.366.121 The compound of any one of claims 88 to 120, wherein j2 is 1.367.122 The compound of any one of claims 88 to 120, wherein j2 is 2.368.123 The compound of any one of claims 88 to 122, wherein j3 is 1.369.124 The compound of any one of claims 88 to 122, wherein j3 is 2.

125. The compound of claim 88, wherein the delivery construct is selected from:371.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-PEG2-;372.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG2-;373.Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-; and374.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bta-PEG2-, wherein:375.PEGs is ~(CH2-CH2-O)s-CH2-CO- or ~(CH2-CH2-O)s-CH2-CH2-CO-; PEG4is -(CH2-CH2-O)4-CH2-CO- or -(CH2-CH2-O)4-CH22-CH2-CO-, and PEG2is -(CH2-CH2-O)2-CH2-CO- or ~-(CH2-CH2-O)2-CH2-CH2-CO-.

126. The compound of claim 125, wherein:377.PEG8 is -(CH2-CH2-O)s-CH2-CH2-CO-;378.PEG4 is (CH2-CH2-O)4-CH2-CH2-CO-; and379.PEG2 is ~(CH2-CH2-O)2-CH2-CO-.

127. The compound of claim 88, wherein the delivery construct is selected from: Ac-KKKRK-PEG2-K(cyclo[FGFRHRHQ])-PEG2-RF-PEG4-;380.Ac-YAr\TtRrGPR-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4-; and Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEGs-,381.wherein:382.PEG8 is -(CH2-CH2-O)S-CH2-CO- or -(CH2-CH2-O)8-CH2-CH2-CO-; PEG4 is (CH2-CH2-O)4-CH2-CO- or (CH2-CH2-O)4-CH2-CH2-CO-; and PEG2is -(CH2-CH2-O)2-CH2-CO- or ~-(CH2-CH2-O)2-CH2-CH2-CO-128. The compound of claim 127, wherein:384.PEG8 is -(CH2-CH2-O)8-CH2-CH2-CO-;385.PEG4is-(CH2-CH2-O)4-CH2-CH2-CO-; and386.PEG2is -(CH2-CH2-O)2-CFI2-CO-129. The compound of claim 88, wherein the delivery construct is selected from:388.Ac-TKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-;389.Ac-KKTRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-;390.Ac-YArVRRiGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG -; Ac-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ])-PEG2-RG-PEG4-; Ac-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ])-PEG2-RF-PEG4-; Ac-KKKRK-PEG2-K(cyclo[Gf-Nal-GrGrQ])-PEG2-RF-PEG4-;391.Ac-KKKRK-PEG2-K(cyclo[GyYGrGrQJ)-PEG2-RF-PEG -;392.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-PEG4-;393.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG2-;394.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-PEG4-;395.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFR-PEG4~;396.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-R-PEG -, Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-R-PEG4-;397.Ac-KKKR. K-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4-;398.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEGs-;399.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-;400.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(3-Pyr)-PEG4-; Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(2-Pyr)-PEG4-;401.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(4-Pyr)-PEG4-;402.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phe(3-CN)-PEG4-;403.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Trp(5-F)-PEG4;404.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Tyr(Ph)-PEG4-;405.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-HoArg-Bip-PEG4-;406.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-rf-PEG4-;407.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R(me)-F(N-me)-PEG4-;408.Ac-KKK K-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-(4-Pyr)-PEG4-Nal-;409.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Nal-PEG4-F-;410.Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-RF-PEG -, Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG -R-Bip-PEG4-; Ac-KKKRK-PEG4-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-;411.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG4-;412.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFRF-PEG4-;413.Ac-KK. KRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RRFF-PEG4-;414.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-;415.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KFKF-PEG4-;416.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-EF-PEG4-;417.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-PEG4-;418.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FGR-PEG4-;419.Ac-KKKRK-PEG2-K(cyclo[Phe(4-CN)-G-Phe(4-CN)-GRGRQ])-PEG2-RF-PEG4-; Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-K-PEG4-;420.Ac-KKRK-PEG2-K(cyclo[FGFGRrRQ])-PEG2-RF-PEG4-;421.Ac-KKKR. K-PEG2-K(cyclo[FGFGRGRQ]-PEG2-R-F(I)-PEG4-;422.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FR-PEG4-;423.Ac-KKK. RKR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-F-PEG -;424.Ac-KKKRKF-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG4-;425.Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG -;426.Ac-KKKRK-PEG2-K(cyclo[FFGRRGQ])-PEG2-RF-PEG4-;427.Ac-KGKRK-PEG -K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-; Ac-KKGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-;428.Ac-KKKGK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEs-,429.Ac-KKRKG-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-;430.Ac-KKRKK-PEG -K(cyclo[FGFG-Cit-GRQ])-PE 2-RF-PEG4-;431.Ac-KKRKK-PEG2-K(cyclo[FGFGRG-Cit-Q])-PEG2-RF-PEG4-;432.Ac-KKRKK-PEG2-K(cyclo[AGFGRGRQ])-PEG2-RF-PEG4-;433.Ac-KKRKK-PEG2-K(cyclo[FGAGRGRQ])-PEG2-RF-PEG4-;434.Ac-KKKGK-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4-;435.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-SF-PEG4-;436.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RL-PEG -;437.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQj)-PEG2-RY-PEG4-;438.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RW-PEG4-;439.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Cit-F-PEG4-;440.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RPF-PEG4-;441.Ac-KKKRK-PEG2-K(cyclo[FGF-G(N-me)-RGRQ])-PEG2-RPF-PEG4-; Ac-KK. KRK-PEG2-K(cyclo[F-G(N-me)-FGRGRQ])-PEG2-RPF-PEG4-; Ac-KKKRK-PEG2-K(cyclo[FAFARGRQ])-PEG2-RF-PEG4-;442.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-Bip-PEG4-;443.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-F-PEG4-; and Ac-KKKR. K-PEG2-K(cyclo[FGFG-Agp-G-Agp-Q])-PEG2-RF-PEG4-, wherein:444.PEG8 is -(CH2-CH2-O) -CH2-CO- or -(CH2-CH2-O)8-CH2-CH2-CO-; PEG4 is -(CH2-CH2-O)4-CH2-CO- or (CH2-CH2-O)4-CH2-CH2-CO-; and PEG2is -(CH2-CH2-O)2-CH22-CO- or -(CIl2-CH22-O)2-CH2-CH2-CO-130. The compound of claim 129, wherein:446.PEG8 is -(CH2-CH2-O)S-CH2-CH2-CO-;447.PEG4 is~-(CH2-CH2-O)4-CH2-CH2-CO-; and448.PEG2is -(CH2-CH2-O)2-CH2-CO-.

131. The compound of claim 88, wherein the delivery construct is selected from:450.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4-; Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG2-;451.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phg-PEG4-;452.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Hph-PEG4-;453.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Pcpa-F-PEG -;454.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-;455.Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-,456.Ac-KKKRK-PEG2-K(cyclo[Pcpa-G-Pcpa-GRGRQ])-PEG2-RF-PEG4-; and457.Ac-RFGRK-PEG2-K(cyclo FGFGRGRQ])-PEG4-RF-PEG4-,458.wherein:459.PEGs is (CH2-CH2-O)s-CH2-CO- or -(CH2-CH2-O)s-CH2-CH2-CO-;460.PEG4is -(CH2-CH2-O)4-CH2-CO- or ~(CH2-CH22-O)4-CF12-CH2-CO-, and461.PEG2is (CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-.

132. The compound of claim 131, wherein:463.PEG8 is -(CH2-CH2-O)s-CH2-CH2-CO-;464.PEG4 is (CH2-CH2-O)4-CH2-CH2-CO-; and465.PEGz is ~(CH2-CH2-O)2-CH2-CO-.

133. The compound of claim 88, wherein the delivery construct is Ac-YArVRRrGPR-PEG2- K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-, wherein PEG2is -(Cl I2-CI {2-O)2-CH2-CO- or- (CH2-CH2-O)2-CH2-CH2-CO-.

134. The compound of claim 133, wherein PEG2 is ~(CH2-CH2-O)2-CH2-CO-.

135. The compound of any one of claims 88 to 124, wherein the delivery construct is covalently attached to a reactive handle M and the compound is of Formula III(B):mt470.

471. wherein ml is I and M is a reactive handle.472.136 The compound of claim 135, wherein M is OH.

137. The compound of claim 135, wherein M474.

475. is, wherein y’ ’ is an integer from 1 to 4.

138. The compound of any one of claims 135 to 137, wherein the compound is selected from:477.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQj)-PEG8-R-Bip-PEG2-M;478.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG2-M;479.Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-M; and480.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bta-PEG2-M,481.wherein:482.PEGs is (CH2-CH2-O)s-CH2-CO- or -(CH2-CH2-O)s-CH2-CH2-CO-;483.PEG4is -(CH2-CH2-O)4-CH2-CO- or -(CH2-CH2-O)4-CH2-CH2-CO-;484.PEG2is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-; and M is appended to -CO- of the terminal PEG group139. The compound of claim 138, wherein:486.PEG8 is -(CH2-CH2-O)8-CH2-CH2-CO-;487.PEG4 i s - (CH2-CH2-O)4-C H2-CH2-CO-;488.PEG2 is -(CH2-CH2-O)2-CH2-CO-; and489.M is OH.

140. The compound of any one of claims 135 to 137, wherein the compound is selected from:491.Ac-KKKRK-PEG2-K(cyclo[FGFRHRHQ])-PEG2-RF-PEG₄-M;492.Ac-YArVRRrGPR-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4-M; and493.Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEGs-M,494.wh erein:495.PEGs is (CH2-CH2-O)8-CH2-CO- or (CEh-CH2-O)8-CFfc-CH2-CO<496.PEG4is -(CH2-CH2-O)4-CH2-CO- or -(CH2-CH2-0)4-CH2-CH2-C0-;497.PEG2 is (CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-; and498.M is appended to -CO- of the terminal PEG group.

