KS-619-1, a new inhibitor of Ca2+ and calmodulin-dependent cyclic nucleotide phosphodiesterase from Streptomyces californicus.

1 January 1987

journal article
research article
Published by Japan Antibiotics Research Association in The Journal of Antibiotics

Vol. 40 (8) , 1104-1110
https://doi.org/10.7164/antibiotics.40.1104

Abstract

KS-619-1, a new inhibitor of Ca2+ and calmodulin-dependent cyclic nucleotide phosphodiesterase, was isolated from the cultured broth of Streptomyces californicus. KS-619-1 has an anthraquinone moiety. IC50 values for the effect of KS-619-1 on Ca2+ and calmodulin-stimulated activity of bovine brain and heart enzymes were 2.0 and 1.5 .mu.M, respectively. On the other hand, basal activity (the activity in the presence of ethylene bis(oxyethylenenitrilo)-tetraacetic acid (EGTA) instead of Ca2+/calmodulin) of the bovine brain enzyme, calmodulin-independent cyclic nucleotide phosphodiesterase from bovine heart, and protein kinase C from rat brain were inhibited by KS-619-1 to a lesser extent with IC50 values; 12.3, 25.9 and 151 .mu.M, respectively.

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