416 results about "Cyclic peptide" patented technology

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 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 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 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.

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 invention provides a cyclic peptide used for treating, improving or preventing nervous system injury of mammals or diseases or pains caused by the injury, neurodegenerative diseases, anxiety or epilepsy or used as a neuronal protective agent, a conjugate containing the cyclic peptide, a pharmaceutical composition containing the cyclic peptide or the conjugate and application of the cyclic peptide and the conjugate.

The invention provides a bicyclic peptide as well as a preparation method and application thereof in cosmetics. Specifically provided is a bicyclic peptide or a salt thereof, which has a structure as shown in formula I. The bicyclic peptide or the salt thereof provided by the invention can be applied to skin care products, has one or more effects of moisturizing, repairing, anti-aging and the like, and has a good application prospect;

Disclosed are cell-penetrating cyclic peptides. The peptides can be used to deliver peptides and other biologically active moieties into cells. Formulations containing the cell-penetrating cyclic peptides are also described.

The invention belongs to the technical field of nuclear medicine, and relates to a CAIX-targeted cyclic peptide and a preparation method and application thereof, the CAIX-targeted cyclic peptide structure is shown as a formula 1, Linker is a cyclization connexon, and Chenator is a nuclide chelating group. The CAIX-targeted cyclic peptide provided by the invention has high affinity with CAIX, and has low affinity with isoenzyme CAII of CAIX, so that the CAIX-targeted cyclic peptide has high selective affinity with CAIX; the nuclide-labeled radioactive probe has high labeling rate and excellent in-vitro stability, has excellent pharmacokinetic characteristics in tumor-bearing model mice of human renal clear cell carcinoma, and has extremely high tumor uptake, tumor-muscle ratio and tumor-kidney ratio which can meet diagnosis requirements; due to the long-time retention characteristic in tumors, the polymer has a relatively high tumor treatment application value.

The invention discloses application of a cyclic peptide compound BIM 23042 or a preparation thereof in preparation of medicines for treating bacterial infectious diseases, and belongs to the technical field of medicines. The invention discloses a cyclic peptide compound BIM 23042 as an antibiotic synergist for the first time, and the cyclic peptide compound BIM 23042 is used for treating bacterial infectious diseases. According to the application disclosed by the invention, the cyclopeptide compound BIM 23042 and polymyxin are combined for use, so that the growth of gram-negative bacteria can be effectively and synergistically inhibited. The combined medication scheme shows a remarkable advantage in coping with acinetobacter baumannii. The cyclic peptide compound BIM 23042 disclosed by the invention has an anti-infection capability, and the anti-infection capability is specifically shown as reducing the inflammatory response of macrophage RAW 264.7 induced by LPS (Lipopolysaccharide) and also reducing the apoptosis of the macrophage RAW 264.7 caused by the LPS. The invention provides a new perspective for developing a novel drug-resistant gram-negative bacterium prevention and control strategy, and also provides a new treatment scheme for coping with bacterial infection.

Disclosed are cell-penetrating cyclic peptides. The peptides can be used to deliver peptides and other biologically active moieties into cells. Formulations containing the cell-penetrating cyclic peptides are also described.

The present invention relates to the technical field of medicine, and specifically relates to a disulfide cyclic peptide compound of a polypeptide small molecule-based melanocortin receptor (MCR) agonist. The disulfide cyclic peptide compound has the following structure: R2-R1-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-R3-R4, wherein R2 and R4 are each independently selected from an amino group, an acetyl group or a palmitoyl group, R1 and R3 are each independently selected from Ile, Arg, D-Phe, or Pro, or deleted, R1 and R3 are not deleted at the same time, and when R1 or R3 is deleted, at least one of R2 and R4 is a palmitoyl group. The disulfide cyclic peptide compound provided by the present invention has good selectivity to MCRs (MCR1, MCR3, MCR4, and MCR5).

The application belongs to the technical field of biological medicine, and discloses a cyclic peptide molecule specifically targeting CD5 and purposes thereof. The surface receptor CD5 of immune cells (T cells, B cells) has been proved to be a potential tumor treatment target, the present application uses the phage display technology widely applied to the development of polypeptide or antibody drugs to carry out multiple rounds of in vitro screening on human CD5 protein, and obtains a cyclic peptide molecule with drug potential and capable of specifically combining with CD5 through second-generation sequencing. The cyclic peptide molecule contains two cysteines, is modified into a ring through a specific chemical crosslinking agent, and the affinity of the cyclic peptide molecule to CD5 is determined to be in the low micromolar level through surface plasmon resonance technology, thereby laying a foundation for the development of a CD5-targeting inhibitor.

