A hot spot for protein kinase inhibitor sensitivity.
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.
Bishop
Anthony C
AC
Amherst College, Department of Chemistry, Amherst, MA 01002 USA.
D000970:Antineoplastic Agents / Q000737:chemistry*; D015195:Drug Design; D006801:Humans; D009154:Mutation; D040081:Protein Array Analysis; D047428:Protein Kinase Inhibitors / Q000737:chemistry*; D019061:src-Family Kinases / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000235:genetics
D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D019061:src-Family Kinases