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Research ArticleArticle

Characterization and Comparison of RGS2 and RGS4 as GTPase-Activating Proteins for m2 Muscarinic Receptor-Stimulated Gi

Wendy Cladman and Peter Chidiac
Molecular Pharmacology September 2002, 62 (3) 654-659; DOI: https://doi.org/10.1124/mol.62.3.654
Wendy Cladman
Department of Pharmacology and Toxicology, Faculty of Medicine and Dentistry, University of Western Ontario, London, Ontario, Canada
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Peter Chidiac
Department of Pharmacology and Toxicology, Faculty of Medicine and Dentistry, University of Western Ontario, London, Ontario, Canada
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This article has a correction. Please see:

  • Correction to “Characterization and comparison of RGS2 and RGS4 as GTPase-activating proteins for m2 muscarinic receptor-stimulated Gi ” - October 01, 2002

Abstract

RGS2 and RGS4 were studied for their effects as GTPase activating proteins (GAPs) on receptor-activated Gi in a novel steady-state assay using membranes from Sf9 cells quadruply infected with baculoviruses encoding the m2 muscarinic receptor, Gαi2, Gβ1, and Gγ2. In the presence of the muscarinic agonist carbachol, regulator of G protein signaling 2 (RGS2) and RGS4 each produced up to a 10-fold increase in agonist-dependent GTPase activity. The observedK m for GTP in this system was increased in the presence of RGS4. NaCl and KCl inhibited the GAP activities of both RGS2 and RGS4, although they had no effect on GTPase activity in the absence of RGS proteins. MgCl2 had a complex effect on GTPase activity, with optimal RGS2 and RGS4 GAP activities occurring, respectively, at high micromolar and low millimolar concentrations of free Mg2+. The concentration dependence of RGS GAP activity was assessed, and RGS4 was found to be more potent than RGS2 by up to an order of magnitude. This direct observation confirms a similar difference in potency found when these two RGS proteins were compared for their ability to inhibit signaling downstream of Gi(Heximer et al., 1999). RGS2 yielded Hill coefficients greater than 2.0, suggesting that it may bind in a positively cooperative manner to oligomeric structures containing more than one G protein. Furthermore, RGS4 yielded a bell-shaped dose-dependence under low magnesium (0.5 mM) conditions, which is also consistent with the idea of RGS cooperativity.

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Molecular Pharmacology: 62 (3)
Molecular Pharmacology
Vol. 62, Issue 3
1 Sep 2002
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Research ArticleArticle

Characterization and Comparison of RGS2 and RGS4 as GTPase-Activating Proteins for m2 Muscarinic Receptor-Stimulated Gi

Wendy Cladman and Peter Chidiac
Molecular Pharmacology September 1, 2002, 62 (3) 654-659; DOI: https://doi.org/10.1124/mol.62.3.654

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Research ArticleArticle

Characterization and Comparison of RGS2 and RGS4 as GTPase-Activating Proteins for m2 Muscarinic Receptor-Stimulated Gi

Wendy Cladman and Peter Chidiac
Molecular Pharmacology September 1, 2002, 62 (3) 654-659; DOI: https://doi.org/10.1124/mol.62.3.654
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