Ontology highlight
ABSTRACT:
SUBMITTER: Maurer T
PROVIDER: S-EPMC3325706 | biostudies-literature | 2012 Apr
REPOSITORIES: biostudies-literature
Maurer Till T Garrenton Lindsay S LS Oh Angela A Pitts Keith K Anderson Daniel J DJ Skelton Nicholas J NJ Fauber Benjamin P BP Pan Borlan B Malek Shiva S Stokoe David D Ludlam Mary J C MJ Bowman Krista K KK Wu Jiansheng J Giannetti Anthony M AM Starovasnik Melissa A MA Mellman Ira I Jackson Peter K PK Rudolph Joachim J Wang Weiru W Fang Guowei G
Proceedings of the National Academy of Sciences of the United States of America 20120319 14
The Ras gene is frequently mutated in cancer, and mutant Ras drives tumorigenesis. Although Ras is a central oncogene, small molecules that bind to Ras in a well-defined manner and exert inhibitory effects have not been uncovered to date. Through an NMR-based fragment screen, we identified a group of small molecules that all bind to a common site on Ras. High-resolution cocrystal structures delineated a unique ligand-binding pocket on the Ras protein that is adjacent to the switch I/II regions a ...[more]