133 results about "Peptide inhibitor" patented technology

The invention provides an antibacterial peptide cAMP048 sourced from microorganisms in a deep sea environment and application of the antibacterial peptide cAMP048, and belongs to the technical field of peptide inhibitors. The antibacterial peptide cAMP048 has an amino acid sequence as shown in SEQ ID NO: 1 (Sequence Identity Number 1). The antibacterial peptide can inhibit the growth of acinetobacter baumannii at 64 mu M, inhibit the growth of multi-drug-resistant acinetobacter baumannii and multi-drug-resistant enterococcus faecium at 128 mu M and inhibit the growth of escherichia coli, staphylococcus aureus and multi-drug-resistant klebsiella pneumoniae at 256 mu M. The antibacterial peptide can be used for preparing products with antibacterial and / or bactericidal performance, and can be applied to preparation of antibacterial and / or bactericidal products. Such as food, skin care products or medical supplies.

The invention discloses a polypeptide derived from deep sea microorganisms, and belongs to the technical field of peptide inhibitors. The polypeptide has an amino acid sequence as shown in SEQ ID NO: 1; the polypeptide has a bacteriostatic and / or bactericidal function. The polypeptide can inhibit the growth of acinetobacter baumannii at 8 [mu] M and inhibit the growth of escherichia coli and multi-drug-resistant acinetobacter baumannii at 16 [mu] M, and can be used for preparing products with bacteriostatic and / or bactericidal performance, such as food, daily necessities or medical products.

The present disclosure relates to compositions and methods, including Trim / inhibitors that find use in the treatment of disease, such as therapies for cancer, including cancers that are resistant to anti-checkpoint agents, infectious diseases and inflammatory diseases.

The invention provides an antibacterial peptide CN-3 and application thereof, and relates to the technical field of peptide inhibitors. The amino acid sequence of the antibacterial peptide CN-3 is GPGGAWAAKVIS, and is as shown in SEQ ID NO. 1. The minimum inhibitory concentration (MIC) of the antibacterial peptide CN-3 to staphylococcus aureus and escherichia coli is 5.0 mg / mL. According to the antibacterial peptide CN-3 and the application thereof, the CN-3 has staphylococcus aureus and escherichia coli bacteriostatic activity, and plays a role by destroying bacterial cell membranes; cN-3 is not easy to generate drug resistance, low in cytotoxicity and high in cell selectivity, and can be used for preparing an antibacterial composition for treating staphylococcus aureus and escherichia coli infection.

The application discloses a covalent polypeptide inhibitor targeting protein kinase A, a conjugate, a kit, a pharmaceutical composition and application. The general formula of the covalent polypeptide inhibitor is Z1-Seq-Z2; wherein Seq is an amino acid sequence; the C-terminal of Seq comprises a pseudo-substrate recognition motif recognized by protein kinase A, a non-natural amino acid with a covalent reaction group, and can be covalently crosslinked with a Cys200 residue on a catalytic subunit of protein kinase A; Z1 is selected from hydrogen, an acyl group, a fluorescent group, biotin, an isotopic tag or a biological ortho-reaction group; and Z2 is selected from a hydroxyl group, an amino group, a cell-penetrating peptide or a stabilization modification group. The covalent polypeptide inhibitor can strongly and irreversibly inhibit PKA activity, and can be used as an active probe to specifically label active PKA in a complex biological sample, and is used for biological research and drug development.

This disclosure features structurally-stabilized and / or cysteine-reactive peptide inhibitors for selective targeting of BFL-1, or dual targeting of BFL-1 and MCL-1. Also disclosed are methods of using such structurally-stabilized and cysteine-reactive peptides in the treatment of BFL-1- and / or MCL-1-expressing or -dependent cancers or diseases of cellular excess (e.g., autoimmune or inflammatory conditions). Also provided are combination therapies comprising such structurally-stabilized and / or cysteine-reactive peptides and inhibitors of the DNA damage response pathway, such as an ATM kinase inhibitor, ATR kinase inhibitor, CHK1 / 2 inhibitor, or PARP inhibitor; or an inhibitor of MCL-1, or a selective inhibitor of BCL-2, or an inhibitor of BCL-2 / BCL-XL, for the treatment of BFL-1-expressing or -dependent cancers (e.g., AML), BFL-1 and MCL-1-expressing or -dependent cancers, or diseases of cellular excess (e.g., autoimmune or inflammatory conditions).

The inventors discovered that calcitonin gene-related peptide (CGRP) inhibitors reduce pain caused by bone fracture without impeding healing of the fracture. Accordingly, disclosed herein are methods for treating pain in a subject that has sustained a bone fracture, and the methods comprise administering a therapeutically effective amount of a CGRP inhibitor to the subject.

The present disclosure relates to a lipid conjugated bivalent peptide ligand which bind to Protein Interacting with C Kinase – 1 (PICK1) and thereby inhibit PICK1. The PICK1 inhibitors of the present disclosure comprise a peptide portion comprising two peptide ligands of PICK1, and a non-peptide portion comprising a linker, linking the two peptide ligands, and a lipid. The disclosure furthermore relates to therapeutic and diagnostic use of said PICK1 inhibitor for treatment of diseases or disorders associated with maladaptive plasticity.

