282results about "Tetrapeptides" patented technology

Provided are an antibody-drug conjugate, a preparation method therefor, and use thereof. The antibody-drug conjugate has a structure represented by the formula Ab-[M-L-E-D]x, has a superior drug-to-antibody ratio, and has an excellent targeted killing effect on various cancers or tumors.

Compositions and methods for treating diseases associated with dysregulation of miR-21, particularly cancer, are disclosed.

Provided are an antibody-drug conjugate, a method for preparing same, and use thereof. The antibody-drug conjugate has a structure represented by formula Ab-[M-L-E-D] x, a superior drug-to-antibody ratio, and an excellent targeted killing effect on various cancers or tumors.

The present invention provides a novel antithrombotic antibody, which targets FIXa and has unique properties, specifically targets the binding site of blood coagulation factors FIXa and FVIIIa, reduces the formation of FVIIIa-FIXa complex, blocks the conversion of FX to FXa, and exerts antithrombotic effects. The antibody of the present invention has suitable antithrombotic properties, has a wide effective therapeutic concentration window, but does not increase the risk of bleeding; it can realize the demand for moderate antithrombotic properties in clinical applications and effectively avoid bleeding problems caused by excessive effects. The present invention also discloses a method for screening drugs that target the FIXa-FVIIIa binding site.

The present disclosure relates to the technical field of polypeptides. Disclosed are a cyclic peptide, and a composition and the use thereof. The cyclic peptide of the present disclosure has a structure as shown in formula (I): Cyclo-[Gly-His-Lys-Lys] (I). The present disclosure specifically relates to the cyclic peptide or a salt thereof, or a composition thereof, and the use thereof in the preparation of a composition for caring or treating skin or mucosa.

The invention relates to coacervate-forming polymers having defined structural formulae. The invention also relates solutions comprising the coacervate-forming polymers and methods of making solutions comprising the coacervate-forming polymers. The invention also relates to polymer coacervates, comprising the coacervate-forming polymers within the coacervates, including polymer coacervates comprising cargo compounds, and methods for making such polymer coacervates. The coacervates of the invention are capable of penetrating into cells and thereby delivering cargo compounds into cells. The invention further relates to compositions, including pharmaceutical compositions, comprising the polymer coacervates. The invention also relates to uses of the coacervate-forming polymers, including medical uses.

The invention described herein pertains to the diagnosis, imaging, and / or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and / or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.

Peptides and methods of use thereof, are disclosed for use in treating various diseases and disorders, including inflammation, pain, oral mucositis, oral lesions, and cancer. The peptides modulate the activity of the transcription factor NF κB.

The invention relates to a novel polypeptide and application thereof. The polypeptide provided by the invention is short in peptide chain and faster and better in absorption. Experimental results show that the polypeptide provided by the invention shows an obvious enteric cavity dilatation relieving effect in pharmacodynamic tests of a zebra fish inflammatory bowel disease model and a rat inflammatory bowel disease model. The polypeptide provided by the invention has a remarkable colitis relieving effect, and can be used for preparing a medicine for treating enteritis, especially a medicine for treating ulcerative colitis.

A novel PACE4 inhibitor and use thereof in anti-osteoarthritis. A novel PACE4 inhibitory peptide is designed and synthesized, which can effectively inhibit the expression of extracellular PACE4 without affecting normal cells, and is stable in joints and unstable in plasma, so that the PACE4 inhibitory peptide has excellent safety and can be effectively used in the prevention and treatment of OA.

Compounds with the following structures and their analogs are provided. Compositions that include these structures can be used to inhibit glucose transporters and stop or decrease the proliferation of cancer, treat possible organ rejection and treat autoimmune disease.

The present invention relates to an antibody conjugate that is particularly suitable for targeting Trop-2 expressing cells, especially tumor cells. The antibody conjugate according to the invention has the structure (1), where AB is an antibody capable of targeting Trop-2 expressing tumors, L is a linker connecting Z to D, Z is a connecting group, and L 6 -GlcNAc(Fuc) w -(G) j -S-(L 7 ) w’ -, in which G is a monosaccharide, j is an integer ranging from 0 to 10, S is a sugar or a sugar derivative, GlcNAc is N-acetylglucosamine, Fuc is fucose, w is 0 or 1, w' is 0, 1, or 2, and L 7 is -N(H)C(O)CH2-, -N(H)C(O)CF2-, or -CH2-, D is exatecan, b is 0 or 1, x is 1 or 2, and y is 1, 2, 3, or 4. The present invention further relates to methods for preparing the antibody conjugates of structure (1) and applications of the antibody conjugates of structure (1).

