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Polypeptide specifically combined with beta-catenin protein with high affinity, and application and synthesis method of polypeptide

A synthesis method and affinity technology, applied in the direction of peptide/protein components, medical preparations containing active ingredients, peptides, etc., can solve the problem of lack of polypeptide β-catenin and BCL9, achieve the induction of cell self-apoptosis, and mass production Potential, the effect of great potential for clinical transformation of drugs

Active Publication Date: 2020-11-10
THE FIRST AFFILIATED HOSPITAL OF MEDICAL COLLEGE OF XIAN JIAOTONG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] There is no development of β-catenin and BCL9 inhibitors in the prior art, and there is no similar polypeptide that can inhibit the combination of β-catenin and BCL9, so the development of β-catenin and BCL9 inhibitors has great significance in cancer treatment. potential

Method used

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  • Polypeptide specifically combined with beta-catenin protein with high affinity, and application and synthesis method of polypeptide
  • Polypeptide specifically combined with beta-catenin protein with high affinity, and application and synthesis method of polypeptide
  • Polypeptide specifically combined with beta-catenin protein with high affinity, and application and synthesis method of polypeptide

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Embodiment Construction

[0019] The present invention will be described in detail below with reference to the drawings and specific embodiments.

[0020] The present invention discloses a polypeptide with high affinity and specific binding to β-catenin protein. The amino acid sequence of the polypeptide is LEHRERSLQT(X1)RDIQRML(X2)P, wherein X1 is leucine (L), norleucine (NLE). ) Or homoleucine (HLE); X2 is phenylalanine (F), 1-naphthylalanine (1-NAL), 2-naphthylalanine (2-NAL), 2-anthracene Alanine (2-Anla) or 9-anthrylalanine (9-Anla).

[0021] The invention also discloses the application of a polypeptide that specifically binds to β-catenin protein with high affinity for inhibiting the growth of cancer cells, specifically for inhibiting the β-catenin / Wnt signal pathway of cancer cells, inhibiting tumor growth, and inducing cells Self-apoptosis, more specifically, is used to inhibit the binding of β-catenin and BCL9 in cancer cells, thereby inhibiting the β-catenin / Wnt signaling pathway.

[0022] The inv...

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Abstract

The invention discloses a polypeptide specifically combined with beta-catenin protein with high affinity, and application and a synthesis method of the polypeptide. The amino acid sequence of the polypeptide is LEHRERSLQT(X1)RDIQRML(X2)P, wherein X1 is leucine, norleucine or homoleucine, and X2 is phenylalanine, 1-naphthyl alanine, 2-naphthyl alanine, 2-anthryl alanine or 9-anthryl alanine. The polypeptide is used for inhibiting growth of cancer cells. By the polypeptide, various tumor treatment targets can be achieved. The polypeptide inhibits opening of a beta-catenin protein-mediated Wnt signal pathway by inhibiting mutual combination of the beta-catenin protein and BCL9 in the cancer cells, so that growth of tumors is inhibited, self-apoptosis of the cells is induced, and the tumor disease treatment targets are achieved. The synthesis method of the polypeptide is simple and easy to implement, and the final product has high yield efficiency, has mass production potential, and has great drug clinical transformation potential.

Description

Technical field [0001] The present invention belongs to the fields of medicinal chemistry and peptide chemistry, and particularly relates to a peptide with high affinity and specific binding to β-catenin protein, and its application and synthesis method. Background technique [0002] Malignant tumors have become one of the main diseases that are increasingly common and threaten human life and quality of life. Primary hepatic carcinoma (Primary hepatic carcinoma) is a malignant tumor caused by abnormal proliferation of hepatocytes. It is highly malignant and progresses rapidly, with a poor prognosis, and is often life-threatening. Its mortality rate ranks fifth among malignant tumors in my country. Colorectal cancer and liver cancer are all gastrointestinal tumors, both of which are among the top 10 malignant tumors in my country. It can be seen that gastrointestinal tumors closely related to diet have seriously threatened the health of Chinese residents. At present, the clinical...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08A61K38/10A61P35/00
CPCC07K7/08A61P35/00A61K38/00
Inventor 何旺骁闫瑾
Owner THE FIRST AFFILIATED HOSPITAL OF MEDICAL COLLEGE OF XIAN JIAOTONG UNIV
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