Provided in the present application are a cyclic peptide mutant and use and product thereof for the preparation of a coronavirus inhibitor, belonging to the technical field of cyclic peptide drugs. The present application is optimized on the basis of the cyclic peptide 6L3-3P11R. The obtained cyclic peptide mutant can resist the enzyme digestion effect of pancreatic enzymes and exhibits further improved antiviral activity, which is of great significance for expanding antiviral applications of cyclic peptide drugs.

The invention provides a molecular probe targeting EDB-FN as well as a preparation method and application of the molecular probe. The structural formula of the molecular probe targeting EDB-FN is shown in the specification, according to the molecular probe targeting EDB-FN, the probe is based on a cyclic peptide probe with Lys-Glu side chain lactam bridge conformation fixed, the connection mode of a DOTA chelating agent is optimized, and the clinical transformation bottlenecks that an existing probe is poor in stability, low in affinity, insufficient in targeting specificity, poor in diagnosis and treatment integration compatibility and the like are solved. The probe can be used for early diagnosis and molecular imaging research of tumors, and provides a reliable basis for tumor malignancy degree evaluation and treatment effect monitoring.

This invention discloses a method for preparing a cyclic peptide compound containing a cisamide bioelectron isosteric cyclic peptide. The method involves introducing a thioamide unit at a specific position on the peptide backbone, making it a potential activatable reaction site. This site is selectively activated by a metal salt and undergoes an intramolecular condensation reaction with an acylhydrazine group located in the same peptide chain, generating a 1,2,4-triazole heterocyclic structure in situ. In a single reaction process, the cyclization of the peptide and the precise construction of the cisamide bioelectron isosteric group in the peptide backbone are achieved simultaneously.

The present invention relates to a cyclic peptide, a conjugate comprising said cyclic peptide and a lipopeptide building block, a bundle of said conjugates, a synthetic virus-like particle comprising at least one bundle of conjugates and pharmaceutical compositions comprising the same. The present invention further relates to said cyclic peptide, said conjugate said bundle of conjugates, said synthetic virus-like particle and said pharmaceutical compositions for use as a medicament, preferably for use in a method for preventing of an infectious disease or reducing the risk of an infectious disease, more preferably for use in a method for preventing or reducing the risk of an infectious disease associated with or caused by a respiratory syncytial virus.

The invention relates to a sulfur-containing tryptophan cyclic peptide compound as well as a synthesis method and application thereof. The synthesis method comprises the following steps: carrying out electrolytic reaction on a tryptophan peptide compound with a structure as shown in a formula I or a stereoisomer thereof and a thiosulfonate compound with a structure as shown in a formula II to obtain the sulfur-containing tryptophan cyclic peptide compound with a structure as shown in a formula III or a stereoisomer thereof. The sulfur-containing tryptophan cyclic peptide compound can be obtained by directly electrolyzing the tryptophan peptide compound by adopting an electrochemical method, so that the use of a transition metal catalyst and stoichiometric alkali is avoided, the generation of chemical wastes is avoided, and the realization of atom economy is facilitated. The method has the advantages of simple operation, high product purity, easy purification, high efficiency and yield, low production cost, mild reaction conditions, no need of inert gas protection, greener reaction system, environmental protection, safety, economy, energy saving and environmental protection, and is more conducive to realization of industrial production.

The invention discloses an STING agonist polypeptide conjugate as well as a composition and application thereof, and belongs to the field of medicinal chemistry, an STING agonist and a straight-chain peptide or a cyclic peptide are directly connected or connected through a linking group, the formed conjugate can target a tumor microenvironment, and the STING agonist is controllably released in specific time and space, so that the tumor microenvironment is inhibited, and the tumor microenvironment is inhibited. Therefore, the drug enrichment amount of the tumor site is increased, the drug treatment efficiency and bioavailability are improved, the toxic and side effects are reduced, and the purposes of effect enhancement and toxicity reduction are achieved. According to the STING agonist polypeptide conjugate, the targeting property of STING agonist drugs on tumor tissues is improved, the toxic and side effects on normal tissues are reduced, the STING agonist polypeptide conjugate is a brand-new immune agonist type coupling drug, and a new scheme is provided for tumor immunotherapy research.

A FAP glycopeptide as represented by Formula (I), and a radionuclide marker thereof and the use thereof. The FAP glycopeptide is obtained by modifying a linker portion that forms a cyclic peptide on the basis of a polypeptide FAP-2286 structure, and further introducing mono- or di-saccharide molecules. After being marked with radionuclides, the glycopeptide shows superior tumor uptake and lower liver uptake compared to FAP-2286, resulting in better imaging outcomes, facilitating the development of candidate radionuclide pharmaceuticals with further research value, and contributing to the ultimate goal of developing FAP-targeted cyclic peptide radiopharmaceuticals with independent intellectual property rights. Drawing_references_to_be_translated

The invention discloses a fully-protected polypeptide and a preparation method thereof, belongs to the technical field of polypeptide compound synthesis, and particularly relates to fully-protected peptide resin prepared through 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.