Compositions comprising specific tetrapeptides, for use in treating, preventing, minimizing, diminishing or reversing various signs of aging of the skin are provided. The compositions are useful in improving the firmness or elasticity of skin, smoothing of fine-lines or wrinkles, reducing skin pores and hyperpigmentation, and increasing skin thickness, radiance and / or softness.

The present invention relates to a new polypeptide and its application. The polypeptide provided by the present invention has a short peptide chain and is absorbed faster and better. Experimental results show that the polypeptide provided in this application exhibits an obvious effect of alleviating intestinal lumen dilation in the zebrafish inflammatory bowel disease model and the rat inflammatory bowel disease model. The polypeptide provided by the present invention has a significant effect of alleviating colitis and can be used to prepare drugs for treating enteritis, especially drugs for ulcerative colitis.

The present invention provides biomolecular glass and its use. The biomolecular glass is obtained by volatilizing a solvent from a solution of biomolecular raw materials, the solution of biomolecular raw materials comprising biomolecular raw materials, a modifier, and a solvent. The biomolecular raw materials include natural amino acids, peptides, amino acid derivatives, peptide derivatives, or mixtures of two or more of the above. The soluble biomolecular glass of the present invention has excellent biocompatibility, high light transmittance, good mechanical strength, flexible processability, and biodegradability, and can be processed into implantable or non-implantable medical materials and / or devices, fillers and stent materials, electronic sensing materials and / or devices, temporary electronic materials and / or devices, etc., and can be decomposed by living organisms or nature, with decomposition products being non-contaminating.

The present invention relates to a method of preparing a salt of a β-turn peptidomimetic cyclic compound of formula (I) where R1, R2, R3, R4, R5, R6, R7, R8, R10, X, Y and n are as defined in the description, in particular a method of preparing a β-turn peptidomimetic cyclic compound having the following structure:

To provide a method for producing a high-purity peptide compound in a high yield under a condensation condition applicable even to a highly rare non-natural amino acid by using an easily available condensing agent and additive capable of suppressing prematurecleavage and also suppressing a side reaction especially in a condensation reaction process of a solid phase synthesis method of a peptide.SOLUTION: Provided is a method for producing a peptide compound, including a step of condensing a first amino acid or peptide and a second amino acid or peptide in the presence of an additive and a condensing agent to obtain a condensate, wherein the number of moles of the additive is smaller than the number of moles of the second amino acid or peptide. By using a small amount of the additive with respect to the amino acid or peptide to be added to the N-terminus, the condensation reaction can be allowed to proceed efficiently even when an amino acid having large steric hindrance is contained, and the target peptide compound can be obtained with high yield and high purity.SELECTED DRAWING: None

Provided is a method for producing a peptide compound or a salt thereof, including a step (linking step) of linking an amino group of a first amino acid or peptide and a carboxy group of a second amino acid or peptide with an amide bond, wherein a stand-alone condensing agent and one or more additive(s) are used in the linking step, and the additive(s) are one or more selected from the group consisting of HOPO, HOAt, HOOBt, HOCt, PfpOH, Oxyma, Oxyma-B, N-HOSu, and K-Oxyma.

To provide an amphiphilic compound capable of suppressing phase separation of a phospholipid membrane and stabilizing a phospholipid structure.SOLUTION: The present invention provides an amphiphilic compound for use as a stabilizer of two or more phospholipid compounds having different phase transition temperatures, the amphiphilic compound being represented by the following general formula (1).SELECTED DRAWING: Figure 2B

The present invention provides immunoconjugates of formula (I) comprising an antibody linked by conjugation to one or more 8-sulfonyl-2-aminobenzazepine derivatives. The present invention also provides 8-sulfonyl-2-aminobenzazepine derivative intermediate compositions comprising reactive functional groups. Such intermediate compositions are suitable substrates for the formation of the present immunoconjugates via a linker or linking moiety. The present invention further provides methods of treating cancer using the present immunoconjugates.

Methods for treating neurological disorders, central or peripheral nervous system injuries, and / or secondary pathologies thereof are provided. [Solution] The present disclosure also includes methods and compositions related to the use of compounds comprising specific peptides linked to dyes. In certain embodiments, the peptide DIRG is linked to a BODIPY dye. In specific embodiments, the compositions are used to treat neurological conditions and their associated secondary pathologies, such as spinal cord injury and Alzheimer's disease.

This invention provides novel antibody compounds and methods for using them. [Solution] Manipulated antibody compounds and their conjugates are provided, which are useful as agents for cancer immunotherapy.

