Article
SCH529074, a small molecule activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquitination of wild type p53.
The Journal of biological chemistry - 2 Apr 2010
Demma Mark, Maxwell Eugene, Ramos Robert, Liang Lianzhu, Li Cheng, Hesk David, Rossman Randall, Mallams Alan, Doll Ronald, Liu Ming, Seidel-Dugan Cynthia, Bishop W Robert, Dasmahapatra Bimalendu
Abstract excerpt
Abrogation of p53 function occurs in almost all human cancers, with more than 50% of cancers harboring inactivating mutations in p53 itself. Mutation of p53 is indicative of highly aggressive cancers and poor prognosis. The vast majority of mutations in p53 occur in its core DNA binding domain (D...
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