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Vol. 53, Issue 4, 778-786, April 1998
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
Metabotropic glutamate (mGlu), Ca2+-sensing,
-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 G
15, G16, Gq, and
chimeric Gq proteins with the last few amino acids of
either Gi2 (Gqi), Go
(Gqo), or Gz (Gqz).
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.
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