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1-(5-异喹啉磺酰基)-2-甲基哌嗪(H-7)是兔血小板中蛋白激酶C的选择性抑制剂。

1-(5-Isoquinolinesulfonyl)-2-methylpiperazine (H-7) is a selective inhibitor of protein kinase C in rabbit platelets.

作者信息

Kawamoto S, Hidaka H

出版信息

Biochem Biophys Res Commun. 1984 Nov 30;125(1):258-64. doi: 10.1016/s0006-291x(84)80362-9.

Abstract

Effects of 1-(5-isoquinolinesulfonyl)-2-methylpeperazine (H-7), a potent inhibitor of protein kinase C in vitro (1), were investigated with regard to stimulus-induced protein phosphorylation of rabbit platelets. While H-7 inhibited the protein kinase C-mediated phosphorylation in 12-0-tetradecanoylphorbol-13-acetate (TPA)-stimulated platelets, this compound did not block the Ca2+-calmodulin-dependent phosphorylation in Ca2+ ionophore A23187-stimulated cells. This selective inhibitor of protein kinase C, in intact cells, will facilitate studies on the biological functions of protein kinase C.

摘要

就刺激诱导的兔血小板蛋白磷酸化而言,研究了1-(5-异喹啉磺酰基)-2-甲基哌嗪(H-7,一种体外蛋白激酶C的有效抑制剂(1))的作用。虽然H-7抑制了12-O-十四烷酰佛波醇-13-乙酸酯(TPA)刺激的血小板中蛋白激酶C介导的磷酸化,但该化合物并未阻断钙离子载体A23187刺激的细胞中Ca2+ -钙调蛋白依赖性磷酸化。这种蛋白激酶C的选择性抑制剂在完整细胞中,将有助于对蛋白激酶C生物学功能的研究。

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