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新型肿瘤启动子激活钙激活的磷脂依赖性蛋白激酶(蛋白激酶C):远藤菌素和脱溴海兔毒素。

Activation of calcium-activated, phospholipid-dependent protein kinase (protein kinase C) by new classes of tumor promoters: teleocidin and debromoaplysiatoxin.

作者信息

Fujiki H, Tanaka Y, Miyake R, Kikkawa U, Nishizuka Y, Sugimura T

出版信息

Biochem Biophys Res Commun. 1984 Apr 30;120(2):339-43. doi: 10.1016/0006-291x(84)91259-2.

Abstract

The new potent tumor promoters teleocidin and debromoaplysiatoxin , which are structurally unrelated to phorbol esters, activate Ca2+-activated, phospholipid-dependent protein kinase (protein kinase C). The concentrations of 12-O-tetradecanoylphorbol-13-acetate, teleocidin and debromoaplysiatoxin for half-maximum activation of protein kinase C were found to be approximately 3 ng/ml, 40 ng/ml and 400 ng/ml, respectively. These three types of tumor promoters bind to protein kinase C, and appear to exhibit their pleiotropic actions through activation of this enzyme.

摘要

新型强效肿瘤促进剂teleocidin和脱溴海兔毒素在结构上与佛波酯无关,它们可激活Ca2+激活的、磷脂依赖性蛋白激酶(蛋白激酶C)。发现12-O-十四酰佛波醇-13-乙酸酯、teleocidin和脱溴海兔毒素使蛋白激酶C达到半数最大激活浓度分别约为3 ng/ml、40 ng/ml和400 ng/ml。这三种类型的肿瘤促进剂与蛋白激酶C结合,并且似乎通过激活该酶来发挥其多效性作用。

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