806 results about "Cyclic peptide" patented technology

This disclosure provides cyclic peptide compounds of formula (A) or formula (II) as inhibitors of Ras kinase, and compositions and use of the same in treating diseases associated with Ras kinase.

Disclosed are a pentapeptide compound and a composition and use thereof, relating to the technical field of polypeptides, the peptide or a salt thereof having a structure as shown in formula (I): R1-Lys-Lys-Leu-Ala-R2 (I). The invention also relates to a cyclic peptide, and the structure of the cyclic peptide is Cyclo-[Lys-Lys-Lys-Leu-Ala]. The compound disclosed by the invention has the effects of controlling oil, repairing, resisting oxidation and the like, and can be used for nursing skin or mucosa.

The present invention relates to compounds of the formulae (I) or (XX) that are panRAS inhibitors for use in a method of treating cancer.

The invention discloses a cyclic hexapeptide for skin care and a composition and application thereof, and relates to the technical field of polypeptides, and the cyclic peptide has the following structure: Cyclo-[Arg-Arg-Gln-D-Met-Glu-Glu]. Specifically, the invention relates to the cyclic peptide or the salt thereof, or a composition of the cyclic peptide and the salt thereof, and application of the cyclic peptide and the salt in preparation of a composition for nursing or treating skin or mucosa.

The invention relates to the field of computer-aided drug design (CADD) and molecular informatics, in particular to a multi-modal representation learning method based on cyclopeptide molecules, which is used for predicting cell membrane permeability of cyclopeptide. The method mainly comprises the following steps: (1) data collection: integrating cyclic peptide permeability data from a ChEMBL database, a CycPeptMPDB database and a CyclicPepeda database and patent literatures; (2) multi-modal learning: for different modal data, a deep learning model is adopted to extract feature representations of the data; the method comprises the following steps of: encoding an SMILES sequence by using ChemBERTa (ChemBERTa); using Vision Transform to extract molecular image features, and learning a molecular image structure and 3D coordinate information based on GNN; (3) multi-modal feature fusion: adopting a self-adaptive extensible fusion mechanism, integrating SMILES feature information into image, graph and 3D coordinate features through a cross-modal feature fusion mechanism, and splicing all modal features to obtain multi-modal molecular representation; and (4) permeability prediction: sending the multi-modal molecular representation into a full connection layer for regression prediction so as to evaluate the permeability of the cyclopeptide.

The invention discloses a cyclic peptide compound as well as a preparation method and application thereof, belongs to the field of polypeptide synthesis and application, and particularly relates to full-protection peptide resin prepared by solid-phase synthesis. Carrying out cutting and monocyclization on the full-protection peptide resin to obtain monocyclic peptide; the monocyclic peptide is subjected to binary cyclization treatment to obtain a cyclic peptide compound Cyclo (His-Lys-Cys-Gly-His-Lys-Cys-Gly-, and a disulfide bond is in bridge connection with Cysamp; and the binary cyclization is cyclized under the action of iodine methanol and ascorbic acid. The cyclopeptide compound prepared by the invention has the advantages of low toxicity, good stability, good antioxidant effect and good anti-inflammatory effect, and the expression of type I collagen can be improved. Therefore, the invention has the advantages of low toxicity, good stability, good antioxidant effect and good anti-inflammatory effect, and can improve the expression of the type I collagen.

Provided herein are novel cyclic peptides, their synthetic process, compositions, properties including stability and pharmacokinetic profiles, and applications for treating solid tumor cancers.

The invention discloses a PEI and targeting peptide modified magnetic nano-carrier and a preparation method and application thereof. The nano-carrier is regular in morphology and uniform in particle size and has good crystallinity and magnetic performance. E5 polypeptide and RGD cyclic peptide on the surface of the nano-carrier are respectively combined with CXCR4 protein and integrin on the surface of a tumor cell, and the nano-carrier and CXCR4 are internalized into lysosome through an integrin-mediated way, so that the target protein CXCR4 is degraded. The PEI in the nano-carrier can load and deliver siRNA into tumor cells to silence the expression of CXCR4 mRNA (messenger Ribonucleic Acid). Through nucleic acid delivery and a protein targeted degradation strategy, the CXCR4 level of tumor cells is jointly reduced, the migration ability of the tumor cells is inhibited, and meanwhile, the anti-tumor effect of M1 type polarization of macrophages is activated.

