钙泊三醇C（UCN - 1028C）是一种新型微生物化合物，是蛋白激酶C的高效特异性抑制剂。

Calphostin C (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C.

作者信息

Kobayashi E, Nakano H, Morimoto M, Tamaoki T

机构信息

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

出版信息

Biochem Biophys Res Commun. 1989 Mar 15;159(2):548-53. doi: 10.1016/0006-291x(89)90028-4.

DOI:10.1016/0006-291x(89)90028-4

PMID:2467670

Abstract

Calphostin C (UCN-1028C), a newly isolated compound from Cladosporium cladosporioides, is a potent and specific inhibitor of protein kinase C, because it was 1000 times more inhibitory to protein kinase C (IC50, 0.05 microM) than other protein kinases such as cAMP-dependent protein kinase and tyrosine-specific protein kinase (IC50, greater than 50 microM). Calphostin C did not inhibit calcium activated neutral protease (calpain)-digested protein kinase C, indicating that it interacts with the regulatory domain of protein kinase C. In addition this compound showed inhibitory effects on the binding of [3H]PDBu to protein kinase C. The potent cytotoxic activity and antitumor activity of calphostin C might be due to the inhibition of protein kinase C, and thus it may be potentially useful for the therapeutic application.

摘要

卡尔佛斯汀C（UCN - 1028C）是一种从枝孢霉菌新分离出的化合物，是蛋白激酶C的一种强效特异性抑制剂，因为它对蛋白激酶C的抑制作用（IC50，0.05微摩尔）比其他蛋白激酶如环磷酸腺苷依赖性蛋白激酶和酪氨酸特异性蛋白激酶（IC50，大于50微摩尔）强1000倍。卡尔佛斯汀C不抑制钙激活中性蛋白酶（钙蛋白酶）消化的蛋白激酶C，表明它与蛋白激酶C的调节结构域相互作用。此外，该化合物对[3H]佛波醇-12，13-二丁酸酯与蛋白激酶C的结合表现出抑制作用。卡尔佛斯汀C的强细胞毒性活性和抗肿瘤活性可能归因于对蛋白激酶C的抑制，因此它可能在治疗应用中具有潜在用途。