Article

Activating p53 <sup>Y220C</sup> with a Mutant-Specific Small Molecule

2024-10-28

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 TR anscriptional A ctivator of p 53 ( TRAP-1 ) due to its ability to engage mutant p53 and BRD4 in a ternary complex, which potently...

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Literature Corpus work: fd4b0975-ad6b-5e5c-96e5-5e00da653a03
DOI: 10.1101/2024.10.23.619961

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