Article
Revealing the mechanism of action of a first-in-class covalent inhibitor of KRASG12C (ON) and other functional properties of oncogenic KRAS by 31P NMR.
The Journal of biological chemistry - 1 Feb 2024
Sharma Alok K, Pei Jun, Yang Yue, Dyba Marcin, Smith Brian, Rabara Dana, Larsen Erik K, Lightstone Felice C, Esposito Dominic, Stephen Andrew G, Wang Bin, Beltran Pedro J, Wallace Eli, Nissley Dwight V, McCormick Frank, Maciag Anna E
Abstract excerpt
Individual oncogenic KRAS mutants confer distinct differences in biochemical properties and signaling for reasons that are not well understood. KRAS activity is closely coupled to protein dynamics and is regulated through two interconverting conformations: state 1 (inactive, effector binding deficient) and state 2 (active, effector binding enabled). Here, we use 31P NMR to delineate the differences in state 1 and...
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