Article
The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors.
Nature structural & molecular biology - 1 Jun 2018
Hansen Rasmus, Peters Ulf, Babbar Anjali, Chen Yuching, Feng Jun, Janes Matthew R, Li Lian-Sheng, Ren Pingda, Liu Yi, Zarrinkar Patrick P
Abstract excerpt
Activating mutations in KRAS are among the most common tumor driver mutations. Until recently, KRAS had been considered undruggable with small molecules; the discovery of the covalent KRASG12C inhibitors ARS-853 and ARS-1620 has demonstrated that it is feasible to inhibit KRAS with high potency in cells and animals. Although the biological activity of these inhibitors has been described, the biochemical mechanism...
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