Compound for promoting apoptosis of human cancer cells and application thereof

A compound and cancer cell technology, applied in the field of compounds, can solve problems affecting the function of p53 protein, and achieve the effect of increasing transcription activity and promoting apoptosis

Inactive Publication Date: 2017-05-31
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to existing statistics, 50% of human cancers have point mutations in p53, which affects the function of p53 protein

Method used

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  • Compound for promoting apoptosis of human cancer cells and application thereof
  • Compound for promoting apoptosis of human cancer cells and application thereof
  • Compound for promoting apoptosis of human cancer cells and application thereof

Examples

Experimental program
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Embodiment Construction

[0036] The present invention will be further described below in conjunction with drawings and embodiments.

[0037] Embodiments of the present invention are as follows:

[0038] 1) Construct the recombinant GST-p53 protein and mark it with GST tag:

[0039] a) The RNA of MCF-7 cells (a breast cancer cell, p53 protein is wild-type) was extracted by Trizol method, and then the RNA was reversed to single-stranded by PrimeScriptTMII 1st Strand cDNA Synthesis Kit (TAKRA, Dalian Baosheng Biology) DNA, and using this single-stranded DNA as a template, amplify the human wild-type p53 gene by PCR, and then use the Fast Mutagenesis System (Transgen, Beijing Quanshijin Biotechnology Co., Ltd.) kit to obtain the 175-position arginine (R) mutant p53 gene mutated to histidine (H), 220 tyrosine mutated to cysteine ​​(C), wild-type and mutant p53 gene sequences were verified by sequencing;

[0040] b) the wild-type p53 gene and the mutant p53 gene obtained in step a) are both digested with ...

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Abstract

The invention discloses a compound for promoting apoptosis of human cancer cells and application thereof. The compound is named 2-(4-hydroxyanilino)phenol; and after being combined with human p53 protein, the compound is capable of restoring the configuration of which the mutant p53 protein is a wild type, enhancing the transcription activity of the p53 protein, and causing apoptosis of cancer cells, thereby inhibiting the cell reproduction. The compound can be combined with the human p53 protein, and can induce the apoptosis of cancer cells by changing the transcription activity of the mutant p53 protein in cancer cells, thereby providing a new idea for subsequent treatment of cancers.

Description

technical field [0001] The invention relates to a compound, a compound for promoting cancer cell apoptosis and application thereof. The compound can induce cancer cell apoptosis by changing the transcription activity of mutated p53 protein in cancer cells. Background technique [0002] As a transcription factor, p53 protein is the guardian of the genome. When the genome is damaged, the transcriptional activity of p53 protein will be activated, thereby causing cell cycle arrest and cell apoptosis. According to existing statistics, point mutations have occurred in p53 in 50% of human cancers, thereby affecting the function of p53 protein. And it has been reported in relevant literature that the restoration of the activity of the mutated p53 protein can significantly prevent the occurrence and development of cancer. [0003] The screening of traditional p53 protein activators is mostly at the cell level, by constructing p53 protein-deficient cell lines, and then screening comp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C215/76A61K31/137A61P35/00
CPCC07C215/76
Inventor 章晓波许晨曦
Owner ZHEJIANG UNIV
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