Article
KRAS G12C Drug Development: Discrimination between Switch II Pocket Configurations Using Hydrogen/Deuterium-Exchange Mass Spectrometry.
Structure (London, England : 1993) - 5 Sept 2017
Lu Jia, Harrison Rane A, Li Lianbo, Zeng Mei, Gondi Sudershan, Scott David, Gray Nathanael S, Engen John R, Westover Kenneth D
Abstract excerpt
KRAS G12C, the most common RAS mutation found in non-small-cell lung cancer, has been the subject of multiple recent covalent small-molecule inhibitor campaigns including efforts directed at the guanine nucleotide pocket and separate work focused on an inducible pocket adjacent to the switch motifs. Multiple conformations of switch II have been observed, suggesting that switch II pocket (SIIP) binders may be...
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