Pelech S L, Meier K E, Krebs E G
Biochemistry. 1986 Dec 30;25(26):8348-53. doi: 10.1021/bi00374a002.
The Ca2+/phosphatidylserine-stimulated protein kinase C (PKC) appears to exist as interconvertible inactive, soluble and active, membrane-bound forms. Changes in the bimodal distribution of PKC induced by diacylglycerol or tumor-promoting phorbol esters have been proposed to regulate the activity of this kinase [Nishizuka, Y. (1984) Nature (London) 308, 693-698]. A rapid microassay for assessment of protein kinase C translocation between cytosol and membranes was developed. This procedure, which relied on the selective digitonin-mediated release of cytoplasmic proteins, eliminated potential homogenization and fractionation artifacts. PKC activity toward histone H1 was determined after limited trypsinolysis, which abolished the Ca2+/phospholipid requirement of the enzyme and prevented interference by inhibitory proteins. Complete translocation of PKC to the membrane fraction and subsequent down-regulation of the kinase in response to 12-O-tetradecanoylphorbol-13-acetate treatment of Swiss 3T3 cells could be demonstrated by this method. Platelet-derived growth factor, insulin-like growth factor 1, vasopressin, and prostaglandin F2 alpha facilitated partial conversions of PKC to the membrane-bound form in quiescent 3T3 cells.
钙离子/磷脂酰丝氨酸刺激的蛋白激酶C(PKC)似乎以可相互转化的无活性、可溶性形式和活性、膜结合形式存在。二酰基甘油或促肿瘤佛波酯诱导的PKC双峰分布变化被认为可调节该激酶的活性[Nishizuka, Y. (1984) Nature (London) 308, 693 - 698]。开发了一种用于评估蛋白激酶C在细胞质和细胞膜之间转位的快速微量测定法。该方法依赖于洋地黄皂苷介导的细胞质蛋白选择性释放,消除了潜在的匀浆和分级分离假象。在有限的胰蛋白酶消化后测定PKC对组蛋白H1的活性,这消除了该酶对钙离子/磷脂的需求并防止了抑制性蛋白的干扰。通过该方法可以证明,在对瑞士3T3细胞进行12 - O - 十四酰佛波醇 - 13 - 乙酸酯处理后,PKC完全转位至膜部分并随后激酶下调。血小板衍生生长因子、胰岛素样生长因子1、血管加压素和前列腺素F2α促进了静止3T3细胞中PKC向膜结合形式的部分转化。