An object of the present invention is to provide a method for predicting cell membrane permeability of a cyclic peptide, which enables versatile design of a cyclic peptide with cell membrane permeability. According to the present invention, there is provided a method for predicting cell membrane permeability of a cyclic peptide, the method including a first step of acquiring a structure of the cyclic peptide; a second step of calculating a molecular shape factor r which is calculated by Expression (1) after a step of carrying out an ellipsoidal approximation for obtaining each of axis lengths a, b, and c in a case where an axis length in a longest axis direction of a main chain structure is denoted by a, and axis lengths in two other directions which are orthogonal to a and are orthogonal to each other are denoted by b and c in the structure acquired in the first step; and a third step of determining that the cyclic peptide having the molecular shape factor r in a range of 0.4 to 0.6 has cell membrane permeability. r=2b2+c2a2+b2+c2+a2

The invention relates to the technical field of nuclear medicine and radiopharmaceuticals, in particular to a labeled precursor, a probe and a preparation method and application of the labeled precursor and the probe. The probe prepared by using the cyclopeptide nuclide ligand disclosed by the invention has good stability, excellent pharmacokinetics, good binding specificity with EPHA2, relatively high tumor uptake, relatively high tumor-muscle uptake ratio and good in-vivo metabolism performance, and has a good clinical application prospect.

This invention discloses a selenylamide-based hydrogenation reaction of acetylacetamide compounds and its application in the modification of selenium-containing peptides and proteins, belonging to the fields of organic chemistry and chemical biology. The reaction involves the reaction of a selenium-containing compound with an acetylacetamide compound in a solvent with the addition of an additive. The applications of this reaction include: 1) selective modification and labeling of selenocysteine ​​in peptides and proteins; 2) cyclization reactions of selenium-containing peptides and selenoproteins; and 3) sequential modification of selenium-containing peptides in the presence of cysteine ​​by precise pH control combined with the hydrogen sulfide reaction of acetylacetamide. This reaction has advantages such as mild conditions, simple operation, fast reaction rate, high yield, good stability, and good selectivity. It provides a new and robust approach for the selective modification and labeling of selenium groups in bioconjugations, peptides, and / or proteins, and also provides a new method for the construction of cyclic peptides, offering a powerful tool for the development of selenium-containing peptide drugs.

The present disclosure describes cyclic peptide inhibitors of Factor XI (FXI), preferably FXIa. Also described are pharmaceutical compositions comprising the cyclic peptides and their use in treating conditions, diseases and / or disorders responsive to FXI, preferably FXIa inhibition, including thrombosis or thrombo-inflammatory conditions.

The application discloses a kind of polypeptides based on limulus and its application of antifungal selective modification.The amino acid sequence is as shown in SEQ ID No:1-22,wherein the polypeptide cyclic peptide of the amino acid sequence shown in SEQ ID No:2 forms disulfide bond between 3C and 12C, and the polypeptide of the amino acid sequence shown in SEQ ID No:1-22 is linear peptide.The polypeptide antibacterial agent SEQ ID NO:1-11 of the application minimizes the impact on bacteria while maintaining potent inhibition of fungi, which is conducive to maintaining the balance of microbial community and exhibits great application potential in medical and personal care products.

This invention belongs to the field of biochemistry, specifically relating to the preparation and application of a cyclic peptide. The structure of the cyclic peptide CYP9 is Lys-Gly-Val-dGlu-Gly-Pro-Asp-CONH2, wherein lysine at position 1 and aspartic acid at position 7 are cyclically linked by an amide bond. This invention investigates the biological activity of the cyclic peptide CYP9, including constructing in vitro cell models and in vivo animal models of pulmonary fibrosis to evaluate its in vitro antifibrotic activity and in vivo therapeutic effects, as well as studying its cytotoxicity, serum stability, and pharmacokinetics. The results show that, compared with the parent peptide YD, the cyclic peptide CYP9 obtained in this invention exhibits superior activity and stability in all aspects, and can be used to prepare drugs for the prevention of pulmonary fibrosis.

Described herein in various embodiments are compositions comprising (a) a cyclic peptide; and (b) an antisense compound, wherein the antisense compound targets exon 44 of the DMD gene in a pre-mRNA sequence.

The present invention provides a cyclic peptide compound optionally linked to a nucleic acid, the cyclic peptide compound having a cyclic moiety wherein: (1) the cyclic moiety is composed of 13 or 14 amino acid residues; (2) among the amino acid residues constituting the cyclic moiety, the number of N-substituted amino acid residues is 7 or more, the number of amino acid residues in a single side chain is 3 or fewer, and the number of native amino acid residues is 4 or fewer; and (3) the ClogP / total amide bond (ClogP / total AB) is 1.0 to 1.8.