A Hot Spot for Protein Kinase Inhibitor Sensitivity Review Article

ATP binding site-directed protein kinase inhibitors are potent weapons in the war on cancer. However, specific mutations at an inhibitor-sensitivity “hot spot” can render these molecules ineffective. In this issue of Chemistry & Biology, Daub and coworkers have used an array of known kinase inhibitors to systematically characterize the desensitizing effects of hot spot mutations .