Provide for herein are cyclic or linear peptides that bind HIV-1 capsid protein and inhibit HIV-1 capsid from assembling and / or disassembling. Further provided are methods of making said peptides and pharmaceutical compositions and methods for treating HIV infection.

The present invention relates to a peptide inhibitor of an interleukin-23 receptor and a use thereof. In particular, the present invention relates to peptide inhibitors of the interleukin-23 receptor, stereoisomers or pharmaceutically acceptable salts or solvates thereof, pharmaceutical compositions thereof, and uses of the peptide inhibitors in the treatment or prevention of diseases or conditions including inflammatory bowel disease, Crohn's disease and psoriasis.

The present invention relates to compounds that are peptide inhibitors of the interleukin-23 receptor (IL-23R) and to their use in the treatment or prevention of a variety of diseases, conditions or disorders, including inflammatory diseases, such as inflammatory bowel disease (e.g. Crohn's disease or ulcerative colitis), psoriasis and psoriatic arthritis. The compound has good physical and chemical stability in the gastrointestinal tract.

Provided herein is a method of decreasing a-syn levels and / or decreasing a-syn toxicity in a cell, the method comprising contacting the cell with a charged multivesicular body protein 2B: a-synuclein (CHMP2B:a-syn) inhibitor and a method of inhibiting neural degeneration, the method comprising administering to a subject in need thereof a charged multivesicular body protein 2B: a-synuclein (CHMP2B:a-syn) inhibitor.

Provided are a novel peptide inhibitor of the interleukin-23 receptor, a stereoisomer or a pharmaceutically acceptable salt or solvate thereof, or a pharmaceutical composition containing the same, and the use of the peptide inhibitor in the treatment or prevention of diseases or conditions including inflammatory bowel disease, Crohn's disease and psoriasis.

The present invention relates to a peptide inhibitor of interleukin-23 receptor, and a use thereof. In particular, it relates to a peptide inhibitor of interleukin-23 receptor, a stereoisomer, pharmaceutically acceptable salt or solvate thereof, a pharmaceutical composition thereof, and a use of the peptide inhibitor in treating or preventing diseases or conditions comprising inflammatory bowel disease, Crohn's disease, and psoriasis.

The present invention relates to a process for preparing a crystalline form of a monocyclic peptide compound, which is a peptide inhibitor of the interleukin-23 receptor (IL-23R), or a salt or solvate thereof. The crystalline forms are pharmaceutical compositions, methods and / or uses for the treatment of autoimmune inflammatory diseases and related conditions.

This disclosure relates to reversible affinity selection methods useful for the isolation and enrichment of covalent peptide inhibitors directly from large synthetic peptide libraries. Also disclosed herein are synthetic peptides for targeting HPV16 E6 and peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 protein.

The present disclosure relates to peptide inhibitors of the interleukin-23 receptor (IL-23R) or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, methods and / or uses for the treatment of autoimmune inflammation and related diseases and disorders.

The present invention provides specific matrix metalloproteinase (MMP) polypeptide inhibitors and uses thereof in treating MMP-related diseases, in particular cancer, such as breast cancer and glioblastoma.

Uncontrolled secretion of extracellular matrix (ECM) proteins such as collagen can lead to excessive scarring and fibrosis and compromise tissue function. Despite the widespread occurrence of fibrotic diseases and scarring, effective therapies are lacking. The invention provides inhibitors of TANGO1 activity and methods of use thereof. In particular, the invention relates to peptide inhibitors capable of preventing TANGO1 heterodimerisation and / or homodimerisation and thereby prevent collagen export from the endoplasmic reticulum. The inhibitors of the invention are particularly useful for use in methods of treating fibrotic diseases, such as scleroderma.

The present disclosure relates to peptide inhibitors of the interleukin-23 receptor (IL-23R) or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, methods and / or uses for treatment of autoimmune inflammation and related diseases and disorders.

The present invention discloses a PTP1B peptide inhibitor, BimBH3-12-F12A, having the following structural formula: #imgabs0#. This peptide mimetic compound is derived from the core 12-peptide of the BimBH3 domain, in which Phe (F) at position 12 is replaced by Ala (A). It is prepared using peptide solid-phase synthesis, and all amino acids in its structure are natural amino acids. The PTP1B peptide inhibitor, BimBH3-12-F12A, has significant PTP1B inhibitory activity and has potential application in the development of drugs for PTP1B-targeted diseases such as diabetes, cancer, and Alzheimer's disease.

The application discloses a polypeptide and application thereof, and belongs to the technical field of peptide inhibitors. The polypeptide has an amino acid sequence as shown in SEQ ID NO:1; the polypeptide has a bacteriostatic and / or bactericidal function. The polypeptide can inhibit the growth of Vibrio parahaemolyticus at 128 muM, can inhibit the growth of Vibrio harveyi, Vibrio alginolyticus and Vibrio anguillarum at 256 muM, and can inhibit the growth of Aeromonas hydrophila at 512 muM, and can be used for preparing products with bacteriostatic and / or bactericidal properties, such as food or aquaculture products.

