Joel Bockaert

Summary

Country: France

Publications

  1. ncbi request reprint [G-protein-coupled receptors: general features and activation mechanisms]
    Joel Bockaert
    Institut de Genomique Fonctionnelle, CNRS UMR 5203, INSERM U661, Universités de Montpellier 1 et 2 CNRS, Génomique fonctionnelle, 141 rue de la Cardonille 34094 Montpellier cedex 5
    Bull Acad Natl Med 196:1765-75. 2012
  2. doi request reprint [G-protein coupled receptors. Nobel Prize 2012 for chemistry to Robert J. Lefkowitz and Brian Kobilka]
    Joel Bockaert
    CNRS UMR 5203, Institut de Genomique Fonctionnelle, INSERM U661, Université de Montpellier 1 et 2, 34000 Montpellier, France
    Med Sci (Paris) 28:1133-7. 2012
  3. pmc Systems medicine and integrated care to combat chronic noncommunicable diseases
    Jean Bousquet
    Department of Respiratory Diseases, Arnaud de Villeneuve Hospital, CHU Montpellier, INSERM CESP U1018, Villejuif, France
    Genome Med 3:43. 2011
  4. ncbi request reprint Neuronal 5-HT metabotropic receptors: fine-tuning of their structure, signaling, and roles in synaptic modulation
    Joel Bockaert
    CNRS, UMR5203, Montpellier, F 34094, France
    Cell Tissue Res 326:553-72. 2006
  5. ncbi request reprint GPCR interacting proteins (GIPs) in the nervous system: Roles in physiology and pathologies
    Joel Bockaert
    Centre National de la Recherche Scientifique, UMR, Institut de Genomique Fonctionnelle, Montpellier, France
    Annu Rev Pharmacol Toxicol 50:89-109. 2010
  6. ncbi request reprint 5-HT(4) receptors: history, molecular pharmacology and brain functions
    Joel Bockaert
    CNRS UMR 5203, Institut de Genomique Fonctionnelle, Montpellier, France
    Neuropharmacology 55:922-31. 2008
  7. doi request reprint 5-HT(4) receptors, a place in the sun: act two
    Joel Bockaert
    Institut de Genomique Fonctionnelle, Universite de Montpellier, CNRS UMR5203, Montpellier F 34094, France
    Curr Opin Pharmacol 11:87-93. 2011
  8. pmc GLP-1 mediates antiapoptotic effect by phosphorylating Bad through a beta-arrestin 1-mediated ERK1/2 activation in pancreatic beta-cells
    Julie Quoyer
    INSERM, U661, Equipe Avenir, CNRS, UMR5203, Institut de Genomique Fonctionnelle, Université Montpellier I and II, 34094 Montpellier Cedex 5, France
    J Biol Chem 285:1989-2002. 2010
  9. doi request reprint beta-Arrestin 1 is required for PAC1 receptor-mediated potentiation of long-lasting ERK1/2 activation by glucose in pancreatic beta-cells
    Christophe Broca
    Institut de Genomique Fonctionnelle, CNRS, Unite Mixte de Recherche 5203, INSERM, U661, Universite Montpellier I, and Université Montpellier II, 34094 Montpellier Cedex 5, France
    J Biol Chem 284:4332-42. 2009
  10. pmc Beta-arrestin1 phosphorylation by GRK5 regulates G protein-independent 5-HT4 receptor signalling
    Gael Barthet
    Institut de Genomique Fonctionnelle, Universités de Montpellier, CNRS, Montpellier, France
    EMBO J 28:2706-18. 2009

Detail Information

Publications71

  1. ncbi request reprint [G-protein-coupled receptors: general features and activation mechanisms]
    Joel Bockaert
    Institut de Genomique Fonctionnelle, CNRS UMR 5203, INSERM U661, Universités de Montpellier 1 et 2 CNRS, Génomique fonctionnelle, 141 rue de la Cardonille 34094 Montpellier cedex 5
    Bull Acad Natl Med 196:1765-75. 2012
    ..A crystal of an "activated" beta2-adrenergic receptor associated with a Gs protein has been obtained. This knowledge will certainly lead to the discovery of new drugs...
  2. doi request reprint [G-protein coupled receptors. Nobel Prize 2012 for chemistry to Robert J. Lefkowitz and Brian Kobilka]
    Joel Bockaert
    CNRS UMR 5203, Institut de Genomique Fonctionnelle, INSERM U661, Université de Montpellier 1 et 2, 34000 Montpellier, France
    Med Sci (Paris) 28:1133-7. 2012
    ..Brian Kobilka was successful, in 2007, in producing a crystal structure of the β2-adrenergic receptor. This paved the way for the production of a series of almost 50 GPCR crystal structures both in inactive and active forms...
