TP53:Y220C corrector

A TP53:Y220C corrector is a small molecule therapeutic designed to restore the tumor-suppressive function of the p53 protein in cancers harboring the Y220C mutation. This specific mutation creates a surface pocket that destabilizes the p53 DNA-binding domain, causing the protein to unfold and lose its activity at physiological temperatures. Correctors bind to this mutation-induced pocket, acting as molecular chaperones to stabilize the protein's wild-type conformation and restore its ability to regulate genes involved in apoptosis and cell cycle arrest. Research, such as that presented by Astex Pharmaceuticals, explores the use of these correctors in combination with MDM2 antagonists like ASTX295 to enhance p53 signaling and overcome apoptotic resistance in various malignancies, including pancreatic cancer. PMV Pharmaceuticals is also a major developer in this space with its lead candidate rezatapopt (PC14586).

Other names

p53 Y220C correctorp-53 Y220C correctorp 53 Y220C correctorp53 Y220C stabilizerp-53 Y220C stabilizerp 53 Y220C stabilizerp53-Y220C correctorp-53-Y220C correctorp 53-Y220C correctorp53 Y220C chaperonep-53 Y220C chaperonep 53 Y220C chaperone