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蛋白激酶C的新型抑制剂K252a在佛波酯刺激的血小板中可同时抑制40K蛋白磷酸化和5-羟色胺分泌。

K252a, a new inhibitor of protein kinase C, concomitantly inhibits 40K protein phosphorylation and serotonin secretion in a phorbol ester-stimulated platelets.

作者信息

Yamada K, Iwahashi K, Kase H

出版信息

Biochem Biophys Res Commun. 1987 Apr 14;144(1):35-40. doi: 10.1016/s0006-291x(87)80471-0.

DOI:10.1016/s0006-291x(87)80471-0
PMID:3579911
Abstract

K252a isolated from microbial origin was found to potently inhibit protein kinase C in vitro (1). This agent inhibits phosphorylation of 40,000 dalton protein (40K protein) induced by 12-0-tetradecanoylphorbol-13-acetate(TPA) in intact rabbit platelets. This indicates that K252a exhibits the inhibition of protein kinase C in intact cells. The serotonin secretion induced by TPA was inhibited by K252a at nearly equal concentrations required to inhibit the phosphorylation of 40K protein. This provides the evidence to support the cause-effect relationship between the protein phosphorylation and the secretion in TPA-stimulated platelets.

摘要

从微生物中分离出的K252a在体外被发现能有效抑制蛋白激酶C(1)。该药物能抑制12-0-十四烷酰佛波醇-13-乙酸酯(TPA)诱导的完整兔血小板中40000道尔顿蛋白(40K蛋白)的磷酸化。这表明K252a在完整细胞中表现出对蛋白激酶C的抑制作用。TPA诱导的5-羟色胺分泌被K252a抑制,其浓度与抑制40K蛋白磷酸化所需的浓度几乎相等。这为支持TPA刺激的血小板中蛋白磷酸化与分泌之间的因果关系提供了证据。

相似文献

1
K252a, a new inhibitor of protein kinase C, concomitantly inhibits 40K protein phosphorylation and serotonin secretion in a phorbol ester-stimulated platelets.蛋白激酶C的新型抑制剂K252a在佛波酯刺激的血小板中可同时抑制40K蛋白磷酸化和5-羟色胺分泌。
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2
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