  3. pmc Systems medicine and integrated care to combat chronic noncommunicable diseases
    Jean Bousquet
    Department of Respiratory Diseases, Arnaud de Villeneuve Hospital, CHU Montpellier, INSERM CESP U1018, Villejuif, France
    Genome Med 3:43. 2011
    ..This systems medicine strategy, which will take a holistic approach to disease, is designed to allow the results to be used globally, taking into account the needs and specificities of local economies and health systems...
  4. ncbi request reprint Neuronal 5-HT metabotropic receptors: fine-tuning of their structure, signaling, and roles in synaptic modulation
    Joel Bockaert
    CNRS, UMR5203, Montpellier, F 34094, France
    Cell Tissue Res 326:553-72. 2006
    ..The functions of these proteins are starting to be revealed. These proteins have been implicated in targeting, trafficking to or from the membrane, desensitization, and fine-tuning of signaling...
  5. ncbi request reprint GPCR interacting proteins (GIPs) in the nervous system: Roles in physiology and pathologies
    Joel Bockaert
    Centre National de la Recherche Scientifique, UMR, Institut de Genomique Fonctionnelle, Montpellier, France
    Annu Rev Pharmacol Toxicol 50:89-109. 2010
    ..Here, we highlight the role of GIPs in some important neurological and psychiatric disorders, as well as their potential for the future development of therapeutic drugs...
  6. ncbi request reprint 5-HT(4) receptors: history, molecular pharmacology and brain functions
    Joel Bockaert
    CNRS UMR 5203, Institut de Genomique Fonctionnelle, Montpellier, France
    Neuropharmacology 55:922-31. 2008
    ..However, since 5-HT(4) receptors have recognized effects on memory, depression and feeding in animal models, there is still hope for a therapeutic destiny of this interesting target in brain disorders...
  7. doi request reprint 5-HT(4) receptors, a place in the sun: act two
    Joel Bockaert
    Institut de Genomique Fonctionnelle, Universite de Montpellier, CNRS UMR5203, Montpellier F 34094, France
    Curr Opin Pharmacol 11:87-93. 2011
    ..Several major devastating illnesses could benefit from 5-HT(4) receptors-directed therapy such as Alzheimer's disease, feeding-associated diseases such as anorexia and major depressive disorders...
  8. pmc GLP-1 mediates antiapoptotic effect by phosphorylating Bad through a beta-arrestin 1-mediated ERK1/2 activation in pancreatic beta-cells
    Julie Quoyer
    INSERM, U661, Equipe Avenir, CNRS, UMR5203, Institut de Genomique Fonctionnelle, Université Montpellier I and II, 34094 Montpellier Cedex 5, France
    J Biol Chem 285:1989-2002. 2010
    ..Such signaling mechanism may serve as a prototype to generate new therapeutic GLP-1R ligands...
  9. doi request reprint beta-Arrestin 1 is required for PAC1 receptor-mediated potentiation of long-lasting ERK1/2 activation by glucose in pancreatic beta-cells
    Christophe Broca
    Institut de Genomique Fonctionnelle, CNRS, Unite Mixte de Recherche 5203, INSERM, U661, Universite Montpellier I, and Université Montpellier II, 34094 Montpellier Cedex 5, France
    J Biol Chem 284:4332-42. 2009
    ....
  10. pmc Beta-arrestin1 phosphorylation by GRK5 regulates G protein-independent 5-HT4 receptor signalling
    Gael Barthet
    Institut de Genomique Fonctionnelle, Universités de Montpellier, CNRS, Montpellier, France
    EMBO J 28:2706-18. 2009
    ..This is the first demonstration that beta-arrestin1 phosphorylation by GRK5 regulates G protein-independent signalling...
  11. pmc Physical interaction of calmodulin with the 5-hydroxytryptamine2C receptor C-terminus is essential for G protein-independent, arrestin-dependent receptor signaling
    Marilyne Labasque
    Centre National de la Recherche Scientifique, Unite Mixte de Recherche 5203, Institut de Genomique Fonctionnelle, Montpellier F 34094, France
    Mol Biol Cell 19:4640-50. 2008
    ..This signaling pathway might be involved in neurogenesis induced by chronic treatment with 5-HT(2C) receptor agonists and their antidepressant-like activity...
  12. pmc PICK1 uncoupling from mGluR7a causes absence-like seizures
    Federica Bertaso
    CNRS UMR5203, Institut de Genomique Fonctionnelle, Montpellier, France, INSERM, U661, Montpellier, France and Université Montpellier, 1, 2, 141 Rue de Cardonille, 34094 Montpellier, Cedex 5, France
    Nat Neurosci 11:940-8. 2008
    ....
