Evaluating modulators of "Regulator of G-protein Signaling" (RGS) proteins.
Evaluating modulators of "Regulator of G-protein Signaling" (RGS) proteins.
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DOI：
10.1002/0471141755.ph0208s56
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发表时间：
2012-03-01
影响因子：
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通讯作者：
Siderovski, David P
中科院分区：
文献类型：
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作者：
Bosch, Dustin E;Zielinski, Thomas;Siderovski, David P
“G蛋白信号调节剂”（RGS）蛋白构成一类细胞内信号调节剂，其通过异源三聚体Ga亚基加速GTP水解。近年来，RGS蛋白已成为小分子调节的潜在药物靶点。本单元描述了高通量筛选程序，用于鉴定RGS蛋白介导的GTP酶促反应（GAP活性）的调节剂，用于评估RGS结构域/Ga相互作用（当Ga与四氟化铝结合时，在体外最活跃），以及用于用单周转GTP水解试验验证候选GAP调节分子。
"Regulator of G-protein Signaling" (RGS) proteins constitute a class of intracellular signaling regulators that accelerate GTP hydrolysis by heterotrimeric Galpha 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/Galpha interactions (most avid in vitro when Galpha is bound by aluminum tetrafluoride), and for validation of candidate GAP-modulatory molecules with the single-turnover GTP hydrolysis assay.