Fluorescent and photoactive probes for the study of protein kinase C.
A fluorescent diacylglycerol, 2-(12-N-dansylaminododecanoyl)-1-myristoyl-sn-glycerol (dansyl-DAG) and a photoactive diacylglycerol, 2-(12-[N-(4-azido-2-nitrophenyl)] aminododecanoyl)-1-myristoyl-sn-glycerol (azido-DAG) have been synthesized. Both have been shown to bind to protein kinase C by inhibition of phorbol dibutyrate binding. Dansyl-DAG was able to activate protein kinase C at low calcium concentrations. Stimulation of neutrophils with dansyl-DAG resulted in a large release of superoxide radicals from the cells. The physicochemical properties of dansyl-DAG and azido-DAG may allow one to label and follow specifically changes in the location of protein kinase C and to understand some aspects of its function and regulation.
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Azzi
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D000345:Affinity Labels / Q000138:chemical synthesis*; D000818:Animals; D001386:Azides / Q000138:chemical synthesis* / Q000494:pharmacology; D001921:Brain / Q000201:enzymology; D002417:Cattle; D004075:Diglycerides / Q000138:chemical synthesis* / Q000494:pharmacology; D005989:Glycerides / Q000138:chemical synthesis*; D007700:Kinetics; D015240:Phorbol 12,13-Dibutyrate; D010703:Phorbol Esters / Q000378:metabolism; D011485:Protein Binding; D011493:Protein Kinase C / Q000378:metabolism*
D000345:Affinity Labels; D001386:Azides; D004075:Diglycerides; D005989:Glycerides; D010703:Phorbol Esters; C051331:2-(12-N-dansylaminododecanoyl)-1-myristoylglycerol; C051332:2-(12-(N-(4-azido-2-nitrophenyl))aminododecanoyl)-1-myristoylglycerol; D015240:Phorbol 12,13-Dibutyrate; D011493:Protein Kinase C