Evaluating modulators of "Regulator of G-protein Signaling" (RGS) proteins

• Published in: Current protocols in pharmacology Vol. Chapter 2; p. Unit2.8
• Main Authors: Bosch, Dustin E, Zielinski, Thomas, Lowery, Robert G, Siderovski, David P
• Format: Journal Article
• Language: English
• Published: United States 01.03.2012
• Subjects: Biological Assay - methods; Chromatography, Liquid - methods; Fluorescence Resonance Energy Transfer - methods; Fluorescent Dyes; GTP-Binding Protein alpha Subunits - isolation & purification; GTP-Binding Protein alpha Subunits - metabolism; GTP-Binding Proteins - drug effects; GTP-Binding Proteins - metabolism; GTPase-Activating Proteins - metabolism; Hydrolysis; RGS Proteins - drug effects; RGS Proteins - metabolism; Signal Transduction - drug effects; Signal Transduction - physiology
• ISSN: 1934-8290
• DOI: 10.1002/0471141755.ph0208s56

"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.