141. The compound of claim 140, wherein:500.PEG8 is -(CH2-CH2-O)8-CH2-CH2-CO-;501.PEG4 is (CH2-CH2-O)4-CH2-CH2-CO-;502.PEG2 is (CH2-CH2-O)2-CH2-CO-; and503.\! is OH.

142. The compound of any one of claims 135 to 137, wherein the compound is selected from:505.Ac-TKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M;506.Ac-KKTRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M;507.Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-PEG4-M;508.Ac-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ])-PEG2-RG-PEG4-M;509.Ac-KKKRK-PEG2-K(cyclo[G-f(N-me)-FGrGrQ])-PEG2-RF-PEG4-M;510.Ac-KKKRK-PEG2-K(cyclo[Gf-Nal-GrGrQ])-PEG2-RF-PEG4-M;511.Ac-KKKRK-PEG2-K(cyclo[GyYGrGrQJ)-PEG2-RF-PEG4-M; Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-PEG4-M;512.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG2-M;513.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-PEG4-M;514.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFR-PEG4-M;515.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-R-PEG4-M;516.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-R-PEG4-M;517.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Nal-PEG4-M;518.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEGs-M;519.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-M;520.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(3-Pyr)-PEG4-M;521.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQj)-PEG2-R-(2-Pyr)-PEG4-M;522.Ac-KKKRK-PEG2-K(cyclo[FGFGRG Q])-PEG2-R-(4-Pyr)-PEG4-M;523.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phe(3-CN)-PEG4-M;524.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Trp(5-F)-PEG4-M;525.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Tyr(Ph)-PEG4-M;526.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-HoArg-Bip-PEG -M, Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-rf-PEG4-M;527.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R(me)-F(N-me)-PEG4-M; Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-(4-Pyr)-PEG4-Nal-M; Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4-F-M;528.Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-RF-PEG4-M; Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-R-Bip-PEG4-M; Ac-KKKRK-PEG4-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M;529.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG4-M;530.Ac-KKKR. K-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFRF-PEG4-M;531.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RRFF-PEG4-M;532.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG -M,533.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KFKF-PEG4-M;534.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-EF-PEG4-M,535.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-PEG4-M;536.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FGR-PEG4-M; Ac-KKKRK-PEG2-K(cyclo[Phe(4-CN)-G-Phe(4-CN)-GRGRQ])-PEG2-RF-PEG4-M; Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-K-PEG4-M;537.Ac-KKRK-PEG2-K(cyclo[FGFGRrRQ])-PEG2-RF-PEG4-M;538.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ]-PEG2~R-F(I)-PEG4-M;539.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FR-PEG4-M;540.Ac-KKKRKR-PEG2-K(cyclo[FGFGRGRQ])-PEG -F-PEG4-M,541.Ac-KKKRKF-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG4-M;542.Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-M;543.Ac-KKKRK-PEG -K(cyclo[FFGRRGQ])-PEG2-RF-PEG4-M;544.Ac-KGKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M;545.Ac-KKGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M;546.Ac-KKKGK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M;547.Ac-KKRKG-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M;548.Ac-KKRKK-PEG2-K(cyclo[FGFG-Cit-GRQ])-PEG2-RF-PEG4-M;549.Ac-KKRKK-PEG2-K(cyclo[FGFGRG-Cit-Q])-PEG2-RF-PEG4-M;550.Ac-KK. RKK-PEG2-K(cyclo[AGFGRGRQ])-PEG2-RF-PEG4-M;551.Ac-KKRKK-PEG2-K(cyclo[FGAGRGRQl)-PEG2-RF-PEG4-M;552.Ac-KKKGK-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG -M;553.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-SF-PEG4-M,554.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RL-PEG -M;555.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RY-PEG4-M;556.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RW-PEG4-M;557.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Cit-F-PEG4-M;558.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RPF-PEG4-M;559.Ac-KKKRK-PEG2-K(cyclo[FGF-G(N-me)-RGRQ])-PEG2-RPF-PEG4-M;560.Ac-KKKRK-PEG2-K(cyclo[F-G(N-me)-FGRGRQ])-PEG2-RPF-PEG4-M;561.Ac-KKK. RK-PEG2-K(cyclo[FAFARGRQ])-PEG2-RF-PEG4-M;562.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-Bip-PEG4-M;563.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-F-PEG4-M; and564.Ac-KKKRK-PEG2-K(cyclo[FGFG-Agp-G-Agp-Q])-PEG2-RF-PEG4-M,565.wherein: PEGs is CH2-CH2-O CH2-CO- or -(CH2-CH2-O)S-CH2-CH2-CO-;566.PEG4 is -(CIl2-CH2-O)4-CH2-CO- or -(CH2-CH2-0)4-CH2-CH2-C0-;567.PEG2 is -(CH2-CH2-O)2-CH2-CO- or ~-(CH2-CH2-O)2-CH2-CH2-CO-; and568.M is appended to -CO- of the terminal PEG group.

143. The compound of claim 142, wherein:570.PEGs is (CH2-CH2-O)S-CH2-CH2-CO-;571.PEG4 is-(CH2-CH2-O)4-CH2-CH2-CO-,572.PEG2 is -(CH2-CH2-O)2-CH2-CO-; and573.M is OH.

144. The compound of any one of claims 135 to 137, wherein the compound is selected from:575.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RP-PEG -M;576.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG2-M;577.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phg-PEG4-M;578.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Hph-PEG4-M;579.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Pcpa-F-PEG4-M;580.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-M;581.Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M;582.Ac-KKKRK-PEG2-K(cyclo[Pcpa-G-Pcpa-GRGRQ])-PEG2-RF-PEGJ-M; and Ac-RFGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4-M,583.wherein:584.PEGs is (CH2-CH2-O)S-CH2-CO- or (CH2-CH2-O)S-CH2-CH2-CO-;585.PEG4is -(CH2-CH2-O)4-CH2-CO- or -(CH2-CH2-O)4-CH2-CH2-CO-,586.PEG2 is (CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-; and587.M is appended to -CO- of the terminal PEG group.

145. The compound of claim 144, wherein:589.PEGs is ~-(CH2-CH2-O)s-CH2-CH2-CO-;590.PEG4 is-(CH2-CH2-O)4-CH2-CH2-CO-;591.PEG2 is -(CH2-CH2-O)2-CH2-CO-; and592.\l is OH.

146. The compound of any one of claims 135 to 137, wherein compound is Ac-YArVRRrGPR- PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M, wherein PEG2is -(CH2-CH2-O)2-CH2- CO- or -(CH2-CH2-O)2-CH2-CH2-CO- and M is appended to -CO- of the terminal PEG group.

147. The compound of claim 146, wherein PEG? is -(CH?-CH?-O)2-CH?-CO- and M is OH.

148. The compound of any one of claims 88 to 124, wherein the delivery construct is covalently attached to a cargo or a coupling group (M') and the compound is of Formula V(B):

596.

597. wherein m* is 0 or 1; and598.M' comprises -NH-,599.

600. , or a heteroaryl wherein t is an integer from 0 to 10.

149. The compound of claim 148, wherein m* is 0.

150. The compound of claim 148, wherein m* is 1.

151. The compound of any one of claims 148 to 150, wherein the compound is selected from:Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-R-Bip-PEG2-M'-cargo Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG2-M'-cargo;604.Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-M'-cargo; and605.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bta-PEG2-M'-cargo, wherein:606.PEG8 is -(CH2-CH2-O)8-CH2-CO- or -(CH2-CH2-O)s-CH2-CH2-CO-;607.PEG4 is (CH2-CH2-O)4-CH2-CO- or (CH2-CH2-O)4-CH2-CH2-CO-;608.PEG2 is -(CH2-CH2-O)2-CH2-CO- or ~-(CH2-CH2-O)2-CH2-CH2-CO-; and609.M' is present or absent.610.152 The compound of cl im 151, wherein:611.PEG8 is -(CH2-CH2-O CH2-CH2-CO-;612.PEG4 is-(CH22-CFI2-O)4-CH2-CH2-CO-;613.PEG2is (CH2-CH2-O)2-CH2-CO-; and614.M' is absent.

153. The compound of any one of claims 148 to 150, wherein the compound is selected from:616.Ac-KKKRK-PEG2-K(cyclo[FGFRHRFIQ])-PEG2-RF-PEG -M'-cargo;617.Ac-YAr\rRRrGPR-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG4-M'-cargo; and Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEGs-M '-cargo,618.wherein:619.PEG8 is -(CH2-CH2-O)s-CH2-CO- or -(CH2-CH2-O)s-CH2-CI E-CO-;620.PEG4 is (CH2-CH2-O)4-CH2-CO- or ~(CH2-CH2-O)4-CH2-CH2-CO-;621.PEG2is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-; and622.M' is present or absent.

154. The compound of claim 153, wherein:624.PEG8 is -(CH2-CH2-O)s-CH2-CH2-CO-;625.PEGs is (CFl2-CH2-O)4-CH2-CH2-CO-;626.PEGz is -(CH2-CH2-O)2-CH2-CO-; and627.M' is absent.

