A sharper instrument for dissecting signalling events: a specific AGC kinase inhibitor.
Small-molecule inhibitors are now widely used to try to dissect regulatory signalling events. Many of these interfere with the function of protein kinases, often as part of signalling cascades. In addition to their utility as tools for the researcher, the long-term aspiration is that certain of these compounds may be useful as therapeutic agents for the treatment of conditions that arise from the dysregulation of specific signalling pathways. In this issue of the Biochemical Journal, Sapkota and colleagues report the identification and initial validation of a compound that inhibits the RSK (p90 ribosomal S6 kinase) group of protein kinases, which are members of an important family of kinases (the 'AGC kinases') that have overlapping specificities.
Proud
Christopher G
CG
Department of Biochemistry and Molecular Biology, Life Sciences Institute, University of British Columbia, 2350 Health Sciences Mall, Vancouver, BC, Canada V6T 1Z3. cgpr@interchange.ubc.ca
D002460:Cell Line; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D015894:Genome, Human; D006801:Humans; D020929:Mitogen-Activated Protein Kinase Kinases / Q000037:antagonists & inhibitors*; D009154:Mutation; D044345:Phosphoric Triester Hydrolases / Q000037:antagonists & inhibitors*; D010768:Phosphoserine / Q000378:metabolism; D010769:Phosphothreonine / Q000378:metabolism; D011494:Protein Kinases / Q000378:metabolism; D038744:Ribosomal Protein S6 Kinases, 90-kDa / Q000037:antagonists & inhibitors* / Q000235:genetics; D015398:Signal Transduction; D058570:TOR Serine-Threonine Kinases
D004791:Enzyme Inhibitors; D010769:Phosphothreonine; D010768:Phosphoserine; D011494:Protein Kinases; C546842:MTOR protein, human; D038744:Ribosomal Protein S6 Kinases, 90-kDa; D058570:TOR Serine-Threonine Kinases; C116919:mitogen and stress-activated protein kinase 1; D020929:Mitogen-Activated Protein Kinase Kinases; D044345:Phosphoric Triester Hydrolases