Article
Activating p53Y220C with a mutant-specific small molecule.
Nature communications - 2 May 2026
Zhu Xijun, Byun Woong Sub, Pieńkowska Dominika Ewa, Nguyen Kha The, Wang Mengxiong, Nettles Sabin A, Gourisankar Sai, Phillips Nick A, Gerhartz Jan, Geng Qixiang, Qiu Tian, Zhong Jianing, Jiang Zixuan, Sarott Roman C, Hinshaw Stephen M, Zhang Tinghu, Attardi Laura D, Nowak Radosław P, Gray Nathanael S
Abstract excerpt
TP53 is the most commonly mutated gene in cancer, but it remains recalcitrant to clinically meaningful therapeutic reactivation. We present here the discovery and characterization of a small molecule chemical inducer of proximity that activates mutant p53. We named this compound TRanscriptional Activator of p53 (TRAP-1) due to its ability to engage p53Y220C and BRD4 in a ternary complex, which potently activates...
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