Having validated BRAF as a possible therapeutic target, we proceeded to the biochemical characterization of a new BRAF inhibitor, Vemurafenib, in order to confirm the shRNA results with a pharmacologic approach that is more applicable from a clinical standpoint. Vemurafenib is a highly selective inhibitor of BRAF kinase activity, with an IC50 of 44 nmol/L against V600E-mutant BRAF. From a panel of 65 non-RAF kinases covering much of the kinome, only one kinase—BRK (also known as PTK6)...
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