155. The compound of any one of claims 148 to 150, wherein the compound is selected from:Ac-TKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo;629.Ac-KKTRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M '-cargo;630.Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG4-M'-cargo;631.Ac-KKKRK-PEG2-K(cyclo[G-f(N-M'-cargoe)-FGrGrQ])-PEG2-RG-PEG4-M'-cargo; Ac-KKKRK-PEG2-K(cyclo[G-f(N-M'-cargoe)-FGrGrQ])-PEG2-RF-PEG4-M'-cargo; Ac-KKKRK-PEG2-K(cyclo[Gf-Nal-GrGrQ])-PEG2-RF-PEG4-M'-cargo;632.Ac-KKKRK-PEG2-K(cyclo[GyYGrGrQ])-PEG2-RF-PEG4-M'-cargo,633.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-R-Bip-PEG4-M'-cargo;634.Ac-KKK RK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG2- M'-cargo;635.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-PEG4-M'-cargo;636.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RFR-PEG4-M'-cargo;637.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Nal-R-PEG4-M'-cargo;638.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-R-PEG4-M'-cargo,639.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4-M'-cargo;640.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG«-M'-cargo;641.Ac-KK. KRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG -M'-cargo;642.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(3-Pyr)-PEG4-M'-cargo;643.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(2-Pyr)-PEG4-M'-cargo;644.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-(4-Pyr)-PEG4-M'-cargo;645.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phe(3-CN)-PEG4-M'-cargo;646.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Trp(5-F)-PEG4-M'-cargO;647.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Tyr(Ph)-PEG4-M'-cargo;648.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Ho7 g-Bip-PEG4-M'-cargo;649.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-rf-PEG4-M'-cargo;650.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQj)-PEG4-R(me)-F(N-M'-cargoe)-PEG4-M'-cargo;651.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-(4-Pyr)-PEG4-Nal-M'-cargo; Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-R-Nal-PEG4-F-M'-cargo;652.Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-RF-PEG4-M'-cargo; Ac-KKKRK-PEG2-K(cyclo[(4-Pyr)-G-(4-Pyr)-GRGRQ])-PEG2-R-Bip-PEG4-M'-cargo; Ac-KKKRK-PEG4-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo; Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bta-PEG4-M'-cargo;653.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2- FRF-PEG4-M'-cargo;654.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RRFF-PEG4-M'-cargo;655.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-M'-cargo;656.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KFKF-PEG4-M'-cargo;657.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-EF-PEG4-M'-cargo;658.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Bip-PEG4-M '-cargo;659.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FGR-PEG4-M'-cargo,660.Ac-KKKRK-PEG -K(cyclo[Phe(4-CN)-G-Phe(4-CN)-GRGRQ])-PEG2-RF-PEG4-M'-cargo:661.Ac-KKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-K-PEG4-M'-cargo;662.Ac-KK K-PEG2-K(cycio[FGFGRrRQ])-PEG2-RF-PEG4-M'-cargo;663.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ]-PEG2-R-F(I)-PEG4-M'-cargo;664.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FR-PEG4-M'-cargo;665.Ac-KKKRKR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-F-PEG4-M'-cargo;666.Ac-KK. KRKF-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG4-M'-cargo;667.Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-M'-cargo;668.Ac-KKKRK-PEG2-K(cyclo[FFGRRGQ])-PEG2-RF-PEG4-M'-cargo;669.Ac-KGKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo,670.Ac-KKGR. K-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo;671.Ac-KKKGK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo;672.Ac-KKRKG-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo;673.Ac-KKRKK-PEG2-K(cycio[FGFG-Cit-GRQ])-PEG2-RF-PEG4-M'-cargo;674.Ac-KKRKK-PEG2-K(cyclo[FGFGRG-Cit-Q])-PEG2-RF-PEG4-M'-cargo,675.Ac-KKRKK-PEG2-K(cyclo[AGFGRGRQ])-PEG2-RF-PEG4-M'-cargo;676.Ac-KKRKK-PEG2-K(cyclo[FGAGRGRQl)-PEG2-RF-PEG4-M'-cargo;677.Ac-KKKGK-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG -M'-cargo;678.Ac-KKKRK-PEGz-K(cyclo[FGFGRGRQ])-PEG2-SF-PEG4-M'-cargo;679.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RL-PEG -M'-cargo;680.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RY-PEG4-M'-cargo;681.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RW-PEG4-M'-cargo; Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Cit-F-PEG4-M'-cargo;682.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RPF-PEG4-M'-cargo;683.Ac-KKKRK-PEG2-K(cyclo[FGF-G(N-M'-cargoe)-RGRQ])-PEG2-RPF-PEG4-M'-cargo; Ac-KKKRK-PEG2-K(cyclo[F-G(N-M'-cargoe)-FGRGRQ])-PEG2-RPF-PEG4-M'-cargo; Ac-KKKRK-PEG2-K(cyclo[FAFARGRQ])-PEG2-RF-PEG4-M'-cargo;684.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-Bip-PEG4-M'-cargo;685.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Agp-F-PEG4-M '-cargo; and686.Ac-KKKRK-PEG2-K(cyclo[FGFG-Agp-G-Agp-Q])-PEG2-RF-PEG4-M'-cargo, wherein:687.PEGs is (CH2-CH2-O)s-CH2-CO- or (CH2-CH2-O)s-CH2-CH2-CO-;688.PEG4 is -(CFl2-CH2-O)4-CH2-CO- or -(CH2-CH22-O)4-CEI2-CEi2-CO-,689.PEG2 is (CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-; and690.M ' is present or absent.

156. The compound of claim 155, wherein:692.PEGs is (CH2-CH2-O)s-CH2-CH2-CO-;693.PEG4 is-(CH2-CH2-O)4-CH2-CH2-CO-;694.PEG is -(CH2-CH2-O)2-CH2-CO-; and695.M' is absent.

157. The compound of any one of claims 148 to 150, wherein the compound is selected from:697.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4-M '-cargo;698.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG2-M'-cargo;699.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Phg-PEG4-M'-cargo;700.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-Hph-PEG4-M '-cargo;701.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-Pcpa-F-PEG4-M'-cargo;702.Ac-KKK. RK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-M'-cargo;703.Ac-kkkrk-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo;704.Ac-KKKRK-PEG2-K(cyclo[Pcpa-G-Pcpa-GRGRQ])-PEG2-RF-PEGd-M'-cargo; and Ac-RFGRK-PEG2-K(cyclo[FGFGRGRQ])-PEG4-RF-PEG4-M'-cargo,705.wherein:706.PEGs is (CH2-CH2-O)S-CH2-CO- or (CH2-CH2-O)8-CH2-CH2-CO-; PEG4is ~-(CH2-CH2-O)4-CH2-CO- or -(CH2-CH2-O)4-CH2-CH2-CO-;707.PEG2is -(CH22-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH22-CH2-CO-; and708.M' is present or absent.

158. The compound of claim 157, wherein:710.PEG8 is -(CH2-CH2-O)s-CH2-CH2-CO-;711.PEG4 is (CH2-CH2-O)4-CH2-CH2-CO-;712.PEG2is -(CH2-CH2-O)2-CH2-CO-, and713.M' is absent.

159. The compound of any one of claims 148 to 150, wherein the compound is Ac- YAr\fRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-M'-cargo, wherein PEG2is “(CH22-CI -{2-O)2-CH2-CO- or “(CH2-CH2-O)2-CH2-CH2-CO- and M' is present or absent.

160. The compound of claim 159, wherein PEG2is -(CH2-CH2-O)2-CH2-CO- and M' is absent.

161. A compound comprising a delivery construct of Formula 1(C):717.H718.R28st720.

721. or a pharmaceutically acceptable salt thereof;722.wherein: R723. 724.20isH or V;725.wl is 0 or 1;726.al is 0 or 1;727.a3 is 1;728.a4 is 1;729.AAl is an amino acid residue or a peptide comprising 2 to 10 amino acid residues;730.AA3 and AA4 are each independently an amino acid residue or a peptide comprising 1 to 6 amino acids residues, wherein AA3 comprises a hydrophobic amino acid residue, a hydrophilic amino acid residue, or both;731.j I, j 2, and j3 are each independently an integer from 1 to 4;732.xl, x2, and x3 are each independently an integer from 1 to 14;733.n is an integer from 0 to 3;734.y is an integer from 1 to 5;735.R1, R2, R3, R4, R ’, R6, and R7are each independently the side chain an amino acid residue of a cyclic cell penetrating peptide (cCCP) of the formula cyclo[XAXBXcXDXEXEXGYA]) where XA, XBXc, XDXE, XE, and XGare amino acid residues with side chains R1, R2, R3, R4, R5, R6, and R7, respectively, YAis a cCPP bridging amino acid residue characterized by n;736.provided that:737.(a) AA1 comprises K(me)-K(me)-K(me)-R(me)-K(me), KB KBKBRBK, KKKHH, N(Arg)-B-N(Arg)-N(Arg)-B-N(Arg), N(k)-N(k)-N(k)- N(Arg)-N(k), RBRRBR, RFKKRFK, or YArVRRrGPR;738.(b) the cCCP is cyclofGFFGRGRQ], cyclo[GFRGFRGQ], or cyclofRFGGRFGQ];739.(c) AA3 comprises Bip, FRF, KR, R-(4-Pyr), rf, RGF, or R-Nal;740.(d) xlis 0,741.(e) x2 is 8;742.(f) x2 is 8 and x3 is 4; or743.(g) x2 is 2, x3 is 2, x4 is 4 and AA3 comprises Nal.

162. The compound of claim 161, wherein AA1 comprises a sequence selected from: K(me)- K(me)-K(me)-R( e)-K(me), KBKBKBRBK, KKKHH, N(Arg)-B-N(Arg)-N(Arg)-B- N(Arg), N(k)-N(k)-N(k)-N(Arg)-N(k), RBRRBR, RFKKRFK, or YArVRRrGPR.

