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Updated: May 24, 2026

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
Published on: June 9, 2017
Evaluating modulators of "Regulator of G-protein Signaling" (RGS) proteins
Dustin E Bosch1, Thomas Zielinski, Robert G Lowery
1Department of Pharmacology, The University of North Carolina at Chapel Hill, Chapel Hill, North Carolina.
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.
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