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星形孢菌素是一种有效的蛋白激酶C抑制剂,在分离的小鼠表皮细胞中,它无法抑制12 - O -十四烷酰佛波醇-13 -乙酸酯诱导的鸟氨酸脱羧酶。

Staurosporine, a potent protein kinase C inhibitor, fails to inhibit 12-O-tetradecanoylphorbol-13-acetate-caused ornithine decarboxylase induction in isolated mouse epidermal cells.

作者信息

Kiyoto I, Yamamoto S, Aizu E, Kato R

机构信息

Department of Pharmacology, School of Medicine, Keio University, Tokyo, Japan.

出版信息

Biochem Biophys Res Commun. 1987 Oct 29;148(2):740-6. doi: 10.1016/0006-291x(87)90938-7.

Abstract

Staurosporine, a most potent protein kinase C inhibitor, actually inhibited protein kinase C activity obtained either from cytosol or particulate fraction of mouse epidermis. Staurosporine at the concentrations which exert protein kinase C inhibition, however, failed to inhibit, but markedly augmented 12-O-tetradecanoylphorbol-13-acetate (TPA)-caused ornithine decarboxylase (ODC) induction in isolated mouse epidermal cells. Staurosporine by itself induced ODC activity as TPA does. Mechanism of ODC induction seems different between these two compounds. Another protein kinase C inhibitor, H-7, inhibited both staurosporine- and TPA-caused ODC induction.

摘要

星形孢菌素是一种极其有效的蛋白激酶C抑制剂,它实际上能够抑制从小鼠表皮的胞质溶胶或微粒部分获得的蛋白激酶C活性。然而,在能够发挥蛋白激酶C抑制作用的浓度下,星形孢菌素未能抑制,反而显著增强了12-O-十四烷酰佛波醇-13-乙酸酯(TPA)在分离的小鼠表皮细胞中引起的鸟氨酸脱羧酶(ODC)诱导作用。星形孢菌素自身能像TPA一样诱导ODC活性。这两种化合物诱导ODC的机制似乎有所不同。另一种蛋白激酶C抑制剂H-7,能抑制星形孢菌素和TPA引起的ODC诱导作用。

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