title: Evaluation of protein kinase inhibitors in an assay system containing multiple protein kinase activities.
abstract: Specificities of several known protein kinase inhibitors were evaluated using an assay system in which activities of protein kinase A, protein kinase C, protein tyrosine kinase and calmodulin-dependent protein kinase III were simultaneously detected. Inhibitory spectra of H-89, K252a, H-7, staurosporine, tyrphostin and herbimycin A observed in the assay system were similar to those reported in the purified protein kinase assay systems. It was also found that KN-62 selectively inhibited calmodulin-dependent protein kinase III activity. These data suggest that the assay system may be effective and practicable in evaluating specificities and screening of new protein kinase inhibitors.
authors.affiliation: Department of Bioactive Molecules, National Institute of Health, Tokyo, Japan.
authors.forename: P M
authors.initials: PM
authors.lastname: Li
authors.forename: H
authors.initials: H
authors.lastname: Fukazawa
authors.forename: S
authors.initials: S
authors.lastname: Mizuno
authors.forename: Y
authors.initials: Y
authors.lastname: Uehara
mesh_terms: D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / Q000031:analogs & derivatives; D016475:3T3 Cells; D000470:Alkaloids / Q000494:pharmacology; D000818:Animals; D016227:Benzoquinones; D017871:Calcium-Calmodulin-Dependent Protein Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism; D002227:Carbazoles / Q000494:pharmacology; D002396:Catechols / Q000494:pharmacology; D002461:Cell Line, Transformed; D000242:Cyclic AMP / Q000494:pharmacology; D017868:Cyclic AMP-Dependent Protein Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D004533:Egtazic Acid / Q000494:pharmacology; D016391:Genes, src; D026121:Indole Alkaloids; D007546:Isoquinolines / Q000494:pharmacology; D047029:Lactams, Macrocyclic; D051379:Mice; D009570:Nitriles / Q000494:pharmacology; D010879:Piperazines / Q000494:pharmacology; D011493:Protein Kinase C / Q000037:antagonists & inhibitors / Q000378:metabolism; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases / Q000378:metabolism*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism; D011809:Quinones / Q000494:pharmacology; D017828:Rifabutin / Q000031:analogs & derivatives; D019311:Staurosporine; D013449:Sulfonamides; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology; D020032:Tyrphostins
chemical_list: D000470:Alkaloids; D016227:Benzoquinones; D002227:Carbazoles; D002396:Catechols; D026121:Indole Alkaloids; D007546:Isoquinolines; D047029:Lactams, Macrocyclic; D009570:Nitriles; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D011809:Quinones; D013449:Sulfonamides; D020032:Tyrphostins; C060152:tyrphostin 47; D017828:Rifabutin; D004533:Egtazic Acid; C063302:KN 62; C020754:herbimycin; D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; C049985:staurosporine aglycone; D000242:Cyclic AMP; D011494:Protein Kinases; D011505:Protein-Tyrosine Kinases; D017868:Cyclic AMP-Dependent Protein Kinases; D011493:Protein Kinase C; D017871:Calcium-Calmodulin-Dependent Protein Kinases; D019311:Staurosporine; C063509:N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide; D013755:Tetradecanoylphorbol Acetate