Palmer S, Wakelam M J
Molecular Pharmacology Group, Institute of Biochemistry, University of Glasgow, U.K.
Biochem J. 1989 Jun 1;260(2):593-6. doi: 10.1042/bj2600593.
Adrenocortical microsomes possess a single population of Ins(1,4,5)P3-specific binding sites [IC50 5.9 +/- 0.9 nM; Palmer, Hughes, Lee & Wakelam (1988) Cell. Signalling 1, 147-156]. Competition studies showed that Ins(1:2-cyclic,4,5)P3 exhibits a 21-fold lower affinity for the site than Ins(1,4,5)P3 (IC50 124 +/- 16 nM). The affinity of the binding sites for Ins(1,4,5)P3 was not influenced by the non-hydrolysable GTP analogues GTP gamma S and Gpp[NH]p or by preincubation of the binding protein with a preparation of partially purified protein kinase C in the presence of ATP and TPA (12-O-tetradecanoylphorbol 13-acetate). These observations are discussed with reference to the identify and function of the Ins(1,4,5)P3 binding site.
肾上腺皮质微粒体具有单一群体的肌醇-1,4,5-三磷酸(Ins(1,4,5)P3)特异性结合位点[半数抑制浓度(IC50)为5.9±0.9纳摩尔;帕尔默、休斯、李和韦克莱姆(1988年)《细胞信号传导》1, 147 - 156]。竞争研究表明,肌醇-1,2-环化,4,5-三磷酸(Ins(1:2-cyclic,4,5)P3)对该位点的亲和力比Ins(1,4,5)P3低21倍(IC50为124±16纳摩尔)。Ins(1,4,5)P3结合位点对Ins(1,4,5)P3的亲和力不受不可水解的鸟苷三磷酸(GTP)类似物鸟苷-5'-O-(3-硫代三磷酸)(GTPγS)和鸟苷-5'-O-(2-氨基)三磷酸(Gpp[NH]p)的影响,也不受在三磷酸腺苷(ATP)和12-O-十四酰佛波醇-13-乙酸酯(TPA)存在下,将结合蛋白与部分纯化的蛋白激酶C制剂预孵育的影响。结合肌醇-1,4,5-三磷酸(Ins(1,4,5)P3)结合位点的特性和功能对这些观察结果进行了讨论。