Polypeptide, its derivative and its application in the preparation of drugs for preventing and treating tumors

A technology of derivatives and peptides, applied in the direction of antineoplastic drugs, drug combinations, peptides containing positioning/targeting motifs, etc., can solve the problems of complex signaling pathway regulation mechanism, slow and lack of drug development process, etc.
CN110498850BActive Publication Date: 2021-04-09胡卓伟
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
胡卓伟
Publication Date
2021-04-09

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Abstract

The invention discloses a polypeptide specifically binding to β-catenin, which is a TRIB3 mutant whose amino acid sequence is substituted, deleted or added with one or several amino acids and has TRIB3 activity. Also disclosed is a derivative of the polypeptide, which is a chimeric peptide formed by linking the polypeptide with a membrane-penetrating peptide. The invention discloses an anti-tumor pharmaceutical composition containing the polypeptide or polypeptide derivative as an active ingredient. Also disclosed are applications of the polypeptides, polypeptide derivatives and pharmaceutical compositions in the preparation of drugs for preventing and / or treating diseases related to TRIB3 and β-catenin, especially tumors. The pharmaceutical composition has the ability to specifically bind to β-catenin, block the binding of TRIB3 and β-catenin protein, and reduce the protein level of TRIB3. The prepared medicine has the advantages of remarkable curative effect, less toxic and side effects and safe use.
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Description

technical field

[0001] The invention belongs to the field of biotechnology, and specifically relates to polypeptides, their derivatives and their application in the preparation of drugs for preventing and treating tumors. Background technique

[0002] The Wnt / β-catenin signaling pathway is abnormally activated in a variety of tumors (colon cancer, liver cancer, lung cancer, pancreatic cancer, glioma and breast cancer). , tumor drug resistance and maintenance of tumor stemness and other aspects play a role in promoting. As the effector molecule of this signaling pathway, β-catenin is usually phosphorylated by its degradation complex members Axin-2, APC, and GSK-3β, and then enters the ubiquitination pathway for degradation. When Wnt signaling is abnormally activated, the members of its degradation complex disintegrate, and the β-catenin accumulated in the cytoplasm will translocate into the nucleus and form a transcription complex with the LEF / TCF family, which jointly promo...

Claims

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