Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor
Abstract
KRASG12C was recently identified to be potentially druggable by allele-specific covalent targeting of Cys-12 in vicinity to an inducible allosteric switch II pocket (S-IIP). Success of this approach requires active cycling of KRASG12C between its active-GTP and inactive-GDP conformations as accessibility of the S-IIP is restricted only to the GDP-bound state. This strategy proved feasible for inhibiting mutant KRAS in vitro; however, it is...
Paper Details
Title
Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor
Published Date
Jan 1, 2018
Journal
Volume
172
Issue
3
Pages
578 - 589.e17
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Notes
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