Ontology highlight
ABSTRACT:
SUBMITTER: Zhao Q
PROVIDER: S-EPMC10630485 | biostudies-literature | 2023 Nov
REPOSITORIES: biostudies-literature
Zhao Qingci Q Haga Ryoka R Tamura Satoko S Shimada Ichio I Nishida Noritaka N
Scientific reports 20231107 1
KRAS mutations are major drivers of various cancers. Recently, allele-specific inhibitors of the KRAS G12C mutant were developed that covalently modify the thiol of Cys12, thereby trapping KRAS in an inactive GDP-bound state. To study the mechanism of action of the covalent inhibitors in both in vitro and intracellular environments, we used real-time NMR to simultaneously observe GTP hydrolysis and inhibitor binding. In vitro NMR experiments showed that the rate constant of ARS-853 modification ...[more]