Article
Small molecule induced reactivation of mutant p53 in cancer cells.
Nucleic acids research - 1 Jul 2013
Liu Xiangrui, Wilcken Rainer, Joerger Andreas C, Chuckowree Irina S, Amin Jahangir, Spencer John, Fersht Alan R
Abstract excerpt
The p53 cancer mutant Y220C is an excellent paradigm for rescuing the function of conformationally unstable p53 mutants because it has a unique surface crevice that can be targeted by small-molecule stabilizers. Here, we have identified a compound, PK7088, which is active in vitro: PK7088 bound to the mutant with a dissociation constant of 140 μM and raised its melting temperature, and we have determined the...
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