Ontology highlight
ABSTRACT:
SUBMITTER: Liu X
PROVIDER: S-EPMC3695503 | biostudies-literature | 2013 Jul
REPOSITORIES: biostudies-literature
Liu Xiangrui X Wilcken Rainer R Joerger Andreas C AC Chuckowree Irina S IS Amin Jahangir J Spencer John J Fersht Alan R AR
Nucleic acids research 20130429 12
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 binding mode of a close structural analogue by X-ray crystallography. We showed that PK7 ...[more]