Synthetic peptides based on the calmodulin-binding domain of myosin light chain kinase inhibit activation of other calmodulin-dependent enzymes.
Nanomolar concentrations of synthetic peptides corresponding to the calmodulin-binding domain of skeletal muscle myosin light chain kinase were found to inhibit calmodulin activation of seven well-characterized calmodulin-dependent enzymes: brain 61 kDa cyclic nucleotide phosphodiesterase, brain adenylate cyclase, Bordetella pertussis adenylate cyclase, red blood cell membrane Ca++-pump ATPase, brain calmodulin-dependent protein phosphatase (calcineurin), skeletal muscle phosphorylase b kinase, and brain multifunctional Ca++ (calmodulin)-dependent protein kinase. Inhibition could be entirely overcome by the addition of excess calmodulin. Thus, the myosin light chain kinase peptides used in this study may be useful antagonists for studying calmodulin-dependent enzymes and processes.
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors; D000067956:Adenylyl Cyclase Inhibitors; D000818:Animals; D001665:Binding Sites; D001886:Bordetella pertussis / Q000201:enzymology; D001921:Brain / Q000201:enzymology; D019703:Calcineurin; D000252:Calcium-Transporting ATPases / Q000037:antagonists & inhibitors; D002147:Calmodulin / Q000378:metabolism* / Q000494:pharmacology; D002148:Calmodulin-Binding Proteins / Q000037:antagonists & inhibitors; D002417:Cattle; D054677:Cyclic Nucleotide Phosphodiesterases, Type 1; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors; D004910:Erythrocyte Membrane / Q000201:enzymology; D006801:Humans; D009132:Muscles / Q000201:enzymology; D009219:Myosin-Light-Chain Kinase / Q000378:metabolism*; D010446:Peptide Fragments / Q000494:pharmacology*; D010749:Phosphoprotein Phosphatases / Q000037:antagonists & inhibitors; D010764:Phosphorylase Kinase / Q000037:antagonists & inhibitors; D047428:Protein Kinase Inhibitors; D011817:Rabbits; D051381:Rats
D000067956:Adenylyl Cyclase Inhibitors; D002147:Calmodulin; D002148:Calmodulin-Binding Proteins; D004791:Enzyme Inhibitors; D010446:Peptide Fragments; D047428:Protein Kinase Inhibitors; D010764:Phosphorylase Kinase; D009219:Myosin-Light-Chain Kinase; D019703:Calcineurin; D010749:Phosphoprotein Phosphatases; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054677:Cyclic Nucleotide Phosphodiesterases, Type 1; D000252:Calcium-Transporting ATPases