The invention discloses an antibacterial cyclic peptide screening system and method based on a multi-modal cross attention mechanism, and belongs to the field of antibacterial cyclic peptide screening, the antibacterial cyclic peptide screening system comprises the antibacterial cyclic peptide screening system of the multi-modal cross attention mechanism, the antibacterial cyclic peptide screening system of the multi-modal cross attention mechanism comprises a multi-modal cross attention screening model and a multi-modal cross attention screening model, the method is used for screening antibacterial cyclic peptides; data of the data input module comprises a one-dimensional sequence, a two-dimensional structure and a three-dimensional structure, data sources in the data input module comprise but are not limited to APD3, DRAMP and a Un i Prot public database, and the data input module is used for conveying data of the antibacterial cyclic peptide; through cooperative use of the devices, the cross attention fusion module is arranged, and weights of different modals are dynamically allocated, so that a key active region of the antibacterial cyclic peptide is more obvious, and a multi-modal cross attention screening model can more accurately identify related characteristics of the antibacterial activity of the antibacterial cyclic peptide; the screening of the antibacterial cyclic peptide is more accurate.

The invention provides a cyclic peptide as well as a preparation method and application thereof. The cyclic peptide has an amino acid sequence # imgabs0 # represented by formula (1) (wherein X is a Lys residue modified with a fatty acid molecule, and a line connecting Arg and Lys represents an amide bond. The cyclic peptide prepared by the invention has wide antifungal activity and antibacterial activity on drug-resistant bacteria; meanwhile, the biotoxicity and the protease degradation resistance are high, and the in-vivo antibacterial effect of the cyclopeptide can be prolonged. The cyclic peptide can be applied to preparation of anti-bacterial and anti-fungal infection drugs, and can be used as an excellent substitute drug or an auxiliary drug of existing antibiotics. The method for preparing the cyclic peptide is simple, raw materials are easy to obtain, and industrial production can be achieved.

The invention discloses a bidirectional reversible conversion method and system between a peptide molecule SMILES and a sequence expression. The core innovation lies in that a new sequence description syntax is defined to retain information of a polypeptide special bond and specific modification of amino acid; a main chain atom index and adjacency traversal topology identification algorithm is adopted, and end group and topology integrated detection and coding are carried out; a residue recognition algorithm for main chain cutting and template library matching is compatible with any standard or non-standard amino acid residues, an extensible end group library / monomer template library and an automatic increment mechanism, and automatic recognition and sequence annotation of S-S disulfide bonds; the invention relates to a high-fidelity assembly algorithm of HELM anchor points and topology aware cyclic peptide processing. The method solves the problems of incapability of supporting a complex polypeptide topological structure, poor reversibility, insufficient expansibility of a monomer library and the like in the prior art, can be widely applied to scenes of quantitative structure-activity relationship model construction, large-scale polypeptide data cleaning and the like, and has remarkable practicability and innovativeness.

The invention relates to the technical field of cosmetics, in particular to application and a synthesis method of cyclic peptide. The inhibition objects of the cyclic peptide comprise IL-1beta, IL-6 and TNF-alpha (Tumor Necrosis Factor-alpha); when the concentration is less than or equal to 10ppm, the inhibition rate on IL-1beta is greater than or equal to 40%, the inhibition rate on IL-6 is greater than or equal to 50%, and the inhibition rate on TNF-alpha is greater than or equal to 40%. The cyclopeptide has a barrier repairing effect and can improve FLG expression; meanwhile, the moisturizing effect is achieved, and percutaneous moisture loss of the skin can be reduced. The invention provides a group of cyclic peptides, which has excellent anti-inflammatory, moisturizing, barrier repairing and soothing effects, and compared with the existing straight-chain peptides in the market, the group of cyclic peptides has more obvious anti-inflammatory and soothing effects, and has a certain skin barrier repairing effect. The group of cyclic peptides can be applied to the fields of cosmetics and skin care products, and the product efficacy is improved; and the synthetic method of the cyclic peptide is easy to implement and wide in application prospect.

