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Curr Protoc Pharmacol. 2012 Mar;Chapter 2:Unit2.8. doi: 10.1002/0471141755.ph0208s56.

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

Author information

1
Department 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.

PMID:
22382998
PMCID:
PMC3306263
DOI:
10.1002/0471141755.ph0208s56
[Indexed for MEDLINE]
Free PMC Article

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