163. The compound of claim 161, wherein AA1 consists of AA1 comprises a sequence selected from: K(me)-K(me)-K(me)-R(me)-K(me), KBKBKBRBK, KKKHH, N(Arg)-B-N(Arg)- N(Arg)-B-N(Arg), N(k)-N(k)-N(k)-N(Arg)-N(k), RBRRBR, RFKKRFK, or YArVRRrGPR.

164. The compound of any one of claims 161 to 163, wherein the cCPP is cyclo[GFFGRGRQ], cyclo[GFRGFRGQ], or cyclo[RFGGRFGQj.

165. The compound of any one of claims 161 to 164, wherein AA3 comprises a sequence or residue selected from: Bip, FRF, KR, R-(4-Pyr), rf, RGF, and R-Nal;166. The compound of any one of claims 161 to 164, wherein A A3 consists of a sequence or residue selected from: Bip, FRF, KR, R-(4-Pyr), rf, RGF, and R-Nal;167. The compound of any one of claims 161 to 166, wherein xl is 0.

168. The compound of any one of claims 161 to 167, wherein x2 is 8.

169. The compound of any one of claims 161 to 168, ’herein x2 is 8 and x3 is4.

170. The compound of any one of claims 161 to 164, wherein x2 is 2, x3 is 2, x4 is 4 and AA3 compri ses Nal.752.171 The compound of any one of claims 161 to 164, wherein x2 is 2, x3 is 2, x4 is 4 and AA consist of Nal.

172. The compound of any one of claim 161 to 164 or 165 to 171, wherein the cCPP is cyclofFGFGRGRQ],173. The compound of any one of claims 161 or 164 to 172, wherein AA1 comprises KKKRK.

174. The compound of any one of claims 161 or 164 to 172, wherein AA1 consists of KKKRK.

175. The compound of any one of claims 161 to 164, 167 to 169, or 171 to 174, wherein A A3 comprises RF,176. The compound of any one of claims 161 to 164, 167 to 169, or 171 to 174, wherein AA3 consists of RF.

177. The compound of any one of claims 161 to 176, wherein AA4 comprises Bip.

178. The compound of any one of claims 161 to 176, wherein AA4 consists of Bip.

179. The compound of any one of claims 161 to 177, wherein AA4 comprises Nal.

180. The compound of any one of claims 161 to 177, wherein AA4 consists of Nal.

181. The compound of any one of claims 161 to 166 or 172 to 180, wherein xl is 2, 4, 8, or 12.

182. The compound of any one of claims 161 to 166 or 172 to 181, wherein x2 is 2, 4, 8, or 12.

183. The compound of any one of claims 161 to 166 or 172 to 182, wherein x3 is 2, 4, 8, or 12.

184. The compound of any one of claims 161 to 166 or 172 to 183, wherein xl is 2.

185. The compound of any one of claims 161 to 166 or 172 to 183, wherein xl is 4.

186. The compound of any one of claims 161 to 166 or 172 to 183, wherein xl is 8.

187. The compound of any one of claims 161 to 166 or 172 to 183, wherein xl is 12.

188. The compound of any one of claims 161 to 166 or 172 to 187, wherein x2 is 2.

189. The compound of any one of claims 161 to 166 or 172 to 187, wherein x2 is 4.

190. The compound of any one of claims 161 to 166 or 172 to 187, wherein x2 is 8.

191. The compound of any one of claims 161 to 166 or 172 to 187, wherein x2 is 12.

192. The compound of any one of claims 161 to 166 or 172 to 191, wherein x3 is 2.

193. The compound of any one of claims 161 to 166 or 172 to 191, wherein x3 is 4.

194. The compound of any one of claims 161 to 166 or 172 to 191, wherein x3 is 8.

195. The compound of any one of claims 161 to 166 or 172 to 191, wherein x3 is 12.775.1 6. The compound of any one of claims 161 to 195, wherein y is 4.

197. The compound of any one of claims 161 to 196, wherein n is i.

198. The compound of any one of claims 161 to 197, wherein jl is 1.

199. The compound of any one of claims 161 to 197, wherein j 1 is 2.

200. The compound of any one of claims 161 to 199, wherein j2 is 1.780.201 The compound of any one of claims 161 to 199, whereinj2 is 2.781.202 The compound of any one of claims 161 to 201, wherein j3 is 1.782.203 The compound of any one of claims 161 to 201, wherein j3 is 2.783.204 The compound of claim 161, wherein the delivery construct is selected from:784.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-Bip-;785.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Nal-;786.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGs-RF-PEG4-Nal-; and Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-Bip-, wherein:787.PEG8 is -(CH2-CH2-O)s-CH2-CO- or -(CH2-CH2-O)s-CH2-CH2-CO-;788.PEG4is -(CH2-CH2-O)4-CH2-CO- or -(CH2-CI{2-O)4-CH2-CH2-CO-; and PEG2is (CH2-CH2-O)2-CH2-CO- or (CH2-CH2-O)2-CH2-CH2-CO-.

205. The compound of claim 204, wherein:790.PEG8 is -(CH2-CH2-O)s-CH2-CH2-CO-;791.PEG4is (CH2-CH2-O)4-CH2-CH2-CO-; and792.PEG2is -(CH2-CH2-O)2-CH2-CO-.

206. The compound of claim 161, wherein the delivery construct is selected from:Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-F-;794.Ac-PKKKRKV-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG2-Nal-;795.Ac-KKKRK-PEG2-K(cyclo[FfFGRGRQ])-PEGi2-(2-Nal)-PEG2-(2-Nal)-; Ac-KKKRK-PEG2-K(cyclo[FfFGRGRQ])-PEGi2-Bip-PEG -Bip-; and Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-Bip-, wherein:796.PEG12 is (CH2-CH2-O)I2-CH2-CO- or (CH2-CH2-O)i2-CH2-CH2-CO-; PEG8 is -(CH2-CH2-O)s-CH2-CO- or ~-(CH2-CH2-O)s-CH2-CH2-CO-; PEG4 is -(CIl2-CH2-O)4-CH2-CO- or -(CH2-CH2-O)4-CH2-CI{2-CO-; and PEG? is (CH2-CH2-O)2-CH2-CO- or (CH2-CH2-O)2-CH2-CH2-CO-.797.207 The compound of cl im 206, wherein:798.PEGiz is ~-(CH2-CH2-O)i2-CH2-CH2-CO-;799.PEG8 is -(CH2-CH2-O)8-CH2-CH2-CO-;800.PEG4is (CH2-CH2-O)4-CH2-CH2-CO-; and801.PEG? is -(CH2-CH2-O)2-CH2-CO-208. The compound of claim 161, wherein the delivery constaict is selected from:803.Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bta-;804.Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-PEG2-Nal-, and805.Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEGi2-Nal-PEG2-Nal-, wherein:806.PEG12 is -(CH2-CIl2-O)i2-CH2-CO- or ~(CH2-CH2-O)i2-CH2-CH2-CO-; PEG4is -(CH2-CH2-O)4-CH2-CO- or -(CH2-CH2-O)4-CH2-CH2-CO-; and PEG2is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-209. The compound of claim 208, wherein:808.PEG12 is (CH2-CH2-O)i2-CH2-CH2-CO-,809.PEG4is-(CH2-CH2-O)4-CH2-CH2-CO-; and810.PEG2is -(CH2-CH2-O)2-CH2-CO-.

210. The compound of claim 161, wherein the delivery construct is selected from:811.Ac-KKKHH-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG -Bip-,812.Ac-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclofFGFGRGRQ])-PEG2-RF-PEG4-Bip-;813.Ac-KBKBKBRBK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-,814.Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-Bip-;815.Ac-KKKRK-PEG2-K(cyclo[GRFGRFGQ])-PEG2-RF-PEG4-Bip-;816.Ac-RFKKRFK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-;817.Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-;818.Ac-KKKRK-PEG2-K(cyclo[RFGGRFGQ])-PEG2-RF-PEG4-Bip-;819.Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF- PEG4-Bip-;820.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-;821.Ac-(N(Arg))-B-(N(Arg))-(N(Arg))-B-(N(Arg))-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-;822.Ac-KK. KRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FRF-PEG4-Bip-; and823.Ac-KKKRK-PEG2-K(cyclo[GFFGRGRQ])-PEG2-RF-PEG4-Bip-,824.wherein:825.PEG4is ~(CH2-CH2-O)4-CH2-CO- or -(CH2-CH2-O)4-CH2-CH2-CO-; and826.PEG2is -(CIl2-CH2-O)2-CI{2-CO- or -(CH2-CI{2-O)2-CH2-CH2-CO-.

211. The compound of claim 210, wherein:828.PEG4is~(CI l2-CH2-O)4-CH2-CH2-CO-; and829.PEG2is (CH2-CH2-O)2-CH2-CO-.

212. The compound of any one of claims 161 to 203, wherein the delivery construct is covalently attached to a reactive handle M and the compound is of Formula III(C):R30-- (AA1| a;831.XS $833.

834. wherein m l is 1 and M is a reactive handle213. The compound of claim 212, wherein M is OH.836.214 The compound of claim 212, wherein M837.

838. is O, wherein y” is an integer from 1 to 4.

215. The compound of any one of claims 211 to 213, wherein the compound is selected from:840.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG -rf-PEG4-Bip-M;841.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Nal-M;842.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG8-RF-PEG4-Nal-M; and843.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-Bip-M,844.wherein:845.PEG8 is -(CH2-CH2-O)s-CH2-CO- or -(CH2-CH2-O)s-CH2-CH2-CO-;846.PEG4 is -(CH2-CH2-O)4-CH2-CO- or ~-(CH2-CH2-O)4-CH2-CH2-CO-,847.PEG2is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-; and848.M is present or absent.