The invention provides a coordination nano assembly of chiral cyclopeptide and manganese ions as well as a preparation method and application of the coordination nano assembly. According to the method, a manganese superoxide dismutase protein structural domain and a unique tumor microenvironment of melanoma high tyrosinase are combined, and polypeptide sequences L-YD-hL-DD-h, L-YL-HL-DL-H and D-yD-hD-dD-h with different chirality are designed for the first time; the chirality of the polypeptide is regulated and controlled, the in-vivo circulation stability and the cell entry efficiency of the nano assembly are improved, the coordination self-assembly of manganese and different chiral cyclopeptides is realized, and the in-situ oxidation of an in-vivo tumor microenvironment is simulated for photo-thermal therapy and cell membrane coating. The method disclosed by the invention is simple, mild in experimental condition and easy to operate, the prepared cell membrane coated nano assembly not only has long circulation stability and high cell entry efficiency, but also can realize mild photo-thermal therapy through in-situ oxidation, releases manganese ions to activate a CGAS-STING pathway for immunotherapy of tumors, and has a wide application prospect. The potential application value is realized in the field of combined treatment of tumors.

The invention belongs to the technical field of nuclear medicine molecular diagnosis and treatment, and discloses a modified CAIX targeting cyclic peptide, a nuclide marker and application of the modified CAIX targeting cyclic peptide in tumor diagnosis and treatment. According to the CAIX targeted cyclic peptide, a rigid bifunctional chelating agent RESCA is introduced to replace a traditional chelating agent, and a sulfonated or alkylated amino acid connector is combined, so that the enzymolysis resistance and in-vivo stability of the probe are remarkably improved. By optimizing the structure of the connector, the lipophilicity is reduced, liver and gall metabolism and non-specific uptake are reduced, and the high uptake rate of tumor target tissues is maintained. The therapeutic nuclide marker of the cyclopeptide can be used for intratumoral irradiation therapy using DOTA or NOTA in combination with an alkylated amino acid linker or an albumin ligand. Experiments show that the marker has high radiochemical purity, excellent pharmacokinetic characteristics and low kidney retention, and is suitable for precise diagnosis and targeted therapy of CAIX high expression tumors such as kidney cancer, colorectal cancer and brain glioma.

The invention provides a polypeptide boron carrying agent. The polypeptide boron carrying agent comprises a polypeptide and at least one boron-containing group connected with a main chain or side chain amino group of the polypeptide, the polypeptide comprises at least one MAP peptide and a c (RGD-DPhe-K) cyclic peptide, the C end of the at least one MAP peptide is connected with the N end of the c (RGD-DPhe-K) cyclic peptide, and the MAP peptide is a KLALKLALKAALKLA continuous sequence. The polypeptide boron carrying agent provided by the invention has better targeting property and cell penetrability to tumor cells, has high boron loading amount, and meets the requirements of boron neutron capture therapy.

The invention discloses a nanorana alpine antioxidative peptide and application thereof. The antioxidative peptide is a cyclic peptide composed of 29 amino acids, the amino acid sequence of the antioxidative peptide is as shown in SEQ ID NO.1, and cysteine at the seventh position and cysteine at the twelfth position form an intramolecular disulfide bond. The invention further discloses nucleotide for coding the antioxidative peptide of the nanorana pleskei. The antioxidative peptide has good anti-inflammatory and anti-oxidation effects, can protect plasmid DNA damaged by H2O2, inhibits accumulation of CuSO4 induced zebrafish larva active oxygen and migration of neutrophil, and relieves mouse skin injury induced by UVB radiation.

The invention relates to a turtle-derived cyclic peptide compound with an anti-tumor effect and a preparation method thereof. The preparation method comprises the following steps: crushing tortoise plastron, adding water for reflux extraction, filtering, concentrating and drying to obtain tortoise-shell glue; dissolving the obtained tortoise-shell gelatin in water, adding protease for enzymolysis, and centrifuging after enzyme deactivation to take supernate; carrying out graded filtration on the obtained supernate and collecting components; and separating and purifying the collected components to obtain the cyclic peptide. The obtained compound has remarkable anti-tumor activity and has a good application prospect in preparation of anti-tumor drugs.

