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Evaluation of protein kinase inhibitors in an assay system containing multiple protein kinase activities
1Department of Bioactive Molecules, National Institute of Health, Tokyo, Japan.
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.