  13. ncbi request reprint Cdk5 induces constitutive activation of 5-HT6 receptors to promote neurite growth
    Fanny Duhr
    1 CNRS, UMR 5203, Institut de Genomique Fonctionnelle, F 34000 Montpellier, France 2 INSERM, U661, Montpellier, France 3 Universités de Montpellier 1 and 2, UMR 5203, Montpellier, France
    Nat Chem Biol 10:590-7. 2014
    ..These results reveal a functional interplay between Cdk5 and a G protein-coupled receptor to control neuronal differentiation. ..
  14. doi request reprint Shank3-Rich2 interaction regulates AMPA receptor recycling and synaptic long-term potentiation
    Fabrice Raynaud
    Centre National de la Recherche Scientifique CNRS, Unité Mixte de Recherche UMR 5203, Institut de Genomique Fonctionnelle, Montpellier, F 34094, France
    J Neurosci 33:9699-715. 2013
    ..These results identify Rich2-Shank3 as a new postsynaptic protein complex involved in synaptic plasticity...
  15. pmc 5-hydroxytryptamine 4 receptor activation of the extracellular signal-regulated kinase pathway depends on Src activation but not on G protein or beta-arrestin signaling
    Gael Barthet
    Institut de Genomique Fonctionnelle, Montpellier F 34094, France
    Mol Biol Cell 18:1979-91. 2007
    ..Finally, we confirmed that the main route by which 5-HT(4)Rs activate ERKs in neurons was Src dependent. Thus, in addition to classical cAMP/PKA signaling pathways, 5-HT(4)Rs may use ERK pathways to control memory process...
  16. doi request reprint Constitutive activity of serotonin 2C receptors at G protein-independent signaling: modulation by RNA editing and antidepressants
    Marilyne Labasque
    Centre National de la Recherche Scientifique, Unite Mixte de Recherche 5203, Institut de Genomique Fonctionnelle, Universite Montpellier 1 and 2, Montpellier, France
    Mol Pharmacol 78:818-26. 2010
    ..Together, these data provide the first evidence of constitutive activity of a G protein-coupled receptor toward G-independent, β-arrestin-dependent, receptor signaling...
  17. pmc 5-HT4 receptors constitutively promote the non-amyloidogenic pathway of APP cleavage and interact with ADAM10
    Maud Cochet
    CNRS, UMR 5203, Institut de Genomique Fonctionnelle, F 34000 Montpellier, France
    ACS Chem Neurosci 4:130-40. 2013
    ..These findings describe a new mechanism whereby a GPCR constitutively stimulates the cleavage of APP by α-secretase and promotes the nonamyloidogenic pathway of APP processing...
  18. pmc Muscle dystroglycan organizes the postsynapse and regulates presynaptic neurotransmitter release at the Drosophila neuromuscular junction
    Laurent Bogdanik
    CNRS, UMR 5203, Institut de Genomique Fonctionnelle, Montpellier, France
    PLoS ONE 3:e2084. 2008
    ..Dystroglycan is a central component of the DGC because it establishes a link between the extracellular matrix and Dystrophin. In this study, we focused on the synaptic role of Dystroglycan (Dg) in Drosophila...
  19. doi request reprint Pharmacological profile of engineered 5-HT₄ receptors and identification of 5-HT₄ receptor-biased ligands
    Florence Gaven
    CNRS, UMR 5203, Institut de Genomique Fonctionnelle, F 34000 Montpellier, France
    Brain Res 1511:65-72. 2013
    ..This article is part of a Special Issue entitled Optogenetics (7th BRES)...
  20. doi request reprint Quantitative proteomic analysis reveals protein expression changes in the murine neuronal secretome during apoptosis
    Eric Thouvenot
    Institut de Genomique Fonctionnelle, CNRS UMR 5203, INSERM U661, Univ Montpellier I, Univ Montpellier II, F 34094 Montpellier, France
    J Proteomics 77:394-405. 2012
    ..This list of apoptosis-regulated proteins should be considered when using targeted quantitative proteomics approaches to characterize or validate CSF biomarkers of neurodegenerative disorders...
  21. pmc Epac mediates PACAP-dependent long-term depression in the hippocampus
    Jeanne Ster
    CNRS, UMR 5203, Institut de Genomique Fonctionnelle, Montpellier, France
    J Physiol 587:101-13. 2009
    ..Altogether these results provided evidence for a new form of hippocampal LTD...
