PAK'n it in: identification of a selective PAK inhibitor

Chem Biol. 2008 Apr;15(4):305-6. doi: 10.1016/j.chembiol.2008.03.011.

Abstract

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).

Publication types

  • Comment

MeSH terms

  • Animals
  • Disulfides / chemistry
  • Disulfides / metabolism
  • Disulfides / pharmacology
  • Drug Evaluation, Preclinical / methods*
  • Enzyme Activation / drug effects
  • Homeostasis / drug effects
  • Mice
  • Protein Conformation / drug effects
  • Protein Kinase Inhibitors / metabolism*
  • Protein Kinase Inhibitors / pharmacology*
  • Substrate Specificity
  • p21-Activated Kinases / antagonists & inhibitors*
  • p21-Activated Kinases / metabolism*

Substances

  • Disulfides
  • Protein Kinase Inhibitors
  • p21-Activated Kinases