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The tumor protein p53 (Y220C mutant) is a mutated form of the p53 tumor suppressor protein. The Y220C mutation, where tyrosine at position 220 is replaced by cysteine, destabilizes the protein and creates a unique druggable pocket. This loss-of-function mutation impairs p53's ability to bind DNA and activate genes involved in cell cycle arrest and apoptosis, promoting cancer development. It's found in approximately 1-1.8% of cancers. Therapeutic strategies focus on stabilizing the mutant protein with small molecules like H3 compound and Rezatapopt to restore its wild-type function.
Small molecule stabilization of mutant p53 conformation; restoration of wild-type p53 function
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