  22. doi request reprint Calcineurin interacts with the serotonin transporter C-terminus to modulate its plasma membrane expression and serotonin uptake
    Mathieu Seimandi
    Centre National de la Recherche Scientifique, UMR 5203, Institut de Genomique Fonctionnelle, F 34094 Montpellier, France, Institut National de la Sante et de la Recherche Medicale, U661, F 34094 Montpellier, France, Universite Montpellier 1, F 34094 Montpellier, France, Universite Montpellier 2, F 34094 Montpellier, France, and Brain Research Institute, Medical Faculty of the University of Zürich and Department of Health Science and Technology of the Swiss Federal Institute of Technology, CH 8057 Zurich, Switzerland
    J Neurosci 33:16189-99. 2013
    ....
  23. pmc Homer1a-dependent crosstalk between NMDA and metabotropic glutamate receptors in mouse neurons
    Federica Bertaso
    Departement of Neurobiology, Institut de Genomique Fonctionnelle, CNRS UMR 5203, INSERM U661, Université de Montpellier 1 and 2, Montpellier, France
    PLoS ONE 5:e9755. 2010
    ..Whether such a versatile link supports functional crosstalk between the receptors is unknown...
  24. doi request reprint Direct interaction enables cross-talk between ionotropic and group I metabotropic glutamate receptors
    Julie Perroy
    Institut de Genomique Fonctionnelle, CNRS UMR 5203, INSERM U661, Universités de Montpellier 1 and 2, Montpellier 34094, France
    J Biol Chem 283:6799-805. 2008
    ..This direct functional interaction implies a higher degree of target-effector specificity, timing, and subcellular localization of signaling than could ever be predicted with complex signaling pathways...
  25. ncbi request reprint 3,4-N-methlenedioxymethamphetamine-induced hypophagia is maintained in 5-HT1B receptor knockout mice, but suppressed by the 5-HT2C receptor antagonist RS102221
    Gregory Conductier
    UPR CNRS 5203, Génomique fonctionnelle, Montpellier Cedex, France
    Neuropsychopharmacology 30:1056-63. 2005
    ....
  26. ncbi request reprint A single mutation in the 5-HT4 receptor (5-HT4-R D100(3.32)A) generates a Gs-coupled receptor activated exclusively by synthetic ligands (RASSL)
    Sylvie Claeysen
    Centre National de la Recherche Scientifique, UPR 9023, 141 rue de la Cardonille, 34094 Montpellier, Cedex 5, France
    J Biol Chem 278:699-702. 2003
    ..More interestingly, two synthetic ligands behave as antagonists on the wild type but as agonists on the 5-HT(4)-RASSL...
  27. pmc Plant insecticide L-canavanine repels Drosophila via the insect orphan GPCR DmX
    Christian Mitri
    Institut de Genomique Fonctionnelle, CNRS UMR5203, INSERM U661, University of Montpellier I and II, Montpellier, France
    PLoS Biol 7:e1000147. 2009
    ..These findings show that the DmX receptor, which does not belong to the Gr family, fulfills a gustatory function necessary to avoid eating a natural toxin...
  28. pmc Degradation of cAMP-responsive element-binding protein by the ubiquitin-proteasome pathway contributes to glucotoxicity in beta-cells and human pancreatic islets
    Safia Costes
    Institut National de la Sante et de la Recherche Medicale INSERM, U661, Equipe Avenir, Institut de Genomique Fonctionnelle, Montpellier, France
    Diabetes 58:1105-15. 2009
    ..The transcription factor cAMP-responsive element-binding protein (CREB) is crucial for beta-cell survival and function. We investigated whether prolonged exposure of beta-cells to high glucose affects the functional integrity of CREB...
  29. ncbi request reprint Uncoupling and endocytosis of 5-hydroxytryptamine 4 receptors. Distinct molecular events with different GRK2 requirements
    Gael Barthet
    CNRS UMR5203, Montpellier, F 34094, France
    J Biol Chem 280:27924-34. 2005
    ..These results clearly demonstrate that the uncoupling and endocytosis of 5-HT4R require different GRK2 concentrations and involve distinct molecular events...
  30. pmc Anorexia induced by activation of serotonin 5-HT4 receptors is mediated by increases in CART in the nucleus accumbens
    Alexandra Jean
    Centre National de Recherche Scientifique, Unite Mixte de Recherche 5203, Institut National de Santé et de Recherche Médicale, U661, Université Montpellier I and II, Institut de Genomique Fonctionnelle, département de neurobiologie, Montpellier, France
    Proc Natl Acad Sci U S A 104:16335-40. 2007
    ..Collectively, these results demonstrate that 5-HT(4)R-mediated up-regulation of CART in the NAc triggers the appetite-suppressant effects of ecstasy...
  31. pmc Gαo is required for L-canavanine detection in Drosophila
    Isabelle Devambez
    CNRS, UMR 5203, Institut de Genomique Fonctionnelle, Montpellier, France
    PLoS ONE 8:e63484. 2013
    ..In conclusion, our study revealed that Gαo47A plays a crucial role in L-canavanine detection...
