Evaluating modulators of "regulator of G-protein signaling" (RGS) proteins

Dustin E. Bosch, Thomas Zielinski, Robert G. Lowery, David P. Siderovski

Research output: Contribution to journalArticlepeer-review

10 Scopus citations


"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-turnoverGTP hydrolysis assay.

Original languageEnglish
Article number2.8
JournalCurrent Protocols in Pharmacology
Issue numberSUPPL.56
StatePublished - Mar 2012


  • Fluorescence polarization (FP)
  • Förster resonance energy transfer (FRET)
  • Heterotrimeric G-protein α subunits
  • Regulator of G-protein signaling (RGS) proteins
  • Single-turnover GTP hydrolysis


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