title: Evaluating modulators of "Regulator of G-protein Signaling" (RGS) proteins.
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.
authors.affiliation: Department of Pharmacology, The University of North Carolina at Chapel Hill, Chapel Hill, North Carolina.
authors.forename: Dustin E
authors.initials: DE
authors.lastname: Bosch
authors.forename: Thomas
authors.initials: T
authors.lastname: Zielinski
authors.forename: Robert G
authors.initials: RG
authors.lastname: Lowery
authors.forename: David P
authors.initials: DP
authors.lastname: Siderovski
mesh_terms: D001681:Biological Assay / Q000379:methods*; D002853:Chromatography, Liquid / Q000379:methods; D031541:Fluorescence Resonance Energy Transfer / Q000379:methods; D005456:Fluorescent Dyes; D044385:GTP-Binding Protein alpha Subunits / Q000302:isolation & purification / Q000378:metabolism; D019204:GTP-Binding Proteins / Q000187:drug effects / Q000378:metabolism*; D020690:GTPase-Activating Proteins / Q000378:metabolism; D006868:Hydrolysis; D020710:RGS Proteins / Q000187:drug effects / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects / Q000502:physiology*
chemical_list: D005456:Fluorescent Dyes; D044385:GTP-Binding Protein alpha Subunits; D020690:GTPase-Activating Proteins; D020710:RGS Proteins; D019204:GTP-Binding Proteins