  32. ncbi request reprint G protein-coupled receptors: dominant players in cell-cell communication
    Joel Bockaert
    UPR CNRS 9023, Montpellier, France
    Int Rev Cytol 212:63-132. 2002
    ..Mutations of GPCRs are responsible for a wide range of genetic diseases. The importance of GPCRs in physiological processes is illustrated by the fact that they are the target of the majority of therapeutical drugs and drugs of abuse...
  33. ncbi request reprint Difference in mass analysis using labeled lysines (DIMAL-K): a new, efficient proteomic quantification method applied to the analysis of astrocytic secretomes
    Nicolas Delcourt
    département de neurobiologie, Institut de Genomique Fonctionnelle, 141 rue de la Cardonille, 34094 Montpellier Cedex 5, France
    Mol Cell Proteomics 4:1085-94. 2005
    ..We showed that DIMAL-K was more sensitive and accurate than densitometric image analysis and allowed the detection and quantification of novel proteins...
  34. ncbi request reprint The proteomic analysis of mouse choroid plexus secretome reveals a high protein secretion capacity of choroidal epithelial cells
    Eric Thouvenot
    CNRS UMR 5203, Montpellier, France
    Proteomics 6:5941-52. 2006
    ..These proteins may play a critical role in neuronal growth, differentiation and function as well as in brain pathologies...
  35. pmc Dynamic remodeling of scaffold interactions in dendritic spines controls synaptic excitability
    Enora Moutin
    Centre National de la Recherche Scientifique, UMR 5203, Institut de Genomique Fonctionnelle, F 34000 Montpellier, Cedex 16, France
    J Cell Biol 198:251-63. 2012
    ..Such protein scaffold remodeling represents a form of homeostatic control of synaptic excitability...
  36. doi request reprint Techniques for studying inverse agonist activity of antidepressants at recombinant nonedited 5-HT(₂C-INI) receptor and native neuronal 5-HT(₂C) receptors
    Mathieu Seimandi
    Centre National de la Recherche Scientifique, Institut de Genomique Fonctionnelle, Montpellier, France
    Methods Enzymol 485:61-79. 2010
    ....
  37. pmc G protein activation by serotonin type 4 receptor dimers: evidence that turning on two protomers is more efficient
    Lucie P Pellissier
    Institut de Genomique Fonctionnelle, Universite de Montpellier, CNRS UMR5203, F 34094 Montpellier, France
    J Biol Chem 286:9985-97. 2011
    ..These results, together with previous findings, demonstrate that, differently from class C GPCR dimers, class A GPCR dimers have pleiotropic activation mechanisms...
  38. ncbi request reprint Co-assembly of two GluR6 kainate receptor splice variants within a functional protein complex
    Françoise Coussen
    Laboratoire Physiologie Cellulaire de la Synapse, CNRS, UMR 5091, Institut Francois Magendie, Universite Bordeaux, 2, rue C Saint Saëns, 33077 Bordeaux Cedex, France
    Neuron 47:555-66. 2005
    ..Thus, GluR6a and GluR6b bring in close proximity two separate subsets of interacting proteins that contribute to the fine regulation of KAR trafficking and function...
  39. ncbi request reprint Adaptive changes in serotonin neurons of the raphe nuclei in 5-HT(4) receptor knock-out mouse
    Gregory Conductier
    Unité mixte de Recherche Centre National de la Recherche Scientifique 5203, INSERM, U661, University Montpellier I, University Montpellier II, Institut de Genomique Fonctionnelle, département de neurobiologie, Montpellier, France
    Eur J Neurosci 24:1053-62. 2006
    ..The mechanisms whereby 5-HT(4)R mediate a tonic positive influence on the firing activity of DRN 5-HT neurons and 5-HT content remain to be determined...
  40. ncbi request reprint Increased number of neural progenitors in human temporal lobe epilepsy
    Arielle Crespel
    Institut de Genomique Fonctionnelle, CNRS UMR 5023 INSERM U661, UM1 UM2, 141 rue de la Cardonille, F 34094 Montpellier Cedex 5, France
    Neurobiol Dis 19:436-50. 2005
    ..These findings demonstrate that neural progenitors proliferate in chronic epilepsy and suggest that the fissura hippocampi behaves like another neurogenic area...
  41. doi request reprint Epileptiform activity induces vascular remodeling and zonula occludens 1 downregulation in organotypic hippocampal cultures: role of VEGF signaling pathways
    Mélanie Morin-Brureau
    Institut de Genomique Fonctionnelle, Centre National de la Recherche Scientifique Unité Mixte de Recherche 5203, INSERM U661, Universite Montpellier 1, 2 Montpellier, France
    J Neurosci 31:10677-88. 2011
    ..This suggests that Src pathway could be a therapeutic target for BBB protection in epilepsies...