The invention relates to washing and cleaning agents, in particular, liquid washing and cleaning agents, and particularly preferably liquid textile washing agents, comprising a) at least one protease, preferably in an amount of 0.0001 to 1 wt. %, relative to the total weight of the washing and cleaning agent, b) at least one peptide (peptidic inhibitor), preferably in a 0.5-, 1.0-, 1.5-, 2.0-, 2.5-, 3.0-, 3.5-, 4.0-, 4.5-, 5.0-, 10-, 15-, 18-, 20-, 25-, 27-, or 30-fold molar excess relative to the molarity of the protease used, preferably in a 15-, 18-, 20-, 25-, or 27-fold molar excess, the peptide preferably having a length of 50 to 200, preferably 55 to 190, and more preferably 60 to 180, amino acid functional groups, and c) at least one washing and cleaning agent ingredient, preferably in an amount of 0.01 to 99.9 wt. %, relative to the total weight of the washing and cleaning agent. Also included in the invention are the corresponding washing and cleaning processes, the use of the agents described herein, and the use of a peptidic inhibitor to improve the stability of a protease in washing or cleaning agents.

To provide selective targeting of ubiquitin- and ubiquitin-like E1-activating enzymes by structurally-stabilized peptides.SOLUTION: This disclosure features structurally stabilized and / or warhead-bearing structurally stabilized peptide inhibitors for targeting ubiquitin activating enzymes (E1). Methods of using such structurally stabilized peptides and warhead-bearing structurally stabilized peptides in the treatment of E1-expressing cancers or diseases or E1-dependent cancers or diseases are also disclosed. Combination therapies comprising such structurally stabilized and / or warhead-bearing structurally stabilized peptides for the treatment of E1-expressing diseases or E1-dependent diseases are also provided.SELECTED DRAWING: None

The invention relates to a polypeptide inhibitor as well as a preparation method and application thereof. In particular, the present invention relates to a compound represented by general formula (I), a preparation method thereof, a pharmaceutical composition containing the compound, and a use thereof as an inhibitor in the treatment of a variety of inflammatory, autoimmune diseases and cancers, each substituent in the general formula (I) being as defined in the specification. # imgabs0 #

The present invention relates to a peptide inhibitor for inhibiting activation of TGF-β1 with the participation of TSP-1, or the pharmaceutically acceptable salt, solvate or prodrug thereof, and a pharmaceutical composition comprising the peptide or the pharmaceutically acceptable salt, solvate or prodrug thereof, and a method for treating or preventing TGF-β1 related diseases, in particular fibrosis and solid tumors, by using the peptide inhibitor or the pharmaceutically acceptable salt, solvate or prodrug thereof and the pharmaceutical composition.

Synthetic peptides mimicking the nsp10 sequence in the region interacting with nsp16 capable of penetrating cell membranes and inhibiting SARS-CoV-2 replication for the treatment of moderate to severe COVID-19. The invention relates to peptides inhibiting SARS-CoV-2 replication, likely through inhibition of Methyltransferase complexes (NSP10 / NSP16 and NSP10 / NSP14). The peptide of the present invention, P3, contains sequences corresponding to amino acids 89-96 of the non-structural protein 10 (NSP10) of SARS-CoV-2, with the only Cysteine modified to a Methionine. This peptide was made based on two previous designs P1 and P2, which constituted the amino acids 68-96 of the NSP10 protein of SARS-CoV-2.

The invention relates to a cyclic peptide for inhibiting a drug-resistant bacterium AcrB protein as well as a delivery vector and application of the cyclic peptide. The amino acid sequence of the cyclic peptide comprises any one of sequences as shown in SEQ ID No.1-SEQ ID No.15. The invention discloses a cyclic peptide inhibitor for reversing the drug resistance of antibiotics. The method comprises the following steps: firstly, designing and screening out cyclic peptide capable of forming high affinity with AcrB protein; secondly, the delivery carrier entraps the cyclopeptide to a bacterial membrane to cause membrane disturbance, the cyclopeptide enters the bacterial membrane to be combined with AcrB on an inner membrane to inhibit antibiotic excretion, the sensitivity of bacteria to the antibiotics is enhanced, and the MIC of the antibiotics is reduced.

This disclosure provides peptides which have an affinity for the focal adhesion targeting (FAT) domain of focal adhesion kinase (FAK). In particular, the peptides are modified and derived from the sequence of the LD2 alpha helical domain of paxillin (e.g., LD2 peptides), the LD4 domain of paxillin (e.g., LD4 peptides), and CD8 peptides. These peptides are capable of blocking an interaction between paxillin and FAK, thereby inhibiting FAK activity related to FAK-paxillin interaction. The invention further provides uses for such peptides as therapeutics for the treatment of cancer and other diseases characterized with FAK activity and / or expression (e.g., fibrosis).

Uses of a peptide inhibitor of the interleukin-23 receptor (IL-23R) or a pharmaceutically acceptable salt or solvate form thereof for the treatment of generalized pustular psoriasis or erythrodermic psoriasis are described.