216. The compound of claim 215, wherein:849.PEG8 is -(CH2-CH2-O)8-CH2-CH2-CO-;850.PEG4 is~(CH2-CH2-O)4-CH2-CH2-CO-;851.PEG2 is -(CH2-CH2-O)2-CH2-CO-; and852.M is absent.

217. The compound any one of claims 211 to 213, wherein the compound is selected from:854.Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-F-M;855.Ac-PKKKRKV-PEG2-K(cyclo[FfFGRGRQ])-PEG2-RF-PEG2-Nal-M;856.Ac-KKKRK-PEG2-K(cyclo[FfFGRGRQ])-PEGi2-(2-Nal)-PEG2-(2-Nal)-M;857.Ac-KKKRK-PEG2-K(cyclo[FffGRGRQ])-PEGi2-Bip-PEG2-Bip-M; and858.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-Bip-M, wherein:859.PEG12 is (CH2-CH2-O)I2-CH2-CO- or (CH2-CH2-O)i2-CH2-CH2-CO-;860.PEG8 is -(CH2-CH2-O)s-CH2-CO- or -(CH2-CH2-O)s-CH2-CH2-CO-;861.PEG4 is -(CH2-CH2-O)4-CH2-CO- or -(CH2-CH2-O)4-CH2-CH2-CO-;862.PEG2 is ~(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-; and863.M is present or absent.

218. The compound of claim 217, wherein:865.PEG12 is -(CH2-CH2-O)i2-CH2-CH2-CO-;866.PEGs is ~(CH2-CH2-O)s-CFl2-CH2-CO-;867.PEG4 is (CH2-CH2-O)4-CH2-CH2-CO-;868.PEG2 is -(CH2-CH2-O)2-CH2-CO-, and869.M is absent.

219. The compound any one of claims 211 to 213, wherein the compound is selected from:871.Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bta-M;872.Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-PEG2-Nal-M; and873.Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEGi2-Nal-PEG2-Nal-M,874.wherein:875.PEG12 is -(CH2-CH2-O)i2-CH2-CO- or (CH2-CH2-O)i2-CH2-CH2-CO-; PEG4is ~(CH2-CH2-O)4-CH2-CO- or -(CH2-CH2-O)4-CH2-CH2-CO-;876.PEG2 is -(CH2-CH2-O)2-CH2-CO- or -(CM2-CH2-O)2-CFl2-CH2-CO-; and877.M is present or absent.

220. The compound of claim 219, wherein:879.PEG12 is -(CH2-CH2-O)I2-CH2-CH2-CO-;880.PEG4 is (CH2-CH2-O)4-CH2-CH2-CO-;881.PEG2is -(CH2-CH2-O)2-CH2-CO-, and882.M is absent.

221. The compound any one of claims 211 to 213, wherein the compound is selected from.884.Ac-KKKHH-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M;885.Ac-K(me)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M;886.Ac-KBKBKBRBK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M;887.Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG4-Bip-M;888.Ac-KKKRK-PEG2-K(cyclo[GRFGRFGQ])-PEG2-RF-PEG4-Bip-M;889.Ac-RFKKRFK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M;890.Ac-YAr\T RrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M;891.Ac-KKKRK-PEG2-K(cyclo[RFGGRFGQ])-PEG2-RF-PEG4-Bip-M;892.Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEGi-Bip-M;893.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M;894.Ac-(N(Arg))-B-(N(Arg))-(N(Arg))-B-(N(Arg))-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M;895.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FRF-PEG4-Bip-M; and896.Ac-KKKRK-PEG2-K(cyclo[GFFGRGRQ])-PEG2-RF-PEG4-Bip-M,897.wherein:898.PEG4 is ~(CFl2-CH2-O)4-CH2-CO- or (Cl I2-CH2-O)4-CFI2-CH2-CO-;899.PEG2 is -(CH2-CH2-O)2-CH2-CO- or ~-(CH2-CH2-O)2-CH2-CH2-CO-; and900.M is present or absent.

222. The compound of claim 221, wherein:901.PEG4 i S-(CH2-CH2-O)4-C H2-CH2-CO-;902.PEG2 is ~(CH2-CH2-O)2-CH2-CO-; and903.M is absent.

223. The compound of any one of claims 161 to 203, wherein the delivery' construct is covalently attached to a cargo or a coupling group (M') and the compound is of Formula V(C):905.H ■ H i O H... tl at >■ ay w Y g j2 (AA3L aS y p Ha4' ’x? O i / 11 x3 c. i < O{H906.a 0907.a'''y, & H H Z'''»3 RSA908.d \ ®909.

910. R* wherein m* is 0 or 1; and911.M' comprises -NH-,912. 913.l' '* or a heteroaryl wherein t is an integer from 0 to 10.

224. The compound of claim 223, wherein m* is 0.

225. The compound of claim 223, wherein m* is 1.

226. The compound of any one of claims 223 to 225, wherein the compound is selected from:917.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-rf-PEG4-Bip-M'-cargo;918.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Nal-M'-cargo;919.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEGx-RF-PEG4-Nal-M'-cargo; and Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-KF-PEG4-Bip-M'-cargo, wherein:920.PEG8 is -(CH2-CH2-O)8-CH2-CO- or ~-(CH2-CH2-O)s-CH2-CH2-CO-;921.PEGfis -(CH2-CH2-O)4-CH2-CO- or -(CH2-CH2-O)4-CH2-CH2-CO-;922.PEG2is (CH2-CH2-O)2-CH2-CO- or (CH2-CH2-O)2-CH2-CH2-CO-; and M' is present or absent.

227. The compound of claim 226, wherein:924.PEG8 is -(CH2-CH2-O)8-CI{2-CH2-CO-;925.PEG4 is (CH2-CH2-O)4-CH2-CH2-CO-;926.PEG2is -(CH2-CH2-O)2-CE12-CO-; and927.M is absent.

228. The compound any one of claims 223 to 225, wherein the compound is selected from:929.Ac-PKKKRKV-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-F-M'-cargo;930.Ac-PKKKRKV-PEG2-K(cycIo[FffGRGRQ])-PEG2-RF-PEG2-Nal-M'-cargo;931.Ac-KKKRK-PEG2-K(cyclo[FfFGRGRQ])-PEGi2-(2-Nal)- PEG2-(2-Nal)-M '-cargo; Ac-KKKRK-PEG2-K(cyclo[FflFGRGRQ])-PEGi2-Bip-PEG2-Bip-M'-cargo; and Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RGF-PEG4-Bip-M'-cargo, wherein:932.PEG12 is -(CH2-CH2-O)i2-CH2-CO- or -(CH2-CH2-O)I2-CH2-CH2-CO-;933.PEG8 is -(CH2-CH2-O)S-CE12-CO- or -(CH2-CH2-O)8-CH2-CI I2-CO-;934.PEG4 is (CH2-CH2-O)4-CH2-CO- or (CH2-CH2-O) -CH2-CH2-CO-;935.PEG2 is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-; and M' is present or absent.

229. The compound of claim 228, wherein:937.PEG12 is -(CH2-CH2-O)i2-CH2-CH2-CO-;938.PEGs is ~-(CH2-CH2-O)s-CH2-CH2-CO-;939.PEG4 is-(CH2-CH2-O)4-CH2-CH2-CO-;940.PEG2 is -(CH2-CH2-O)2-CH2-CO-; and941.M’ is absent.

230. The compound any one of claims 223 to 225, wherein the compound is selected from: Ac-RBRRBR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bta-M '-cargo;942.Ac-RBRRBR-K(cyclo[FGFGRGRQ])-PEG4-Nal-PEG2-Nal-M'-cargo; and943.Ac-RBRRBR-K(cyclo[FfFGRGRQ])-PEGi2-Nal-PEG2-Nal-M'-cargo,944.wherein:945.PEG12 is -(CH2-CH2-O)I2-CH2-CO- or -(CH2-CH2-O)I2-CH2-CH2-CO-;946.PEG4is (CH2-CH2-O)4-CH2-CO- or (CH2-CH2-O)4-CH2-CH2-CO-;947.PEG2is -(CH2-CH2-O)2-CH2-CO- or ~(CH2-CH2-O)2-CH2-CH2-CO-; and948.M' is present or absent.949.231 The compound of cl im 230, wherein:950.PEG) 2 is --(CH2-CH2-O)i2-CH2-CH2-CO-;951.PEG4 is-(CH22-CH2-O)4-CH2-CH2-CO-;952.PEG2is (CH2-CH2-O)2-CH2-CO-; and953.M' is absent.

232. The compound any one of claims 223 to 225, wherein the compound is selected from:955.Ac-KKKHH-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M'-cargo;956.Ac-K(nie)-K(me)-K(me)-R(me)-K(me)-PEG2-K(cyclo[FGFGRGRQp-PEG2-RF-PEG4- Bip-M'-cargo;957.Ac-KBKBKBRBK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M'-cargo;958.Ac-KKKRK-PEG2-K(cyclo[GFRGFRGQ])-PEG2-RF-PEG -Bip-M'-cargo;959.Ac-KKKRK-PEG2-K(cyclo[GRFGRFGQ])-PEG2-RF-PEG4-Bip-M'-cargo;960.Ac-RFKKRFK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M'-cargo;961.Ac-YArVRRrGPR-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M'-cargo;962.Ac-KKKRK-PEG2-K(cyclo[RFGGRFGQ])-PEG2-RF-PEG4-Bip-M'-cargo;963.Ac-(N(k))-(N(k))-(N(k))-(N(Arg))-(N(k))-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF- PEG4-Bip- M'-cargo;964.Ac-KKKR. K-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-M'-cargo;965.Ac-(N(Arg))-B-(N(Arg))-(N(Arg))-B-(N(Arg))-K(cyclo[FGFGRGRQ])-PE 2-RF-PEG4-Bip-M'-cargo;966.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-FRF-PEG4-Bip-M'-cargo; and Ac-KKKRK-PEG2-K(cyclo[GFFGRGRQ])-PEG2-RF-PEG4-Bip-M'-cargo, wherein:967.PEG4is -(CH2-CH2-O)4-CH2-CO- or ~-(CH2-CH2-O)4-CH2-CH2-CO-;968.PEG2is -(CH2-CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-; and M' is present or absent.

