Article
Progress on Covalent Inhibition of KRAS(G12C).
Cancer discovery - 1 Mar 2016
Westover Kenneth D, Jänne Pasi A, Gray Nathanael S
Abstract excerpt
Recent reports of small-molecule approaches to directly inhibit oncogenic KRAS(G12C) have invigorated the RAS research community by raising the possibility of drugging a protein that was long considered "undruggable." A new iteration of covalent compounds targeting the allosteric switch II pocket of KRAS(G12C) showed improved potency and selectivity and enabled studies demonstrating that KRAS(G12C) rapidly cycles...
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