J P Pin
- New perspectives for the development of selective metabotropic glutamate receptor ligandsJ P Pin
Centre INSERM CNRS de Pharmacologie Endocrinologie, UPR 9023 CNRS, Laboratoire des Mécanismes Moléculaires des Communications Cellulaires, Montpellier, France
Eur J Pharmacol 375:277-94. 1999..No doubt that in the near future a multitude of new tools to modulate the activity of these receptors will be discovered, enabling the identification of the possible therapeutic applications for these new neuroactive molecules...
- mGluR7-like metabotropic glutamate receptors inhibit NMDA-mediated excitotoxicity in cultured mouse cerebellar granule neuronsM Lafon-Cazal
UPR 9023, CCIPE, Montpellier, France
Eur J Neurosci 11:663-72. 1999..The present results add to the hypothesis that presynaptic mGluRs, probably mGluR7, may be the targets of drugs decreasing glutamate release and then neuronal death observed in some pathological situations...
- Molecular mechanisms of GABA(B) receptor activation: new insights from the mechanism of action of CGP7930, a positive allosteric modulatorV Binet
Laboratory of Functional Genomics, CNRS UPR 2580, Montpellier, France
Biochem Soc Trans 32:871-2. 2004..Thus the heptahelical domain of GABA(B2) behaves similar to a rhodopsin-like receptor. These results open new strategies for studying the mechanism of activation of GABA(B) receptor and examine any possible role of GABA(B2)...
- Comparative effect of L-CCG-I, DCG-IV and gamma-carboxy-L-glutamate on all cloned metabotropic glutamate receptor subtypesI Brabet
Centre INSERM CNRS de Pharmacologie Endocrinologie, UPR 9023 CNRS, Montpellier, France
Neuropharmacology 37:1043-51. 1998..These observations will be useful for the development of more potent and selective mGlu receptor agonists and antagonists...
- mGluR7-like receptor and GABA(B) receptor activation enhance neurotoxic effects of N-methyl-D-aspartate in cultured mouse striatal GABAergic neuronesM Lafon-Cazal
CNRS UPR 9023, CCIPE, Montpellier, France
Neuropharmacology 38:1631-40. 1999....
- Conservation of the ligand recognition site of metabotropic glutamate receptors during evolutionM L Parmentier
Centre INSERM CNRS de Pharmacologie Endocrinologie, UPR 9023 CNRS, rue de la Cardonille, 34094, Montpellier, France
Neuropharmacology 39:1119-31. 2000..These data indicate that there has been a strong selective pressure during evolution to maintain the ligand recognition selectivity of mGluRs...
- G-protein-coupled receptor oligomers: two or more for what? Lessons from mGlu and GABAB receptorsJ P Pin
Institut de Genomique Fonctionnelle, Département de Pharmacologie Moléculaire, CNRS UMR5203, INSERM U661, University of Montpellier 1 and 2, Montpellier, France
J Physiol 587:5337-44. 2009..We propose that GABA(B) receptor oligomerization offers a way to increase the possibility of modulating receptor signalling and activity, allowing the same receptor protein to have specific properties in neurons at different locations...
- [Use of a G-protein-coupled receptor to communicate. An evolutionary success]J Bockaert
CNRS UPR 9023 CCIPE, Montpellier, France
C R Acad Sci III 321:529-51. 1998..GPCR can adopt several 'active' conformations some of them being found in mutated receptors responsible for pathologies...
- Molecular tinkering of G protein-coupled receptors: an evolutionary successJ Bockaert
UPR CNRS 9023, CCIPE, 141 rue de la Cardonille, 34094 Montpellier Cedex 5, France
EMBO J 18:1723-9. 1999..Finally, some GPCRs are unfaithful to G proteins and interact directly, via their C-terminal domain, with proteins containing PDZ and Enabled/VASP homology (EVH)-like domains...
- Allosteric interactions between GB1 and GB2 subunits are required for optimal GABA(B) receptor functionT Galvez
, CNRS-UPR9023, CCIPE, 141 rue de la Cardonille, F-34094 Montpellier, France
EMBO J 20:2152-9. 2001..These data indicate that multiple allosteric interactions between the two subunits are required for wild-type functioning of the GABA(B) receptor and highlight further the importance of the dimerization process in GPCR activation...
- Alternative splicing generates a novel isoform of the rat metabotropic GABA(B)R1 receptorT Pfaff
Molecular Neurobiology of Signal Transduction, Max Planck Institute for Biophysical Chemistry, Gottingen, Germany
Eur J Neurosci 11:2874-82. 1999..1/3.2 channels in Xenopus oocytes and to PLC-activating chimeric G(alpha)qo subunits in HEK-293 cells with a similar EC50 for agonists. These data suggest that the R1c isoform represents a functional GABA(B)R in the rat brain...
- Ca(2+) requirement for high-affinity gamma-aminobutyric acid (GABA) binding at GABA(B) receptors: involvement of serine 269 of the GABA(B)R1 subunitT Galvez
Centre Institut National de la Santé et de la Recherche Médicale Centre National de la Recherche Scientifique de Pharmacologie Endocrinologie, UPR 9023 Centre National de la Recherche Scientifique, Montpellier, France
Mol Pharmacol 57:419-26. 2000..Taken together, these results show that Ser269, which is conserved in the GABA(B)R1 protein from Caenorhabditis elegans to mammals, is critical for the Ca(2+)-effect on the heteromeric GABA(B) receptor...
- The C terminus of the metabotropic glutamate receptor subtypes 2 and 7 specifies the receptor signaling pathwaysJ Perroy
CNRS, UPR 9023, CCIPE, 34094 Montpellier Cedex 5, France
J Biol Chem 276:45800-5. 2001..These results show that the C terminus of mGlu2 and mGlu7 receptors is a key structural determinant that allows these receptors to select a specific signaling pathway in neurons...
- Coupling of metabotropic glutamate receptors 2 and 4 to G alpha 15, G alpha 16, and chimeric G alpha q/i proteins: characterization of new antagonistsJ Gomeza
UPR Centre Nationale de Recherche Scientifique 9023, Mecanismes Moleculaires des Communications Cellulaires, CCIPE, Montpeller, France
Mol Pharmacol 50:923-30. 1996..Using this functional assay, (R,S)-alpha-methyl-4-phosphonophenylglycine was found to have a similar KB value for mGluR2 and mGluR4...