The invention discloses a radix pseudostellariae extract with high content of radix pseudostellariae cyclic peptide B and a preparation method and cosmetic application of the radix pseudostellariae extract, and belongs to the technical field of cosmetics. The preparation method comprises the following steps: (1) crushing radix pseudostellariae, adding alcohol and performing ultrasonic treatment to obtain feed liquid; (2) adding a compound enzyme into the feed liquid to carry out enzymolysis, enzyme deactivation, solid-liquid separation, concentration and impurity removal to obtain an enzymatic hydrolysate; and (3) eluting the enzymatic hydrolysate with macroporous resin to obtain an eluent, and drying to obtain the product, the compound enzyme is prepared from pectinase, papain, beta-glucosidase, cellulase and xylanase according to the mass ratio of (5 to 10) to (0.5 to 1) to (3 to 7) to (0.3 to 1). The radix pseudostellariae extract disclosed by the invention is prepared by adopting an enzymolysis process, more active ingredients can be reserved, the content of radix pseudostellariae cyclic peptide B in the obtained extract is high, and the radix pseudostellariae extract has relatively good anti-inflammatory, soothing, repairing and anti-aging effects.

The invention relates to an acinetobacter baumannii resistant cyclic peptide and application thereof, in particular to a compound shown in a formula (I), a tautomer, a stereoisomer, a hydrate, a solvate, pharmaceutically acceptable salt or prodrug of the compound and a preparation method of the tautomer, the stereoisomer, the hydrate, the solvate and the pharmaceutically acceptable salt or prodrug of the compound. The invention further discloses application of the acinetobacter baumannii in preparation of drugs for treating or preventing infection and diseases caused by the acinetobacter baumannii. # imgabs0 #

The invention belongs to the technical field of polypeptides and biological medicines, and particularly relates to a WK7 series antibacterial peptide and application thereof in the aspects of resisting bacteria and preventing and treating diabetic foot, pneumonia and septicemia. According to the invention, a linear peptide WK7-line with an amino acid sequence of WKRWKRW is used as a minimum active unit, and modification is carried out to form a plurality of linear modified peptides; meanwhile, a cyclic peptide WK7-cyl is formed on the basis of the linear peptide WK7-line through cyclization, and the cyclic peptide WK7-cyl is further modified to form an annular modified peptide. The linear peptide WK7-line, the linear modified peptide, the cyclic peptide WK7-cyl and the cyclic modified peptide jointly form the WK7-series antibacterial peptide, and the WK7-series antibacterial peptide is artificially synthesized polypeptide, is small in molecular weight, easy to synthesize, free of cytotoxicity, almost free of hemolysis risk, high in sterilization speed and broad-spectrum antibacterial property and can be used for preparing the antibacterial peptide. The traditional Chinese medicine composition has a certain effect on prevention and treatment of diabetic foot ulcer, pneumonia and septicemia.

This invention belongs to the field of biomedical technology and discloses a method for targeting GABA. A The receptor-dependent cyclic peptide analgesic DZ2 has the following amino acid sequence: Cys-Asn-Thr-Glu-Arg-Pro-Gly-Met-Leu-Asp-Phe-Lys-Gly-Lys-Ala-Lys-Trp-Asp-Ala-Trp-Cys, where the N-terminal Cys and C-terminal Cys are cyclically linked by a disulfide bond, and the molecular weight is 2454.81 g / mol. This cyclic peptide can be obtained through classic Fmoc-solid-phase synthesis, using GABA... A Receptor-targeting drugs play an important role in drug development. The compounds provided in this invention can activate GABA. A The receptor generates a GABA-like inward current. Furthermore, DZ2 exhibits excellent analgesic effects in a mouse pain model, providing a potential alternative for GABA-based analgesics. A This provides new ideas and theoretical basis for the development of receptor-based analgesics.

The invention discloses an anti-aging and anti-oxidation bicyclic peptide compound as well as a preparation method and application thereof, belongs to the technical field of polypeptide compound synthesis, and particularly relates to full-protection peptide resin prepared by solid-phase synthesis. Carrying out cutting and unitary cyclization on the full-protection peptide resin to obtain unitary cyclic peptide; carrying out binary cyclization treatment on the unitary cyclic peptide to obtain a bicyclic peptide compound Cyclo (His-Cys-Lys-Gly-His-Cys-Lys-Gly-, and bridging a disulfide bond with Cysamp; the binary cyclization comprises cyclization under the action of iodo methanol and ascorbic acid; or the binary cyclization is cyclized in DMSO (Dimethylsulfoxide). The anti-aging and anti-oxidation bicyclic peptide compound prepared by the preparation method disclosed by the invention has the following beneficial effects of low toxicity, good stability, capability of improving I-type collagen expression, good anti-oxidation effect and good anti-inflammatory effect.

