An Isoform-Selective, Small-Molecule Inhibitor Targets the Autoregulatory Mechanism of p21-Activated Kinase

Autoregulatory domains found within kinases may provide more unique targets for chemical inhibitors than the conserved ATP-binding pocket targeted by most inhibitors. The kinase Pak1 contains an autoinhibitory domain that suppresses the catalytic activity of its kinase domain. Pak1 activators reliev...

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Veröffentlicht in:	Chemistry & biology 2008-04, Vol.15 (4), p.322-331
Hauptverfasser:	Deacon, Sean W., Beeser, Alexander, Fukui, Jami A., Rennefahrt, Ulrike E.E., Myers, Cynthia, Chernoff, Jonathan, Peterson, Jeffrey R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals CHEMBIO Disulfides - chemistry Disulfides - metabolism Disulfides - pharmacology Drug Evaluation, Preclinical - methods Enzyme Activation - drug effects Fibroblasts - drug effects Fibroblasts - metabolism Homeostasis - drug effects Isoenzymes - antagonists & inhibitors Isoenzymes - metabolism Mice Naphthols - chemistry Naphthols - metabolism Naphthols - pharmacology p21-Activated Kinases - antagonists & inhibitors p21-Activated Kinases - metabolism Platelet-Derived Growth Factor - metabolism Protein Conformation - drug effects Protein Kinase Inhibitors - metabolism Protein Kinase Inhibitors - pharmacology SIGNALING Small Molecule Libraries - metabolism Small Molecule Libraries - pharmacology Substrate Specificity
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