Unit

UNIT 2.8 Evaluating Modulators of “Regulator of G-protein Signaling” (RGS) Proteins

  1. Dustin E. Bosch1,2,
  2. Thomas Zielinski3,
  3. Robert G. Lowery3,
  4. David P. Siderovski1,2

Published Online: 1 MAR 2012

DOI: 10.1002/0471141755.ph0208s56

Current Protocols in Pharmacology

Current Protocols in Pharmacology

How to Cite

Bosch, D. E., Zielinski, T., Lowery, R. G. and Siderovski, D. P. 2012. Evaluating Modulators of “Regulator of G-protein Signaling” (RGS) Proteins. Current Protocols in Pharmacology. 56:2.8:2.8.1–2.8.15.

Author Information

  1. 1

    Department of Pharmacology, The University of North Carolina at Chapel Hill, Chapel Hill, North Carolina

  2. 2

    UNC Neuroscience Center and Lineberger Comprehensive Cancer Center, The University of North Carolina at Chapel Hill, Chapel Hill, North Carolina

  3. 3

    BellBrook Labs, Madison, Wisconsin

Publication History

  1. Published Online: 1 MAR 2012
  2. Published Print: MAR 2012

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. Curr. Protoc. Pharmacol. 56:2.8.1-2.8.15. © 2012 by John Wiley & Sons, Inc.

Keywords:

  • regulator of G-protein signaling (RGS) proteins;
  • heterotrimeric G-protein α subunits;
  • Förster resonance energy transfer (FRET);
  • single-turnover GTP hydrolysis;
  • fluorescence polarization (FP)