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Salvation of the fallen angel: Reactivating mutant p53
Author(s) -
Li Yang,
Wang Zhuoyi,
Chen Yuchen,
Petersen Robert B.,
Zheng Ling,
Huang Kun
Publication year - 2019
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.14572
Subject(s) - mutant , suppressor , biology , loss function , transcription factor , mutation , nucleic acid , gain of function , cancer research , function (biology) , genome , computational biology , genetics , microbiology and biotechnology , gene , phenotype
The transcription factor p53 is known as the guardian of the genome for its powerful anti‐tumour capacity. However, mutations of p53 that undermine their protein structure, resulting in loss of tumour suppressor function and gain of oncogenic function, have been implicated in more than half of human cancers. The crucial role of mutant forms of p53 in cancer makes it an attractive therapeutic target. A large number of candidates, including low MW compounds, peptides, and nucleic acids, have been identified or designed to rescue p53 mutants and reactivate their anti‐tumour capacity through a variety of mechanisms. In this review, we summarize the progress made in the reactivation of mutant forms of p53, focusing on the pharmacological mechanisms of the reactivators of p53 mutants.