The invention relates to the technical field of nuclear medicines, and particularly discloses a Nectin-4-targeting bicyclic peptide nuclide ligand, a probe, a preparation method and application thereof. The invention relates to a Nectin-4-targeted bicyclic peptide nuclide ligand, which has a structure as shown in a formula I: # imgabs0 # formula I, and the Nectin-4-targeted bicyclic peptide nuclide ligand has a structure as shown in a formula II. The bicyclic peptide nuclide ligand and the probe have remarkable advantages in the aspects of radioactive stability, pharmacokinetic characteristics, tumor Nectin-4 binding specificity, tumor uptake ability, tumor and muscle uptake ratio, in-vivo metabolic performance and the like.

The invention relates to a cyclopeptide inhibitor aiming at human STING (stimulating interferon gene) and application of the cyclopeptide inhibitor. The cyclic peptide can specifically bind to and inhibit activation of human STING. The invention also provides a nanoparticle delivery system for loading the cyclopeptide on a cationic polymer PBAE and an amphiphilic polymer pDMA-pEPEMA, and a preparation method of the nanoparticle delivery system. The cyclic peptide and the nanoparticles thereof can be used for preparing medicines for treating autoimmune diseases (such as systemic lupus erythematosus and the like) caused by excessive activation of the cGAS-STING signal pathway. Compared with the existing small molecule STING inhibitor, the cyclopeptide inhibitor provided by the invention has higher specificity, stability and inhibition effect.

The present invention relates to a fibroblast activation protein alpha (FAP)-targeting conjugate comprising Formula I: Y-L-X, wherein Y is a chelator or cytotoxic drug, L is a linker, and X is a molecule comprising a cyclic peptide of formula A-[Z-AA1-AA2-AA3-AA4-AA5-AA6-AA7-Z]-B. A is N-terminal structure. B is C-terminal structure, and each of the Z, AA1, AA2, AA3, AA4, AA5, AA6, AA7 is a residue of an amino acid.

The present invention discloses a class of bicyclic peptide compounds and their applications, belonging to the technical field of bicyclic peptide compounds. Specifically, the invention relates to the preparation of a fully protected peptide resin using solid-phase synthesis; cleavage and monocyclic cyclization of the fully protected peptide resin to obtain a monocyclic polypeptide; and dicyclic cyclization of the monocyclic polypeptide to obtain a bicyclic peptide compound, wherein the dicyclic cyclization is carried out under the action of iodine methanol and ascorbic acid. The bicyclic peptide compound prepared by the present invention has the following beneficial effects: good safety, low cytotoxicity, good stability, slow degradation rate, good effect on enhancing collagen expression, good effect on enhancing elastin expression, and good effect on inhibiting neurotransmitter release.

The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of membrane type 1 metalloprotease (MT1-MMP). The invention also describes drug conjugates comprising said peptides, conjugated to one or more effector and / or functional groups which have utility in imaging and targeted cancer therapy.

The present invention relates to a heterotandem bicyclic peptide complex which comprises a first peptide ligand, which binds to Nectin-4, conjugated via a linker to two second peptide ligands, which bind to CD137. The invention also relates to the use of said heterotandem bicyclic peptide complex in preventing, suppressing or treating cancer.

The invention belongs to the technical field of biochemistry, and particularly relates to a DR8 cyclic peptide analogue and application thereof. The structure of the DR8 cyclopeptide analogue is R1-dAsp-His-Asn-Cys-Pro-Gln-dAla-Cys-CONH2, in the structural formula, R1 is a chain alkyl group with 1 to 30 carbon atoms, and a fourth amino acid and an eighth amino acid are subjected to cyclization through the chain alkyl group. The biological activity of the DR8 cyclic peptide analogue is researched, and an in-vitro cell model and an in-vivo animal model of renal fibrosis are constructed to evaluate indexes such as in-vitro anti-fibrosis activity, inhibition effect and in-vivo treatment effect of the DR8 cyclic peptide analogue. And the cytotoxicity, serum stability and pharmacokinetics of the DR8 cyclopeptide analogue are researched. Results show that compared with the polypeptide DR3penA, the DR8 cyclic peptide analogue obtained by the invention has better activity indexes and stability in all aspects, and can be used for preparing medicines for preventing renal fibrosis diseases.

Provided herein are novel cyclic peptides, their synthetic process, compositions, properties including stability and pharmacokinetic profiles, and applications for treating solid tumor cancers.