233. The compound of claim 232, wherein:970.PEG4 is-(CH2-CH2-O)4-CH2-CH2-CO-,971.PEG2is -(CH2-CH2-O)2-CH2-CO-; and972.M' is absent.

234. A compound comprising a delivery construct of Formula 1(E):

975. 977.or a pharmaceutically acceptable salt thereof;978.wdierein: O979.JM980.R20isH or ''981.wl is 0 or 1;982.al is 0 or 1;983.a2 is 1;984.AA1 is an amino acid residue or a peptide comprising 2 to 10 amino acid residues;985.A 2 is amino acid residue or a peptide comprising 1 to 6 amino acids residues, wherein AA2 comprises a hydrophobic amino acid residue, a hydrophilic amino acid residue, or both,986.j 1 and j2 are each independently an integer from 1 to 4;987.xl and x2 are each independently an integer from 1 to 14;988.n is an integer from 0 to 3;989.y is an integer from 1 to 5;990.R1, R2, R3, R4, R5, R”, and Rzare each independently the side chain an amino acid residue of a cyclic cell penetrating peptide (cCCP) of the formula cyclo[XAXnXcXDXEXrXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with side chains R1, R2, R3, R4, R5, R6, and R7, respectively, YAis a cCPP bridging amino acid residue characterized by n;991.provided that:992.(a) x2 is 2 or 8;993.(b) AA2 comprises R-Bip; or994.(c) AA1 comprises KKKRK, cCPP is cyclofFGFGRGRQ], AA2 comprises RF, and x2 is 4.

235. The compound of claim 234, wherein x2 is 2 or 8.

236. The compound of claim 234, wherein x2 is 2.

237. The compound of claim 234, wherein x2 is 8.

238. The compound of any one of claims 234 to 237, wherein AA2 comprises R-Bip.

239. The compound of any one of claims 234 to 237, wherein AA2 consists of R-Bip.

240. The compound of any one of claims 234 to 237, wherein AA2 comprises RF241. The compound of any one of claims 234 to 237, wherein AA2 consists of RF.

242. The compound of any one of claims 234 to 241, wherein AA1 comprises KKKRK.

243. The compound of any one of claims 235 to 241, wherein AA1 consists of KKKRK.

244. The compound of any one of claims 234 or 238 to 243, wherein x2, is 4.

245. The compound of any one of claims 234 to 244, wherein xl is 2.

246. The compound of any one of claims 234 to 244, wherein xl is 4.1006.247 The compound of any one of claims 234 to 244, wherein xl is 8.1007.248 The compound of any one of claims 234 to 244, wherein xl is 12.1008.249 The compound of any one of claims 234 to 248, wherein n is 1.1009.250 The compound of any one of claims 234 to 248, wherein y is 4.

251. The compound of any one of claims 234 to 250, wherein j 1 is 1.

252. The compound of any one of claims 234 to 250, wherein j 1 is 2.

253. The compound of any one of claims 234 to 251, wherein j2 is 1.

254. The compound of any one of claims 234 to 251, wherein j2 is 2.

255. The compound of claim 234 wherein the deliver}' construct is selected from Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-R-Bip-PEGs-;1015.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG4-; and1016.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQj)-RF-PEG2-,1017.wherein:1018.PEG8 is -(CH2-CH2-O)8-CH2-CH -CO-;1019.PEG4 is (CH2-CH2-O)4-CH2-CH2-CO-; and PEGz is ~(CH2-CH2-O)2-CH2-CO-256. The compound of claim 255, wherein:1021.PEGs is -(CFl2-CH2-O)s-CH2-CH2-CO-;1022.PEG4 is (CH2-CH2-O)4-CH2-CH2-CO-; and1023.PEGc is -(CH2-CH2-O)2-CH2-CO-257. The compound of any one of claims 234 to 254, wherein the delivery' construct is covalently attached to a reactive handle M and the compound is of Formula 111(E):1026. 1027. wherein ml is 1 and M is a reactive handle.

258. The compound of claim 257, wherein M is OH.1029.W'1030.H259. The compound of claim 257, wherein1032. 1033. \l is 0, wherein y” is an integer from 1 to 4.

260. The compound of any one of claims 257 to 259, wherein the compound is selected from Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-R-Bip-PEG8-M;1034.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG4-M; and1035.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG2-M,1036.wherein:1037.PEG8 is -(CH2-CH2-O)8-CH2-CH2-CO-;1038.PEG4 i s - (CH2-CH2-O)4-C H2-CH2-CO-;1039.PEG2is -(CH2-CH2-O)2-CH2-CO-, and1040.M is present or absent.1041.261 The compound of claim 260, wherein:1042.PEG8 is -(CH2-CH2-O CH2-CH2-CO-;1043.PEG4 is-(CIl2-CH2-O)4-CH2-CH2-CO-;1044.PEG2is (CH2-CH2-O)2-CH2-CO-; and1045.M is OH.

262. The compound of any one of claims 234 to 254, wherein the delivery' construct is covalently attached to a cargo or a coupling group (M') and the compound is of Formula V(E):1047. 1048. wherein in* is 0 or 1, and1049.M' comprises -NH-,1050. 1051. or a heteroaryl wherein t is an integer from 0 to 10.

263. The compound of claim 262, wherein m* is 0.

264. The compound of claim 262, wherein m* is 1.

265. The compound of any one of claims 261 to 264, wherein the compound is selected from Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-R-Bip-PEGs-M ’-cargo;1055.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG4-M'-cargo; and1056.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-RF-PEG2-M'-cargo,1057.wherein:1058.PEG8 is -(CH2-CH2-O)S-CH2-CH2-CO-;1059.PEG4 i S-(CH2-CH2-O)4-C H2-CH2-CO-;1060.PEG2is ~(CH2-CH2-O)2-CH2-CO-; and M' is present or absent.

266. The compound of claim 265, wherein:1062.PEGs is -(CFl2-CH2-O)s-CI{2-CH2-CO-;1063.PEG4 i s - (CH2-CH2-O)4-C H2-CH2-CO-;1064.PEG2 is -(CH2-CH2-O)2-CH2-CO-; and1065.M' is absent.

267. A compound comprising a delivery construct of Formula 11(F):1067.(AA3)1068.X3 Q O1070. 1071. or a pharmaceutically acceptable salt thereof;1072.wherein:1073.o1074.R1075. 1076.20isH or1077.R40is H or Clb;1078.wl is 0 or 1;1079.al is 0 or 1,1080.AA1 is an amino acid residue or a peptide comprising 2 to 10 amino acid residues;1081.AA3 and AA4 are each independently an amino acid residue or a peptide comprising 1 to 6 amino acids residues, wherein AA3 comprises a hydrophobic amino acid residue, a hydrophilic amino acid residue, or both; j 1, j2, j 3, and j4 are each independently an integer from 1 to 4;1082.xl, x2, x3, and x4 are each independently an integer from 1 to 14; n is an integer from 0 to 3;1083.y is an integer from 1 to 5; and1084.Rl, R2, R3, R4, R5, R6, and R7are each independently the side chain an amino acid residue of a cyclic cell penetrating peptide (cCCP) of the formula cyclo[XAXBXcXDXEXFXGYA]) where XA, XB, Xc, XD, XE, XF, and XGare amino acid residues with side chains R1, R2, R3, R4, R5, R6, and R7, respectively, YAis a cCPP bridging amino acid residue characterized by n1085.268 The compound of claim 267, wherein wl is 0.1086.269 The compound of claim 267 or 268, wherein AA1 comprises K. KKRK.

270. The compound of claim 267 or 268, wherein AA1 consists of KKKRK.

271. The compound of any one of claims 267 to 270, wherein AA3 comprises PKKKRKV, R, orRF.

272. The compound of any one of claims 267 to 270, wherein AA3 consists of PKKKRKV, R, or RF.

273. The compound of any one of claims 267 to 272, wherein AA4 comprises RF, F, or Bip.

274. The compound of any one of claims 267 to 272, wherein AA4 consists of RF, F, or Bip.

275. The compound of any one of claims 267 to 274 wherein:1093.R" and R7are the side chain of arginine;1094.R4and R6are H or an amino acid side chain; and1095.two of R1, R2, and R3, are, independently the side chain of phenylalanine and one of R1, R2, and R3i s H, or1096.or R1, R2, and R3are the side chain of phenylalanine.

276. The compound of any one of claims 267 to 275, wherein the cCPP is cyclofFGFGRGRQ],277. The compound of any one of claims 267 to 276, wherein xl, is 2, 4, 8, or 12 278. The compound of any one of claims 267 to 277, wherein xl, is 2.

279. The compound of any one of claims 267 to 277, wherein xl, is 4.

280. The compound of any one of claims 267 to 277, wherein xl, is 8.

281. The compound of any one of claims 267 to 277, wherein xl, is 12.

282. The compound of any one of claims 267 to 281, wherein x2, is 2, 4, 8, or 12.

283. The compound of any one of claims 267 to 281, wherein x2, is 2.1103.284 The compound of any one of claims 267 to 281, wherein x2, is 4.1104.285 The compound of any one of claims 267 to 281, wherein x2, is 8.1105.286 The compound of any one of claims 267 to 281, wherein x2, is 12.1106.287 The compound of any one of claims 267 to 286, wherein x3, is 2, 4, 8, or 12.

