Inhibition of casein kinase II by heparin
Casein kinase II, a cyclic nucleotide-independent protein kinase from rabbit reticulocytes, was shown to be inhibited by heparin. Heparin specifically inhibited the enzyme and had no effect on other protein kinases, including casein kinase I, the type I and II cAMP-dependent protein kinases, proteas...
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Veröffentlicht in: | The Journal of biological chemistry 1980-09, Vol.255 (17), p.8038-8041 |
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Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | Casein kinase II, a cyclic nucleotide-independent protein kinase from rabbit reticulocytes, was shown to be inhibited by heparin.
Heparin specifically inhibited the enzyme and had no effect on other protein kinases, including casein kinase I, the type
I and II cAMP-dependent protein kinases, protease-activated kinase I, and the hemin-controlled repressor. Heparan sulfate
was found to be 40-fold less effective than heparin towards casein kinase II; other acid mucopolysaccharides had little or
no effect on the enzymatic activity. Steady state studies revealed that heparin acted as a competitive inhibitor with respect
to the substrate, casein. A value of 20 ng/ml or about 1.4 nM was obtained for the apparent Ki. The inhibition was not reversed
by ATP and varying the ATP and heparin concentrations in the assay only altered the maximum velocity. |
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ISSN: | 0021-9258 1083-351X |
DOI: | 10.1016/S0021-9258(19)70601-2 |