Article
Targeting codon 158 p53-mutant cancers via the induction of p53 acetylation.
Nature communications - 29 Apr 2020
Kong Li Ren, Ong Richard Weijie, Tan Tuan Zea, Mohamed Salleh Nur Afiqah Binte, Thangavelu Matan, Chan Jane Vin, Koh Lie Yong Judice, Periyasamy Giridharan, Lau Jieying Amelia, Le Thi Bich Uyen, Wang Lingzhi, Lee Miyoung, Kannan Srinivasaraghavan, Verma Chandra S, Lim Chwee Ming, Chng Wee Joo, Lane David P, Venkitaraman Ashok, Hung Huynh The, Cheok Chit Fang, Goh Boon Cher
Abstract excerpt
Gain of function (GOF) DNA binding domain (DBD) mutations of TP53 upregulate chromatin regulatory genes that promote genome-wide histone methylation and acetylation. Here, we therapeutically exploit the oncogenic GOF mechanisms of p53 codon 158 (Arg158) mutation, a DBD mutant found to be prevalent in lung carcinomas. Using high throughput compound screening and combination analyses, we uncover that acetylating...
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