288. The compound of any one of claims 267 to 287, wherein x3, is 2.

289. The compound of any one of claims 267 to 287, wherein x3, is 4.

290. The compound of any one of claims 267 to 287, wherein x3, is 8.

291. The compound of any one of claims 267 to 287, wherein x3, is 12.

292. The compound of any one of claims 267 to 2 1, wherein n is 1.

293. The compound of any one of claims 267 to 292, wherein y is 4.

294. The compound of any one of claims 267 to 293, wherein jl is 1.

295. The compound of any one of claims 267 to 293, wherein jl is 1.

296. The compound of any one of claims 267 to 295, wherein j 2 is 1.

297. The compound of any one of claims 267 to 295, wherein j2 is 2298. The compound of any one of claims 267 to 297, wherein j3 is 1.

299. The compound of any one of claims 267 to 297, wherein j 3 is 2.

300. The compound of cl im 267, wherein the delivery construct is selected from:1119.Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEGs-RF-PEG4-;1120.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG2-F-PEG4-; and1121.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-PEG4-,1122.wherein:1123.PEGs is ~-(CH2-CH2-O)S-CH2-CH2-CO-;1124.PEG4is~(CI I2-CH2-O)4-CE12-CH2-CO-; and1125.PEG2is -(CH2-CH2-O)2-CH2-CO-301. The compound of claim 300, wherein:1127.PEG8 is -(CH2-CH2-O)8-CH2-CH2-CO-;1128.PEG4 is (CH2-CH2-O)4-CH2-CH2-CO-; and1129.PEG2is -(CH2-CH2-O)2-CH2-CO-.

302. The compound of any one of claims 267 to 299, wherein the delivery construct is1131.covalently attached to a reactive handle M and the compound is of Formula V1(F):1132.RH / 28 < AA4k-N- / (Mi M O1134. 1135. wherein l is 1 and M is a reactive handle303. The compound of claim 302, wherein M is OH.1137.X'1138.W*1139.LA,^H21140.< W n1141.H H304. The compound of claim 302, wherein M is1143. 1144. O, wherein y” is an integer from 1 to 4.

305. The compound of any one of claims 302 to 304, wherein the compound is selected from:1146.Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEGs-RF-PEG4-M;1147.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG2-F-PEGi-M; and1148.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG -RF-PEG4-Bip-PEG4-M, wherein:1149.PEG8 is -(CH2-CH2-O)s-CH2-CH2-CO-;1150.PEG4 is-(CH2-CH2-O)4-CH2-CH2-CO-;1151.PEG2is (CH2-CH2-O)2-CH2-CO-; and1152.M is present or absent.

306. The compound of claim 305, wherein:1154.PEG8 is -(CH2-CH2-O)S-CH2-CH2-CO-;1155.PEG4 is~-(CH2-CH2-O)4-CH2-CH2-CO-;1156.PEG8 is -(CH2-CH2-O)2-CH2-CO-; and1157.M is absent.

307. The compound of any one of claims 267 to 299, wherein the delivery construct is covalently attached to a cargo or a coupling group (M') and the compound is of Formula VI(F):H i Q, O j j H / \ Rz(l. (AAt)--N a1 ' 'xio i AH* 'xio ' '<* o - =w1 VNH O.-^! / ;n ( o O; A &R7 / --N HN--<^Oo. ' / , NHRii 40 y to2RR\H HHZ"'° °\-NH H...,l' R’R< Tr. a1159. 1160. O wherein m* is 0 or 1; and1161.\F comprises -NH-,1162. 1163. or a heteroaryl wherein t is an integer from 0 to 10.

308. The compound of claim 307, wherein m* is 0.

309. The compound of claim 307, wherein m* is 1.

10. The compound of any one of claims 307 to 309, wherein the compound is selected from:1167.Ac-K(cyclo[FGFGRGRQ])-PEG2-PKKKRKV-PEGs-RF-PEG4-M'-cargo;1168.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-R-PEG2-F-PEG4-M '-cargo; and1169.Ac-KKKRK-PEG2-K(cyclo[FGFGRGRQ])-PEG2-RF-PEG4-Bip-PEG4-M'-cargo,1170.wherein:1171.PEGs is (CH2-CH -O)8-CH2-CH2-CO-;1172.PEG is (CH2-CH2-O)4-CH2-CH -CO-;1173.PEGs is (CH2-CH2-O)2-CH2-CO-; and1174.M' is present or absent.

311. The compound of claim 310, wherein:1176.PEGs is -(CFI2-CH2-O)S-CI{2-CH2-CO-;1177.PEG4i s (CH2-CH2-O)4-CH2-CH2-CO-;1178.PEG2is -(CH2-CH2-O)2-CH2-CO-; and M' is absent.

312. A compound comprising a delivery construct Ac-PKKKRKV-PEG2-k(cyclo[Bta-G-Bta- GRGRQ])-PEG8- (SEQ ID NOS: 18, 38), wherein PEG2is -(CH2-CH2-O)2-CH2-CO- or - (CH2-CH2-O)2-CH2-CH2-CO-, and PEGS is (CH2-CH2-O)8-CH2-CO- or (CH2-CH2-O)8- CH2-CH2-CO-.

313. A compound comprising the delivery construct of claim 312, wherein the delivery construct is covalently attached to a reactive handle M and is Ac-PKKKRKV-PEG?- k(cyclo[Bta-G-Bta-GRGRQ])-PEGs-M (SEQ ID NOS: 18, 38), wherein PEG2is (CH2- CH2-O)2-CH2-CO- or -(CH2-CH2-O)2-CH2-CH2-CO-, and PEG8 is -(CH2-CH2-O)8-CH2- CO- or -(CH2-CH2-O)s-CH2-CH2-CO-, and wherein M is OH.

314. A compound comprising the delivery construct of claim 312, wherein the delivery construct is covalently attached to a cargo or a coupling group (M') and is Ac-PKKKRKV- PEG2-k(cyclo[Bta-G-Bta-GRGRQ])-PEGs-M'-cargo (SEQ ID NOS: 18, 38), wherein PEG2is -(CH2-CH2-O 2-CH2-CO- or-(CH2-CH2-O)2-CH2-CH2-CO-, and PEG8 is -(CH2-CH2- O)s-CH2-CO- or --(CH2-CH2-O)g-CH2-CH2-CO-, and wherein M' is present or absent.

15. The compound of claim 314, where M' is absent.

316. The compound of any of compounds 312 to 314, wherein PEG2 is ”(CH2-CH2-O)2-CH2- CO- and PEGs is-(CH2-CH2-O)g-CH2-CH2-CO.

317. The compound of any one of claims 69 to 87, 148 to 160, 223 to 233, 262 to 266, 307 to 311, or 315 to 315, wherein the cargo comprises a therapeutic moiety.

318. The compound of any one of claims 69 to 87, 148 to 160, 223 to 233, 262 to 266, 307 to 311, or 315 to 317, wherein the cargo comprises a polypeptide, a small molecule, an oligonucleotide, one or more components of gene editing machinery, or any combination thereof319. The compound of any one of claims 69 to 87, 148 to 160, 223 to 233, 262 to 266, 307 to 311, or 315 to 318, wherein the cargo comprises a polypeptide.

320. The compound of any one of claims 69 to 87, 148 to 160, 223 to 233, 262 to 266, 307 to 311, or 315 to 319, wherein the cargo comprises an antibody.

321. The compound of any one of claims 69 to 87, 148 to 160, 223 to 233, 262 to 266, 307 to 311, or 315 to 318, wherein the cargo comprises a small molecule.

322. The compound of any one of claims 69 to 87, 148 to 160, 223 to 233, 262 to 266, 307 to 311, or 315 to 318, wherein the cargo comprises one or more components of gene editing machinery7.1189.323 The compound of any one of claims 69 to 87, 148 to 160, 223 to 233, 262 to 266, 307 to 311, or 31 to 318, wherein the cargo comprises an oligonucleotide.

324. The compound of any one of claims 69 to 87, 148 to 160, 223 to 233, 262 to 266, 307 to 311, 315 to 318, or 323 wherein the cargo comprises an antisense oligonucleotide (ASO).

325. The compound of any one of claims 69 to 87, 148 to 160, 223 to 233, 262 to 266, 307 to 311, 315 to 318, or 323 to 324, wherein m* is 0 (M' is absent) absent and the cargo comprises an antisense oligonucleotide (ASO).

326. The compound of claim 325, wherein the ASO has a length of 15 to 30 nucleotides.

327. The compound of claim 325, wherein the ASO has a length of 20 to 30 nucleotides.

328. The compound of claim 325, wherein the ASO has a length of 20 to 25 nucleotides.

329. The compound of any one of claims 324 to 328, wherein the ASO is conjugated at its 3’ end1196.330 The compound of any one of claims 324 to 328, wherein the ASO is conjugated at its 5’ end.

331. The compound of any of one claims 324 to 328, wherein the ASO is a PMO332. The compound of claim 331, wherein m* is 0 and the PMO is conjugated at its 3’ end.

333. The compound of claim 331, wherein m* is 0 cargo is a PMO and the PMO is conjugated at its 3’ end.

334. A compound comprising a deliver}' construct selected from the deliver}' constructs shown in FIG. 4A, 5A, 6A, 7A, 8A, 9A, 10A, UA, 12A, 13A, 14A, 15A, 16A, 17A, 18A, 19A, 20A, 21A, 22A, 23A, 24A, 25A, and 26A.

