61 results about "Peptide inhibitor" patented technology

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.

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 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.

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.

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.

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).

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 present invention relates to methods for preparing crystalline forms of a monocyclic peptide compound, or salts or solvates thereof, which is a peptide inhibitor of the interleukin-23 receptor (IL-23R). The crystalline forms are useful in pharmaceutical compositions, methods and / or uses for treatment of autoimmune inflammation diseases and related disorders.

The present invention relates to a pharmaceutical composition containing a polypeptide inhibitor and a use of the pharmaceutical composition. The composition has good stability and drug dissolution rate; the product has controllable quality; and a preparation method has simple process, strong operability, good reproducibility, and is suitable for large-scale industrial production.

The problem to be solved by the present invention is to provide an extract of bacteria of the genus Sphingomonas, which may be used as an inhibitor of the kallikrein-kinin system and can reduce the occurrence of redness.SOLUTION: The present invention relates to an extract of bacteria of the genus Sphingomonas, to a composition comprising at least one bacterium of the genus Sphingomonas or said extract, to the uses thereof and to the implementation thereof in a cosmetic method.SELECTED DRAWING: None

The present invention relates to: a peptide inhibitor, which targets FOXO4-p53 interactions, for removing senescent cells; and a use thereof. The peptide inhibitor according to the present invention is designed on the basis of a p53 transactivation domain (TAD) sequence, thus exhibiting strong selectivity for senescent cells, has a synthesis cost due to being short and having an L-type amino acid configuration, and has the effect of efficiently interfering with FOXO4-p53 interactions despite being short and having an L-type amino acid configuration. Therefore, the peptide inhibitor according to the present invention is expected to be widely used in various health / medical fields requiring the removal of senescent cells.

Provided herein are synthetic peptide inhibitors of fibrinolysis, pharmaceutical compositions comprising at least one of the presently disclosed peptides, or a pharmaceutically acceptable salt thereof, and uses thereof.

Peptide inhibitors of STING, pharmaceutical formulations containing these inhibitors, and methods of using them to treat STING associated diseases are presented.

Disclosed are multi-peptide compositions and / or methods of use of the multi-peptide compositions for subjects suffering from or at risk for a neural disease. Pharmaceutically acceptable embodiments administered subjects may treat or prevent the neural disease. In certain embodiments, a flavonoid compound is administered in conjunction with a peptide. In still other embodiments, a porosome complex is administered with the peptide and / or with the flavonoid compound.

Disclosed are compositions and methods for engineered peptide inhibitors of NLRP3 infiammasome and methods of their use in the treatment of Myelodysplastic Syndromes. In one aspect, disclosed herein are engineered inhibitors of NACHT, LRR and PYD domains-containing protein 3 (NLRP3) inflammasome comprising a Helix 2 of POP1 comprising one or more substitutions at residues 18, 21, 22, 25, 26, 28, 29, and / or 30 of POP1 as set forth in SEQ ID NO:1.

This invention relates to a peptide inhibitor targeting the SDC4-HS complex and its application, belonging to the field of biomedical technology. It addresses one of the problems in existing technologies regarding inaccurate early diagnosis of MASLD, poor efficacy and safety of therapeutic drugs, and the lack of specific peptide inhibitors targeting the SDC4-HS complex. This invention provides a peptide inhibitor targeting the SDC4-HS complex, comprising a WYGP sequence, the amino acid sequence of which is shown in SEQ ID NO. 1 of the sequence listing. This invention provides a specific peptide inhibitor targeting the SDC4-HS complex, capable of blocking key pathogenic pathways of MASLD, achieving safe and efficient treatment and early intervention for fatty liver.

The present invention belongs to the field of pharmaceutical formulations, and particularly relates to a pharmaceutical composition or pharmaceutical formulation formulated in single-dose form. The pharmaceutical composition or pharmaceutical formulation comprises an active ingredient M and a pharmaceutically acceptable excipient. The active ingredient M is selected from a cyclic peptide compound, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, or a dimer thereof, wherein the peptide compound has an amino acid sequence represented by formula (I): Xa1-Xa2-Xa3-Xa4-Xa5-Xa6-Xa7-Xa8-Xa9-Xa10-Xa11-Xa12-Xa13 (I). The pharmaceutical composition or pharmaceutical formulation comprises 1 mg to 1000 mg of the active ingredient M, on the basis of the content of a free base form. The present invention also relates to use of the pharmaceutical composition or pharmaceutical formulation in the preparation of a drug for preventing and treating a disease or disorder overexpressing IL-23 in diseased tissue of a subject.

The present invention relates to a peptide inhibitor of the interleukin-23 receptor and the use thereof. Specifically, the present invention relates to a peptide inhibitor of the interleukin-23 receptor, a stereoisomer or pharmaceutically acceptable salt or solvate thereof, a pharmaceutical composition thereof, 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 provides novel peptide inhibitors of the interleukin-23 receptor, and related compositions and methods of using these peptide inhibitors to treat or prevent a variety of diseases and disorders, including inflammatory bowel diseases.

The present invention relates to a peptide of 5 to 20 amino acids in size, preferably of 7 to 15 amino acids in size, wherein the peptide is (i) a fragment of an amino acid sequence NQGNQPQCRCLPGFLGDRCQYRQCSGYCEN (SEQ ID NO:1), said fragment comprising at least 5 consecutive amino acids of SEQ ID NO:1, or (ii) a functional variant of said fragment, preferably deriving from said fragment by deletion, insertion, and / or substitution of one or more amino acids, wherein the fragment or functional variant derived therefrom includes at least one of the amino acid R9, G16, D17, R18, C19, Q20, and Y21 of SEQ ID NO:1, and to its use as medicament or in diagnostic.

A PCSK9 cyclic peptide inhibitor or a stereoisomer, a racemate, or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a use thereof. Compound (I) disclosed herein has good PCSK9 inhibitory activity and can be used for treating diseases such as hyperlipidemia.