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KS - 619 - 1，一种来自加利福尼亚链霉菌的新型钙和钙调蛋白依赖性环核苷酸磷酸二酯酶抑制剂。

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

作者信息

Matsuda Y, Kase H

机构信息

Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan.

出版信息

J Antibiot (Tokyo). 1987 Aug;40(8):1104-10. doi: 10.7164/antibiotics.40.1104.

DOI:10.7164/antibiotics.40.1104
PMID:3680022
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 microM, 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 microM, respectively.

摘要

KS - 619 - 1是一种新型的钙和钙调蛋白依赖性环核苷酸磷酸二酯酶抑制剂，从加利福尼亚链霉菌的培养液中分离得到。KS - 619 - 1含有蒽醌部分。KS - 619 - 1对牛脑和心脏酶的钙和钙调蛋白刺激活性的IC50值分别为2.0和1.5微摩尔。另一方面，牛脑酶的基础活性（在存在乙二醇双(氧乙烯腈)四乙酸(EGTA)而非Ca2+/钙调蛋白的情况下的活性）、牛心脏的钙调蛋白非依赖性环核苷酸磷酸二酯酶以及大鼠脑的蛋白激酶C被KS - 619 - 1抑制的程度较小，IC50值分别为12.3、25.9和151微摩尔。

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