Article
Targeting the p53 cancer mutants Y220C, Y220N, and Y220S with the small-molecule stabilizer rezatapopt.
Cell death & disease - 26 Feb 2026
Mavridi Danai, Funk Julianne S, Balourdas Dimitrios-Ilias, Krämer Andreas, Khan Tareque Raysa, Timofeev Oleg, Spencer John, Stiewe Thorsten, Joerger Andreas C
Abstract excerpt
The cavity-creating p53 cancer mutation Y220C, which accounts for an estimated 125,000 new cancer cases per year, serves as an excellent paradigm for the development of mutant p53 reactivators. Several molecules that reactivate this thermolabile cancer mutant by targeting the mutation-induced crevice have been developed, and one of them, rezatapopt, is currently in clinical trials. The less frequently occurring...
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