  42. doi request reprint Enhanced detection of CNS cell secretome in plasma protein-depleted cerebrospinal fluid
    Eric Thouvenot
    Centre National de la Recherche Scientifique, UMR 5203, Institut de Genomique Fonctionnelle, Montpellier, France
    J Proteome Res 7:4409-21. 2008
    ..Hence, removal of 20 major plasma proteins from CSF improves detection of brain cell-derived proteins in CSF and should facilitate identification of relevant biomarkers in CSF proteome profiling analyses...
  43. doi request reprint Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-hydroxytryptamine-4 receptors
    Lucie P Pellissier
    Centre National de Recherche Scientifique Unité Mixte de Recherche 5203, Institut de Genomique Fonctionnelle, Institut National de Sant et de Recherche Médicale U661, Universites Montpellier 1 and 2, Montpellier, France
    Mol Pharmacol 75:982-90. 2009
    ..R(*)-5-HT is probably attained through other routes of activation. Thus, different conformational arrangements occur during stabilization of R(*)basal, R(*)-5-HT, R(*)-benzamides, and R(*)-BIMU8...
  44. ncbi request reprint Inverse agonist and neutral antagonist actions of antidepressants at recombinant and native 5-hydroxytryptamine2C receptors: differential modulation of cell surface expression and signal transduction
    Benjamin Chanrion
    Institut de Genomique Fonctionnelle, Universités de Montpellier, CNRS UMRS 5203, INSERM U661, 141 rue de la Cardonille, F 34094 Montpellier Cedex 5, France
    Mol Pharmacol 73:748-57. 2008
    ..The clinical significance of inverse agonist versus neutral antagonist properties both during and after drug administration will be of interest to elucidate...
  45. ncbi request reprint A 5-HT4 receptor transmembrane network implicated in the activity of inverse agonists but not agonists
    Lara Joubert
    Centre National de la Recherche Scientifique, UPR 9023, Montpellier, France
    J Biol Chem 277:25502-11. 2002
    ..Molecular modeling indicated that Asp-100, Phe-275, and Trp-272 might constitute a network required for stabilization of the silent state by the described inverse agonists. However, this network is not necessary for agonist activity...
  46. pmc 5-HT(6) receptor recruitment of mTOR as a mechanism for perturbed cognition in schizophrenia
    Julie Meffre
    CNRS, UMR 5203, Institut de Genomique Fonctionnelle, Montpellier, France
    EMBO Mol Med 4:1043-56. 2012
    ..These observations suggest that recruitment of mTOR by prefrontal 5-HT(6) receptors contributes to the perturbed cognition in schizophrenia, offering new vistas for its therapeutic control...
  47. ncbi request reprint Shank expression is sufficient to induce functional dendritic spine synapses in aspiny neurons
    Gautier Roussignol
    Institut de Genomique Fonctionnelle, Unite Mixte de Recherche 5203, 34000 Montpellier, France
    J Neurosci 25:3560-70. 2005
    ..These results strongly suggest that Shank proteins and the associated glutamate receptors participate in a concerted manner to form spines and functional synapses...
  48. pmc Quantitative phosphoproteomics unravels biased phosphorylation of serotonin 2A receptor at Ser280 by hallucinogenic versus nonhallucinogenic agonists
    Samah Karaki
    CNRS, UMR 5203, Institut de Genomique Fonctionnelle, F 34094 Montpellier, France
    Mol Cell Proteomics 13:1273-85. 2014
    ..This study reveals a biased phosphorylation of the 5-HT(2A) receptor in response to hallucinogenic versus nonhallucinogenic agonists, which underlies their distinct capacity to desensitize the receptor...
  49. ncbi request reprint Widespread brain distribution of the Drosophila metabotropic glutamate receptor
    Jean Marc Devaud
    CNRS, UMR5203, Institut de Genomique Fonctionnelle, Montpellier, France
    Neuroreport 19:367-71. 2008
    ..Using a specific antibody, we report DmGluRA expression in most neuropile areas in both larvae and adults, but not in the lobes of the mushroom bodies. These observations suggest a key role for glutamate in the insect brain...
  50. ncbi request reprint Up-regulation of the PACAP type-1 receptor (PAC1) promoter by neurotrophins in rat PC12 cells and mouse cerebellar granule cells via the Ras/mitogen-activated protein kinase cascade
    Francoise Jamen
    UPR CNRS 9023, Montpellier, France
    J Neurochem 82:1199-207. 2002
    ..Our results show that the PAC1 promoter can be up-regulated by diverse neurotrophins via an MAPK-dependent pathway and suggest a role for the Ras protein...
