PAK'n it in: identification of a selective PAK inhibitor.
p21-activated kinases are important signaling kinases for which no specific chemical inhibitors are known. In this issue of Chemistry & Biology, Deacon et al. target allosteric transitions undergone during PAK activation to identify a selective inhibitor (Deacon et al., 2008).
Bokoch
Gary M
GM
Departments of Immunology and Cell Biology, The Scripps Research Institute, La Jolla, CA 92037, USA. bokoch@scripps.edu
D000818:Animals; D004220:Disulfides / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D004789:Enzyme Activation / Q000187:drug effects; D006706:Homeostasis / Q000187:drug effects; D051379:Mice; D011487:Protein Conformation / Q000187:drug effects; D047428:Protein Kinase Inhibitors / Q000378:metabolism* / Q000494:pharmacology*; D013379:Substrate Specificity; D054462:p21-Activated Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism*
D004220:Disulfides; D047428:Protein Kinase Inhibitors; D054462:p21-Activated Kinases