G蛋白信号调节（RGS）蛋白赋予G蛋白门控钾通道激动剂依赖性舒张门控作用。
A regulator of G protein signalling (RGS) protein confers agonist-dependent relaxation gating to a G protein-gated K+ channel.
作者信息
Fujita S, Inanobe A, Chachin M, Aizawa Y, Kurachi Y
机构信息
Department of Pharmacology II, Graduate School of Medicine, Osaka University, Suita, Osaka 565-0871, Japan.
出版信息
J Physiol. 2000 Jul 15;526 Pt 2(Pt 2):341-7. doi: 10.1111/j.1469-7793.2000.00341.x.
Abstract
- The effects of RGS4 on the voltage-dependent relaxation of G protein-gated K+ (KG) channels were examined by heterologous expression in Xenopus oocytes. 2. While the relaxation kinetics was unaffected by the acetylcholine concentration ([ACh]) in the absence of RGS4, it became dependent on [ACh] when RGS4 was co-expressed. 3. Kinetic analyses indicated that RGS4 confers to the KG channel a voltage-independent inhibitory gating mechanism, which was attenuated by ACh in a concentration-dependent fashion. 4. In vitro biochemical studies showed that RGS4 could bind to the protein complex containing KG channel subunits. 5. Since the native cardiac KG channel exhibited similar agonist-dependent relaxation kinetics to that mediated by RGS4, it is suggested that KG channel gating is a novel physiological target of RGS protein-mediated regulation.
摘要
- 通过在非洲爪蟾卵母细胞中的异源表达，研究了RGS4对G蛋白门控钾离子（KG）通道电压依赖性松弛的影响。2. 在没有RGS4的情况下，松弛动力学不受乙酰胆碱浓度（[ACh]）的影响，但当共表达RGS4时，它变得依赖于[ACh]。3. 动力学分析表明，RGS4赋予KG通道一种电压非依赖性抑制门控机制，该机制被ACh以浓度依赖性方式减弱。4. 体外生化研究表明，RGS4可以与包含KG通道亚基的蛋白质复合物结合。5. 由于天然心脏KG通道表现出与RGS4介导的类似的激动剂依赖性松弛动力学，因此提示KG通道门控是RGS蛋白介导调节的一个新的生理靶点。
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