Researchers characterized an inhibitor of KRAS, a cellular signaling enzyme whose mutations drive a range of cancers; the inhibitor, BI-2852, bound with high affinity to both active and inactive forms of KRAS in a shallow pocket of the protein that was thought to be undruggable, and reduced proliferation of cells with mutant KRAS in lab assays, paving the way toward development of potent and specific RAS inhibitors for cancer treatment, according to the authors.
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Article #19-04529: "Drugging an undruggable pocket on KRAS," by Dirk Kessler et al.
MEDIA CONTACT: Darryl Benjamin McConnell, Boehringer Ingelheim, Vienna, AUSTRIA; e-mail: darryl.mcconnell@boehringer-ingelheim.com
Proceedings of the National Academy of Sciences