Article
Construction of Small-Molecule Deubiquitinase-Targeting Chimeras to Reactivate and Stabilize Mutant p53 Y220C in Vitro and in Vivo.
Angewandte Chemie (International ed. in English) - 16 Jan 2026
He Chen, Li Junda, Cui Chenxi, Xie Jia, Feng Jiajie, Zhang Baixue, Huang Xingting, Ma Ruoping, Zheng Lufeng, Xu Jinyi, Yao Hong, Xu Shengtao
Abstract excerpt
Wild-type p53 is a tumor suppressor protein that is crucial in various pathological processes. The predominant strategy for p53 Y220C mutant involves binding reactivators to mutation-induced pocket to stabilize the protein thermally and restore wild-type structure. However, the corrected p53 Y220C remains vulnerable to ubiquitination, reducing protein levels and impairing function. Herein, we report the...
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