评估“G蛋白信号调节剂”（RGS）蛋白的调节剂。
Evaluating modulators of "Regulator of G-protein Signaling" (RGS) proteins.
作者信息
Bosch Dustin E, Zielinski Thomas, Lowery Robert G, Siderovski David P
机构信息
Department of Pharmacology, The University of North Carolina at Chapel Hill, Chapel Hill, North Carolina.
出版信息
Curr Protoc Pharmacol. 2012 Mar;Chapter 2:Unit2.8. doi: 10.1002/0471141755.ph0208s56.
Abstract
"Regulator of G-protein Signaling" (RGS) proteins constitute a class of intracellular signaling regulators that accelerate GTP hydrolysis by heterotrimeric Gα subunits. In recent years, RGS proteins have emerged as potential drug targets for modulation by small molecules. Described in this unit are high-throughput screening procedures for identifying modulators of RGS protein-mediated GTPase acceleration (GAP activity), for assessment of RGS domain/Gα interactions (most avid in vitro when Gα is bound by aluminum tetrafluoride), and for validation of candidate GAP-modulatory molecules with the single-turnover GTP hydrolysis assay.
摘要
“G蛋白信号调节因子”（RGS）蛋白构成一类细胞内信号调节因子，可加速异源三聚体Gα亚基的GTP水解。近年来，RGS蛋白已成为小分子调节的潜在药物靶点。本单元介绍了高通量筛选程序，用于鉴定RGS蛋白介导的GTP酶加速（GAP活性）的调节剂、评估RGS结构域/Gα相互作用（当Gα与四氟化铝结合时，在体外最强烈），以及通过单周转GTP水解试验验证候选GAP调节分子。
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