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K-252b、c和d,源自微生物的蛋白激酶C强效抑制剂。

K-252b, c and d, potent inhibitors of protein kinase C from microbial origin.

作者信息

Nakanishi S, Matsuda Y, Iwahashi K, Kase H

出版信息

J Antibiot (Tokyo). 1986 Aug;39(8):1066-71. doi: 10.7164/antibiotics.39.1066.

Abstract

Nocardiopsis sp. K-290 was found to produce novel metabolites, designated K-252b, c and d, which were structurally related to K-252a. These compounds were isolated from the culture broth and the physico-chemical and biochemical properties were examined. The compounds strongly inhibited protein kinase C. IC50 values (the concentrations causing 50% inhibition) for the effects of K-252b, c and d on the rat brain enzyme were 38.3, 214, and 337 nM, respectively.

摘要

发现诺卡氏菌属菌株K-290能产生与K-252a结构相关的新型代谢产物,命名为K-252b、c和d。这些化合物从培养液中分离出来,并对其理化性质和生化特性进行了检测。这些化合物强烈抑制蛋白激酶C。K-252b、c和d对大鼠脑酶作用的IC50值(引起50%抑制的浓度)分别为38.3、214和337 nM。

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