Article
Inhibition of Nonfunctional Ras.
Cell chemical biology - 18 Feb 2021
Nussinov Ruth, Jang Hyunbum, Gursoy Attila, Keskin Ozlem, Gaponenko Vadim
Abstract excerpt
Intuitively, functional states should be targeted; not nonfunctional ones. So why could drugging the inactive K-Ras4BG12Cwork-but drugging the inactive kinase will likely not? The reason is the distinct oncogenic mechanisms. Kinase driver mutations work by stabilizing the active state and/or destabilizing the inactive state. Either way, oncogenic kinases are mostly in the active state. Ras driver mutations work...
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