  51. pmc PACAP type I receptor transactivation is essential for IGF-1 receptor signalling and antiapoptotic activity in neurons
    Nicolas Delcourt
    CNRS UMR 5203, Montpellier, France
    EMBO J 26:1542-51. 2007
    ....
  52. ncbi request reprint The Drosophila metabotropic glutamate receptor DmGluRA regulates activity-dependent synaptic facilitation and fine synaptic morphology
    Laurent Bogdanik
    Laboratoire de Génomique Fonctionnelle, Centre National de la Recherche Scientifique, Unite Propre de Recherche 2580, 34094 Montpellier Cedex 05, France
    J Neurosci 24:9105-16. 2004
    ....
  53. doi request reprint β-Arrestin2 plays a key role in the modulation of the pancreatic beta cell mass in mice
    Magalie A Ravier
    CNRS, UMR 5203, Institut de Genomique Fonctionnelle, 141 rue de la Cardonille, 34094, Montpellier, France
    Diabetologia 57:532-41. 2014
    ....
  54. ncbi request reprint 5-HT receptor-associated protein networks: new targets for drug discovery in psychiatric disorders?
    Philippe Marin
    Institut de Genomique Fonctionnelle, 141 rue de la Cardonille, Montpellier F 34094 Montpellier Cedex 5, France
    Curr Drug Targets 13:28-52. 2012
    ....
  55. ncbi request reprint MacMARCKS interacts with the metabotropic glutamate receptor type 7 and modulates G protein-mediated constitutive inhibition of calcium channels
    Federica Bertaso
    CNRS, UMR5203, Montpellier INSERM, U661, Montpellier, University Montpellier I and II, Montpellier, France
    J Neurochem 99:288-98. 2006
    ..These results suggest that competitive interactions of Ca2+/calmodulin and MacMARCKS with mGluR7 control the tonic inhibition of VSCCs by G-proteins...
  56. pmc Exchange protein activated by cAMP (Epac) mediates cAMP activation of p38 MAPK and modulation of Ca2+-dependent K+ channels in cerebellar neurons
    Jeanne Ster
    Institute of Functional Genomics, Centre National de la Recherche Scientifique, Unite Mixte de Recherche 5203, Institute National de la Santé et de la Recherche Médicale U661, Universites Montpellier I et II, 34095 Montpellier, France
    Proc Natl Acad Sci U S A 104:2519-24. 2007
    ..These effects involve activation of Rap and p38 MAPK, which mobilizes intracellular Ca2+ stores. These findings reveal a cAMP Epac-dependent and protein kinase A-independent signaling cascade that controls neuronal excitability...
  57. ncbi request reprint ERK1/2 control phosphorylation and protein level of cAMP-responsive element-binding protein: a key role in glucose-mediated pancreatic beta-cell survival
    Safia Costes
    INSERM U661, Equipe Avenir, Institut de Genomique Fonctionnelle, 141, rue de la Cardonille, 34094 Montpellier Cedex 5, France
    Diabetes 55:2220-30. 2006
    ..Our results indicate that ERK1 and -2 control the phosphorylation and protein level of CREB and play a key role in glucose-mediated pancreatic beta-cell survival...
  58. ncbi request reprint Identification and functional roles of metabotropic glutamate receptor-interacting proteins
    Laurent Fagni
    Laboratory of Functional Genomics, CNRS UPR 2580, CCIPE, 141 rue de la Cardonille, 34094 Montpellier Cedex 05, France
    Semin Cell Dev Biol 15:289-98. 2004
    ..Here we will focus on those proteins that interact with the subgroup of metabotropic glutamate (mGlu) receptors, and review the methods used for their identification, as well as their functional roles in neurons...
  59. ncbi request reprint GPCR-GIP networks: a first step in the discovery of new therapeutic drugs?
    Joel Bockaert
    Laboratoire de Génomique Fonctionnelle, UPR CNRS 2580, 34094 Montpellier Cedex 5, France
    Curr Opin Drug Discov Devel 7:649-57. 2004
    ..Finally, we discuss the possibilities for developing new therapeutic drugs capable of modulating GPCR signaling by disrupting or reinforcing specific GPCR-GIP interactions...
  60. ncbi request reprint [Feeding disorders in 5-HT4 receptor knockout mice]
    Valérie Compan
    Laboratoire de Génomique Fonctionnelle, UPR CNRS 2580, 141 rue de la Cardonille, 34094 Montpellier
    J Soc Biol 198:37-49. 2004
    ....