The present invention provides a conjugate of an antibody and a functional substance, said conjugate having excellent desired properties, or a salt thereof. More particularly, the present invention provides a conjugate of an antibody and a functional substance, said conjugate containing a structural unit represented by formula (1) [wherein: Ig represents an immunoglobulin unit containing two heavy chains and two light chains and bonded to LA adjacent to Ig via thiol groups in the side chains of a plurality of cysteine residues in the two heavy chains and two light chains; HG represents a hydrophilic group or a monovalent group containing a hydrophilic group; CS represents a divalent group containing a cleavable moiety; ring A represents a divalent aromatic ring group which may have a substituent (wherein the divalent aromatic ring group constitutes a π-electron conjugated system together with the aforesaid cleavable moiety); V represents an oxygen atom, a sulfur atom or an amino(NH) group; LA and LB independently represent a divalent group; D represents a functional substance; and the average number n of the aforesaid bonds per immunoglobulin unit is 1.5 or more] or a salt thereof, and substances related thereto.

Peptides and Peptide-lipid conjugates are provided in which the peptide has the general Formula (I), wherein, A1 is selected from serine, threonine, O-C1-6 alkyl serine, and O-C1-6 alkyl threonine; A2 is selected from serine, threonine, O-C1-6 alkyl serine, and O-C1-6 alkyl threonine; A3 is selected from glutamic acid, glutamine, asparagine, and aspartic acid; A4 is proline; each A5 is independently selected from a natural or modified amino acid; The peptide-lipid conjugates can be used in lipid formulations for the delivery of nucleic acids.

The invention belongs to the technical field of organic synthesis and medicine, and particularly relates to an optical pure small peptide chemiluminescent probe. By changing the absolute configuration of amino acid on a peptide chain, the length of the peptide chain, the variety of the amino acid and the end-capping group of the peptide, the invention discloses the influence of the small peptide chemiluminescence probe on the recognition performance of mycobacterium tuberculosis based on chiral control and structural transformation, the chemiluminescence intensity and chiral structure-activity relationship, and the application of the small peptide chemiluminescence probe to the mycobacterium tuberculosis. The capability of distinguishing and specifically recognizing clinical sample mycobacteria is achieved. Compared with existing reports, the small peptide chemiluminescent probe disclosed by the invention creates and innovates a chiral environment of a small peptide terminal recognition fragment of the probe from a molecular level, so that a brand-new three-dimensional structure of the small peptide recognition fragment is constructed; further, an electronic effect, a steric hindrance effect, a pi-pi stacking effect, an interaction mode between a subject and an object and the like of a recognition center are changed, and the chemiluminescence probe which is higher in luminous intensity and excellent in recognition performance compared with an existing small peptide type mycobacterium tuberculosis probe is prepared and screened.

Provided are 3-4 residue non-natural macrocyclic oligoamides comprising species of 3 or 4 monomer residues selected from the group consisting of monomers a, b, c, d, e, f, g, h, I, j, k, l, m, n, o, p, q, r, s, t, u, and v as defined in Table 1, and methods for designing such macrocyclic oligoamides.

Polypeptide and its application as CCK receptor agonist / antagonist. This polypeptide has relatively high agonist / antagonist activity on CCK receptor. Compared with polypeptide CCK4, this polypeptide has a long half-life and long duration of therapeutic effect in vivo. Experiments have shown that this polypeptide has obvious improving effect on the spatial memory impairment of aged mice, aged memory impairment mice and Alzheimer's disease mice, so that said polypeptide has great application potential.

The present invention provides an intermediate of an antibody-drug conjugate containing SN38, in which a biologically active water-soluble group PEG is introduced into the linker and the PEG is structurally modified, and a method for preparing the same. This preparation method has a simple procedure, is low cost, and is more environmentally friendly since it does not introduce heavy metal ions during the reaction. Furthermore, the intermediate of the antibody-drug conjugate synthesized by this preparation method has higher stability and efficacy than the intermediate of the antibody-drug conjugate using SN38 as a toxin in the conventional technology.

The invention relates to a novel polypeptide and application thereof. The polypeptide provided by the invention is short in peptide chain and faster and better in absorption. Experimental results show that the polypeptide provided by the invention shows an obvious enteric cavity dilatation relieving effect in pharmacodynamic tests of a zebra fish inflammatory bowel disease model and a rat inflammatory bowel disease model. The polypeptide provided by the invention has a remarkable colitis relieving effect, and can be used for preparing a medicine for treating enteritis, especially a medicine for treating ulcerative colitis.

The invention relates to modified peptides comprising an amino acid sequence of SEQ ID NO: 1 to 80 and a N- and / or C- terminal modification, preferably with an acetyl and / or a carboxyl group modification. The present invention also relates to a composition comprising said modified peptides, to methods for inhibiting contraction of muscle cells and for improving the skin, and the use of said modified peptide.