Article
Toward the rational design of p53-stabilizing drugs: probing the surface of the oncogenic Y220C mutant.
Chemistry & biology - 29 Jan 2010
Basse Nicolas, Kaar Joel L, Settanni Giovanni, Joerger Andreas C, Rutherford Trevor J, Fersht Alan R
Abstract excerpt
The p53 cancer mutation Y220C induces formation of a cavity on the protein's surface that can accommodate stabilizing small molecules. We combined fragment screening and molecular dynamics to assess the druggability of p53-Y220C and map ligand interaction sites within the mutational cavity. Eluci...
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