Capillary electrophoresis assay for G protein-coupled receptor-mediated GTPase activity

Anal Chem. 2007 Feb 1;79(3):1158-63. doi: 10.1021/ac061099g.

Abstract

We describe a capillary electrophoresis (CE) assay to detect G protein-coupled receptor (GPCR)-stimulated G protein GTPase activity in cell membranes expressing alpha2A adrenoreceptor-Galphao1 wild-type (wt) or C351I mutant fusion proteins using a fluorescent, hydrolyzable GTP analogue. As no change in total fluorescence is observed by conversion of substrate to product, CE is used to separate the fluorescent substrate (*GTP) from the fluorescent product (*GDP). Using the assay, the alpha2a adrenoceptor agonist UK14,304 was shown to simulate specific production of *GDP in membranes from HEK293T cells expressing receptor-G protein fusion to 525% of basal levels with an EC50 of 0.48 +/- 0.20 microM. The EC50 increased to 9.4 +/- 5 muM with addition of the antagonist yohimbine. Nucleotide hydrolysis was increased further over agonist-stimulated levels with addition of the in vivo modulator protein RGS (regulator of G protein signaling). It is envisioned that this technique could be used for screening for novel GPCR ligands or other G protein signaling modifiers.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Cell Line
  • Cell Membrane / enzymology
  • Drug Evaluation, Preclinical / methods
  • Electrophoresis, Capillary / methods*
  • Fluorescent Dyes / analysis
  • GTP Phosphohydrolases / analysis*
  • GTP Phosphohydrolases / metabolism
  • Guanosine Diphosphate / analysis
  • Guanosine Diphosphate / biosynthesis
  • Guanosine Triphosphate / analysis
  • Guanosine Triphosphate / metabolism
  • Humans
  • Ligands
  • Receptors, Adrenergic, alpha-2
  • Receptors, G-Protein-Coupled*
  • Transfection

Substances

  • ADRA2A protein, human
  • Fluorescent Dyes
  • Ligands
  • Receptors, Adrenergic, alpha-2
  • Receptors, G-Protein-Coupled
  • Guanosine Diphosphate
  • Guanosine Triphosphate
  • GTP Phosphohydrolases