Competitive binding assay for drugs that interfere with calmodulin function.
A direct 125I-calmodulin-binding system utilizing a particulate cytoskeletal preparation of the neuronal calmodulin-dependent protein kinase type II provides a simple, rapid filtration-based method for assessing anti-calmodulin drug activity. The binding assay avoids potential artifacts due to direct drug effects on the standard phosphodiesterase enzyme assay while obtaining comparable IC50 values for a spectrum of drugs. It also provides a tool to probe mechanisms of action of putative anticalmodulin agents which may help elucidate selective pharmacologic modifications of pathophysiological processes.
D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000201:enzymology; D002147:Calmodulin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D003599:Cytoskeleton / Q000201:enzymology; D066298:In Vitro Techniques; D007700:Kinetics; D009474:Neurons / Q000201:enzymology; D011494:Protein Kinases / Q000378:metabolism; D051381:Rats; D014268:Trifluoperazine / Q000378:metabolism / Q000494:pharmacology
D002147:Calmodulin; D014268:Trifluoperazine; D011494:Protein Kinases