Ontology highlight
ABSTRACT:
SUBMITTER: Shin Y
PROVIDER: S-EPMC6746093 | biostudies-literature | 2019 Sep
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20190820 9
KRAS regulates many cellular processes including proliferation, survival, and differentiation. Point mutants of KRAS have long been known to be molecular drivers of cancer. <i>KRAS p.G12C</i>, which occurs in approximately 14% of lung adenocarcinomas, 3-5% of colorectal cancers, and low levels in other solid tumors, represents an attractive therapeutic target for covalent inhibitors. Herein, we disclose the discovery of a class of novel, potent, and selective covalent inhibitors of KRAS<sup>G12C ...[more]