Article
Targeted rescue of a destabilized mutant of p53 by an in silico screened drug.
Proceedings of the National Academy of Sciences of the United States of America - 29 Jul 2008
Boeckler Frank M, Joerger Andreas C, Jaggi Gaurav, Rutherford Trevor J, Veprintsev Dmitry B, Fersht Alan R
Abstract excerpt
The tumor suppressor p53 is mutationally inactivated in approximately 50% of human cancers. Approximately one-third of the mutations lower the melting temperature of the protein, leading to its rapid denaturation. Small molecules that bind to those mutants and stabilize them could be effective an...
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