Wassman, Christopher D. published the artcileComputational identification of a transiently open L1/S3 pocket for reactivation of mutant p53, Product Details of C8H9NO4, the main research area is binding pocket loop1 sheet3 pocket reactivation protein p53; stictic acid reactivation p53 protein osteocarcinoma antitumor.
The tumor suppressor p53 is the most frequently mutated gene in human cancer. Reactivation of mutant p53 by small mols. is an exciting potential cancer therapy. Although several compounds restore wild-type function to mutant p53, their binding sites and mechanisms of action are elusive. Here computational methods identify a transiently open binding pocket between loop L1 and sheet S3 of the p53 core domain. Mutation of residue Cys124, located at the center of the pocket, abolishes p53 reactivation of mutant R175H by PRIMA-1, a known reactivation compound Ensemble-based virtual screening against this newly revealed pocket selects stictic acid as a potential p53 reactivation compound In human osteosarcoma cells, stictic acid exhibits dose-dependent reactivation of p21 expression for mutant R175H more strongly than does PRIMA-1. These results indicate the L1/S3 pocket as a target for pharmaceutical reactivation of p53 mutants.
Nature Communications published new progress about Animal gene, TP53 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 72835-26-8 belongs to class esters-buliding-blocks, name is (2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)methyl propionate, and the molecular formula is C8H9NO4, Product Details of C8H9NO4.
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