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Molecular Pharmacology

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Research ArticleArticle

The G Protein-Coupling Profile of Metabotropic Glutamate Receptors, as Determined with Exogenous G Proteins, Is Independent of Their Ligand Recognition Domain

Marie-Laure Parmentier, Cécile Joly, Sophie Restituito, Joël Bockaert, Yves Grau and Jean-Philippe Pin
Molecular Pharmacology April 1998, 53 (4) 778-786; DOI: https://doi.org/10.1124/mol.53.4.778
Marie-Laure Parmentier
Mécanismes Moléculaires des Communications Cellulaires, UPR-9023 Centre National de la Recherche Scientifique, Institute National de la Santé et de la Recherche Médicale de Pharmacologie/Endocrinologie, 34094 Montpellier Cedex 05, France
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Cécile Joly
Mécanismes Moléculaires des Communications Cellulaires, UPR-9023 Centre National de la Recherche Scientifique, Institute National de la Santé et de la Recherche Médicale de Pharmacologie/Endocrinologie, 34094 Montpellier Cedex 05, France
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Sophie Restituito
Mécanismes Moléculaires des Communications Cellulaires, UPR-9023 Centre National de la Recherche Scientifique, Institute National de la Santé et de la Recherche Médicale de Pharmacologie/Endocrinologie, 34094 Montpellier Cedex 05, France
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Joël Bockaert
Mécanismes Moléculaires des Communications Cellulaires, UPR-9023 Centre National de la Recherche Scientifique, Institute National de la Santé et de la Recherche Médicale de Pharmacologie/Endocrinologie, 34094 Montpellier Cedex 05, France
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Yves Grau
Mécanismes Moléculaires des Communications Cellulaires, UPR-9023 Centre National de la Recherche Scientifique, Institute National de la Santé et de la Recherche Médicale de Pharmacologie/Endocrinologie, 34094 Montpellier Cedex 05, France
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Jean-Philippe Pin
Mécanismes Moléculaires des Communications Cellulaires, UPR-9023 Centre National de la Recherche Scientifique, Institute National de la Santé et de la Recherche Médicale de Pharmacologie/Endocrinologie, 34094 Montpellier Cedex 05, France
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Abstract

Metabotropic glutamate (mGlu), Ca2+-sensing, γ-aminobutyric acidB, and a large number of pheromone receptors constitute a peculiar family of G protein-coupled receptors. They possess a large extracellular domain that has been proposed to constitute their ligand binding domain. The aim of the current study was to examine whether this large ligand binding domain had any influence on the G protein-coupling selectivity of the receptor, and vice versa. We chose mGlu receptors, which are classified into three groups according to their sequence homology and pharmacology, as representatives of this receptor family. To define a G protein-coupling profile for these receptors, we used a set of exogenous phospholipase C-activating G proteins in the same way that synthetic ligands are used to define agonist and antagonist pharmacological profiles. This set includes Gα15, Gα16, Gαq, and chimeric Gαq proteins with the last few amino acids of either Gαi2 (Gαqi), Gαo(Gαqo), or Gαz (Gαqz). Cotransfection of mGlu receptors with these G proteins and examination of their coupling to phospholipase C revealed that group I, II, and III receptors have distinct G protein-coupling profiles. By swapping the extracellular domains of the most distantly related mGlu receptors (the rat group I mGlu1a and the Drosophila melanogaster group II DmGluA receptors), we show that the extracellular domain determines the agonist pharmacological profile and that this domain does not modify the G protein-coupling profile determined by the seven-transmembrane-domain region of mGlu receptors.

Footnotes

    • Received October 2, 1997.
    • Accepted January 2, 1998.
  • Send reprint requests to: Dr. J.-P. Pin, CCIPE, 141 rue de la Cardonille, 34094 Montpellier, Cedex 5, France. E-mail:pin{at}ccipe.montp.inserm.fr

  • ↵1 Current affiliation: Department of Genetics, University of Cambridge, Cambridge CB2 3EH, UK.

  • This work was supported by grants from the Centre Nationale de Recherche Scientifique, the European Community [Biomed2 (BMH4-CT96–0228) and Biotech2 (BIO4-CT96–0049) Programs], the French Ministry of Education, Research and Professional Insertion (ACC-SV5, Grant 9505077), the Fondation pour la Recherche Médicale, the Direction des Recherches et Etudes Techniques (DRET 91/161). and Bayer (France and Germany).

  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 53 (4)
Molecular Pharmacology
Vol. 53, Issue 4
1 Apr 1998
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Research ArticleArticle

The G Protein-Coupling Profile of Metabotropic Glutamate Receptors, as Determined with Exogenous G Proteins, Is Independent of Their Ligand Recognition Domain

Marie-Laure Parmentier, Cécile Joly, Sophie Restituito, Joël Bockaert, Yves Grau and Jean-Philippe Pin
Molecular Pharmacology April 1, 1998, 53 (4) 778-786; DOI: https://doi.org/10.1124/mol.53.4.778

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Research ArticleArticle

The G Protein-Coupling Profile of Metabotropic Glutamate Receptors, as Determined with Exogenous G Proteins, Is Independent of Their Ligand Recognition Domain

Marie-Laure Parmentier, Cécile Joly, Sophie Restituito, Joël Bockaert, Yves Grau and Jean-Philippe Pin
Molecular Pharmacology April 1, 1998, 53 (4) 778-786; DOI: https://doi.org/10.1124/mol.53.4.778
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