Targeting codon 158 p53-mutant cancers via the induction of p53 acetylation

通过诱导 p53 乙酰化来靶向 158 个密码子 p53 突变癌症

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作者:Li Ren Kong, Richard Weijie Ong, Tuan Zea Tan, Nur Afiqah Binte Mohamed Salleh, Matan Thangavelu, Jane Vin Chan, Lie Yong Judice Koh, Giridharan Periyasamy, Jieying Amelia Lau, Thi Bich Uyen Le, Lingzhi Wang, Miyoung Lee, Srinivasaraghavan Kannan, Chandra S Verma, Chwee Ming Lim, Wee Joo Chng, David

Abstract

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 mutp53R158G could render cancers susceptible to cisplatin-induced DNA stress. Acetylation of mutp53R158G alters DNA binding motifs and upregulates TRAIP, a RING domain-containing E3 ubiquitin ligase which dephosphorylates IĸB and impedes nuclear translocation of RelA (p65), thus repressing oncogenic nuclear factor kappa-B (NF-ĸB) signaling and inducing apoptosis. Given that this mechanism of cytotoxic vulnerability appears inapt in p53 wild-type (WT) or other hotspot GOF mutp53 cells, our work provides a therapeutic opportunity specific to Arg158-mutp53 tumors utilizing a regimen consisting of DNA-damaging agents and mutp53 acetylators, which is currently being pursued clinically.

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