335. The compound of claim 334, wherein in the deliver}' construct is the deliver}' construct shown in FIG. 4A.1201.336 The compound of claim 334, wherein in the delivery construct is the deliver}' construct show'll in FIG. 5A.

337. The compound of claim 334, wherein in the delivery construct is the deliver}' construct shown in FIG. 6A.

338. The compound of claim 334, wherein in the delivery constaict is the deliver}' construct shown in FIG. 7A.

339. The compound of claim 334, wherein in the deliver}' construct is the delivery construct shewn in FIG. 8A.

340. The compound of claim 334, w'herein in the deliver}' construct is the delivery constaict shown in FIG. 9A.1206.341 The compound of claim 334, wherein in the delivery construct is the deliver}' construct show'll in FIG. 10A.

342. The compound of claim 334, wherein in the delivery constaict is the deliver}' construct shown in FIG. 11 A.

343. The compound of claim 334, wherein in the delivery constaict is the deliver}' construct shown in FIG. 12A.

344. The compound of claim 334, wherein in the delivery construct is the delivery construct shown in FIG. 13A.

345. The compound of claim 334, wherein in the delivery construct is the delivery construct shown in FIG. 14A.

346. The compound of claim 334, wherein in the delivery construct is the delivery construct shown in FIG. 15A.

347. The compound of claim 334, wherein in the delivery construct is the delivery construct shown in FIG. 16 A.

348. The compound of claim 334, wherein in the deliver}' construct is the deliver}' construct shown in FIG. 17.1213.349 The compound of claim 334, wherein in the delivery construct is the delivery construct shown in FIG. 18A.

350. The compound of claim 334, wherein in the delivery construct is the deliver}' construct shown in FIG. 19 A.

351. The compound of claim 334, wherein in the delivery construct is the deliver}' construct shown in FIG. 20A.

352. The compound of claim 334, wherein in the deliver ' construct is the delivery construct shown in FIG. 21 A.

353. The compound of claim 334, wherein in the deliver' construct is the delivery construct shown in FIG. 22A.1218.354 The compound of claim 334, wherein in the delivery construct is the delivery construct shown in FIG. 23A.

355. The compound of claim 334, wherein in the delivery construct is the deliver ' construct shown in FIG. 24A.

356. The compound of claim 334, wherein in the delivery construct is the deliver}' construct shown in FIG. 25A.

357. The compound of claim 334, wherein in the delivery construct is the delivery construct shown in FIG. 26A.

358. A compound selected from a compound shown in FIG. 4C, 5B, 6B, 7B, 8B, 9B, 10B, 11B, 12B, 13B, 14B, 15B, 16B, 17B, 18B, 19B, 20B, 21 B, 22B, 23B, 24B, 25B, and 26B359. The compound of claim 358, wherein in the compound is the compound shown in FIG. 4B.

360. The compound of claim 358, wherein in the compound is the compound shown in FIG. 5B.

361. The compound of claim 358, wherein in the compound is the compound shown in FIG. 6B.

362. The compound of claim 358, wherein in the compound is the compound shown in FIG. 7B.

363. The compound of claim 358, wherein in the compound is the compound shown in FIG. 8B.

364. The compound of claim 358, wherein in the compound is the compound shown in FIG. 9B.

365. The compound of claim 358, wherein in the compound is the compound shown in FIG.1229.10B.

366. The compound of claim 358, wherein in the compound is the compound shown in FIG.1231.11B.

367. The compound of claim 358, wherein in the compound is the compound shown in FIG.1233.12B.1234.368 The compound of claim 358, wherein in the compound is the compound shown in FIG.1235.13B.

369. The compound of claim 358, wherein in the compound is the compound shown in FIG.1237.14B.

370. The compound of claim 358, wherein in the compound is the compound shown in FIG.1239.15B.

371. The compound of claim 358, wherein in the compound is the compound shown in FIG.1240.16B.

372. The compound of claim 358, wherein in the compound is the compound shown in FIG.1242.17B.

373. The compound of claim 358, wherein in the compound is the compound shown in FIG.1244.18B.

374. The compound of claim 358, wherein in the compound is the compound shown in FIG.1246.19B.1247.375 The compound of claim 358, wherein in the compound is the compound shown in FIG.1248.20A.

376. The compound of claim 358, wherein in the compound is the compound shown in FIG.1250.21A.

377. The compound of claim 358, wherein in the compound is the compound shown in FIG.1252.22B.

378. The compound of claim 358, wherein in the compound is the compound shown in FIG.1254.23B.

379. The compound of claim 358, wherein in the compound is the compound shown in FIG.1256.24B.1257.380 The compound of claim 358, wherein in the compound is the compound shown in FIG.1258.25B.

381. The compound of claim 358, wherein in the compound is the compound shown in FIG.1260.26B.

382. A compound selected from the compounds shown in FIG. 4D, 5C, 6C, 7C, 8C, 9C, 10C, 11C, 12C, 13C, 14C, 15C, 16C, 17C, 18C, 19C, 20C, 21 C, 22C, 23C, 24C, 25C, and 26C.

383. The compound of claim 358, wherein in the compound is the compound shown in FIG.1262.4C.

384. The compound of claim 358, wherein in the compound is the compound shown in FIG.1264.5C.

385. The compound of claim 358, wherein in the compound is the compound shown in FIG.1266.6C.

386. The compound of claim 358, wherein in the compound is the compound shown in FIG.1268.7C.1269.387 The compound of claim 358, wherein in the compound is the compound shown in FIG.1270.8C.

388. The compound of claim 358, wherein in the compound is the compound shown in FIG.1272.9C.

389. The compound of claim 358, wherein in the compound is the compound shown in FIG.1274.IOC.

390. The compound of claim 358, wherein in the compound is the compound shown in FIG.1276.11C.

391. The compound of claim 358, wherein in the compound is the compound shown in FIG.1278.12C.1279.392 The compound of claim 358, wherein in the compound is the compound shown in FIG.1280.13C.

393. The compound of claim 358, wherein in the compound is the compound shown in FIG.1282.14C.

394. The compound of claim 358, wherein in the compound is the compound shown in FIG.1284.15C.

395. The compound of claim 358, wherein in the compound is the compound shown in FIG. 16C.

396. The compound of claim 358, wherein in the compound is the compound shown in FIG.1286.17C.

397. The compound of claim 358, wherein in the compound is the compound shown in FIG.1288.18C.

398. The compound of claim 358, wherein in the compound is the compound shown in FIG.1290.19C.1291.399 The compound of claim 358, wherein in the compound is the compound shown in FIG.1292.20C.

400. The compound of claim 358, wherein in the compound is the compound shown in FIG.1294.21C.

401. The compound of claim 358, wherein in the compound is the compound shown in FIG.1296.22C.

402. The compound of claim 358, wherein in the compound is the compound shown in FIG.1298.23C.

403. The compound of claim 358, wherein in the compound is the compound shown in FIG.1300.24C.1301.404 The compound of claim 358, wherein in the compound is the compound shown in FIG.1302.25C.

405. The compound of claim 358, wherein in the compound is the compound shown in FIG.1304.26C.

406. A compound selected from the compounds shown in FIG. 4E, 5E, 6E, 7E, 8E, 9E, 10E, HE, 12E, 13E, 14E, I5E, 16E, 17E, ISE, I9E, 20E, 21E, 22E, 23E, 24E, 25E, and 26E.

407. The compound of claim 406, wherein in the compound is the compound shown in FIG. 4E.

408. The compound of claim 406, wherein in the compound is the compound shown in FIG. 5E.

409. The compound of claim 406, wherein in the compound is the compound shown in FIG. 6E.

410. The compound of claim 406, wherein in the compound is the compound shown in FIG. 7E.

411. The compound of claim 406, wherein in the compound is the compound shown in FIG. 8E.

412. The compound of claim 406, wherein in the compound is the compound shown in FIG. 9E.

413. The compound of claim 406, wherein in the compound is the compound shown in FIG.1312.10E.

414. The compound of claim 406, wherein in the compound is the compound shown in FIG.1314.HE.

415. The compound of claim 406, wherein in the compound is the compound shown in FIG.1316.12E.

416. The compound of claim 406, wherein in the compound is the compound shown in FIG.1318.13E.

417. The compound of claim 406, wherein in the compound is the compound shown in FIG.1320.14E.1321.418 The compound of claim 406, wherein in the compound is the compound shown in FIG.1322.15E.

419. The compound of claim 406, wherein in the compound is the compound shown in FIG.1324.16E.

420. The compound of claim 406, wherein in the compound is the compound shown in FIG.1326.17E.

421. The compound of claim 406, wherein in the compound is the compound shown in FIG.1327.18E.

422. The compound of claim 406, wherein in the compound is the compound shown in FIG.1329.19E.

423. The compound of claim 406, wherein in the compound is the compound shown in FIG.1331.20E.

424. The compound of claim 406, wherein in the compound is the compound shown in FIG.1333.21E.1334.425 The compound of claim 406, wherein in the compound is the compound shown in FIG.1335.22E.

426. The compound of claim 406, wherein in the compound is the compound shown in FIG.1337.23E.

427. The compound of claim 406, wherein in the compound is the compound shown in FIG.1339.24E.

428. The compound of claim 406, wherein in the compound is the compound shown in FIG.1341.25E.

429. The compound of claim 406, wherein in the compound is the compound shown in FIG.1343.26E.1344.430 A composition comprising a compound of any one of claims 1 to 429.1345.431 A method comprising administering the composition of claim 430 to a subject in need thereof.

Images