前列腺素E1和福斯高林可拮抗人血小板中的C激酶激活。
Prostaglandin E1 and forskolin antagonize C-kinase activation in the human platelet.
作者信息
de Chaffoy de Courcelles D, Roevens P, Van Belle H
机构信息
Department of Biochemistry, Janssen Pharmaceutica, Beerse, Belgium.
出版信息
Biochem J. 1987 May 15;244(1):93-9. doi: 10.1042/bj2440093.
Abstract
In human platelets, prostaglandin E1 and forskolin inhibit 5-hydroxytryptamine-induced phospholipase C, C-kinase and myosin light-chain kinase activity in a concentration-dependent way. Phospholipase C activation, however, was only partly inhibited, and this at higher concentrations than the protein kinases. Direct activation of the C kinase either by exogenous synthetic diacylglycerol or by 12-O-tetradecanoylphorbol 13-acetate was antagonized by prostaglandin E1 and forskolin. Since C-kinase activation is one of the key events in excitatory signal transduction in the platelets, we suggest that the inhibitory effect of agents that increase platelet cyclic AMP on platelet secretion and aggregation might reside in their capacity to antagonize C-kinase activity.
摘要
在人血小板中，前列腺素E1和福斯高林以浓度依赖的方式抑制5-羟色胺诱导的磷脂酶C、C激酶和肌球蛋白轻链激酶活性。然而，磷脂酶C的激活仅受到部分抑制，且所需浓度高于蛋白激酶。前列腺素E1和福斯高林可拮抗外源性合成二酰甘油或12-O-十四烷酰佛波醇-13-乙酸酯对C激酶的直接激活。由于C激酶激活是血小板兴奋性信号转导中的关键事件之一，我们认为增加血小板环磷酸腺苷的药物对血小板分泌和聚集的抑制作用可能在于其拮抗C激酶活性的能力。
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