  61. ncbi request reprint GPCR interacting proteins (GIP)
    Joel Bockaert
    UPR CNRS 2580, CCIPE, 141 rue de la Cardonille, 34094 Montpellier Cedex 5, France
    Pharmacol Ther 103:203-21. 2004
    ..Finally, only few GIPs have been found thus far to interact with the third intracellular loop of GPCRs. The future will tell us if this situation is only due to technical reasons...
  62. ncbi request reprint The 'magic tail' of G protein-coupled receptors: an anchorage for functional protein networks
    Joel Bockaert
    Laboratoire de Génomique Fonctionnelle, UPR CNRS 2580, 141 rue de la Cardonille, 34094 Montpellier Cedex 5, France
    FEBS Lett 546:65-72. 2003
    ..To date, proteins that interact with the GPCR C-terminus are the most abundant and are the focus of this review...
  63. ncbi request reprint Dynamic reorganization of the astrocyte actin cytoskeleton elicited by cAMP and PACAP: a role for phosphatidylInositol 3-kinase inhibition
    Virgili Perez
    UPR 2580 CNRS, Laboratoire de Génomique Fonctionnelle, 141, rue de la Cardonille, 34094 Montpellier Cedex 05, France
    Eur J Neurosci 21:26-32. 2005
    ..Together, these data demonstrate for the first time that depolymerization of stress fibres, and the resulting astrocyte stellation, induced by stimulation of cAMP production involves the inhibition of the PI 3-K-RhoA pathway...
  64. doi request reprint Alzheimer culprits: cellular crossroads and interplay
    Sylvie Claeysen
    CNRS, UMR 5203, Institut de Genomique Fonctionnelle, F 34000 Montpellier, France
    Cell Signal 24:1831-40. 2012
    ..Being able to reduce the formation of the toxic Aβ peptides is obviously an immediate approach in the trial to prevent AD. The following review summarizes the most relevant discoveries in the field of the last decades...
  65. ncbi request reprint GPCR-jacking: from a new route in RTK signalling to a new concept in GPCR activation
    Nicolas Delcourt
    Institut de Genomique Fonctionnelle, Universités de Montpellier, CNRS UMR 5203, 141 rue de la Cardonille, Montpellier Cedex 5, F 34094, France
    Trends Pharmacol Sci 28:602-7. 2007
    ..Here, we provide an overview of the molecular mechanisms involved in this novel cross-communication between GPCRs and RTKs and discuss its relevance in the specification of growth factor signalling and functions...
  66. pmc Subcellular imaging of dynamic protein interactions by bioluminescence resonance energy transfer
    Vincent Coulon
    Institut de Genomique Fonctionnelle, CNRS UMR5203, INSERM U661, University of Montpellier, Montpellier, France
    Biophys J 94:1001-9. 2008
    ..These studies provide a proof of principle as well as experimental parameters and controls required for high-resolution dynamic studies using BRET imaging in single cells...
  67. pmc Effects of oral monosodium (L)-glutamate on insulin secretion and glucose tolerance in healthy volunteers
    Hugues Chevassus
    Section of Clinical Pharmacology, Clinical Investigation Center, Saint Eloi University Hospital, and Research Unit UPRES EA 1677, Faculty of Medicine, Montpellier, France
    Br J Clin Pharmacol 53:641-3. 2002
    ..To investigate the effects of glutamate on insulin secretion and glucose tolerance in humans...
  68. ncbi request reprint Attenuated response to stress and novelty and hypersensitivity to seizures in 5-HT4 receptor knock-out mice
    Valérie Compan
    Unité Propre de Recherche Centre National de la Recherche Scientifique 2580, Génomique fonctionnelle, Montpellier 34094, France
    J Neurosci 24:412-9. 2004
    ..These results provide the first example of a genetic deficit that disrupts the ability of stress to reduce feeding and body weight and suggest that 5-HT4 receptors may be involved in stress-induced anorexia and seizure susceptibility...
  69. ncbi request reprint Immature-like astrocytes are associated with dentate granule cell migration in human temporal lobe epilepsy
    Arielle Crespel
    UPR CNRS 9023, CCIPE, Montpellier, France
    Neurosci Lett 330:114-8. 2002
    ..We suggest that granule cell migration that occurs in adult epileptic focus results from the transient occurrence of immature-like glia throughout the granular layer...
  70. ncbi request reprint Pituitary adenylate cyclase-activating polypeptide receptors mediating insulin secretion in rodent pancreatic islets are coupled to adenylate cyclase but not to PLC
    Francoise Jamen
    Unité Propre de Recherche 9023, Centre National de la Recherche Scientifique, 34094 Montpellier Cedex 05, France
    Endocrinology 143:1253-9. 2002
    ..These results clearly show that the insulinotropic effect of PACAP involved both VPAC and PAC1. The PAC1 variants expressed in rat and mouse pancreatic islets seem to be coupled to adenylate cyclase but not to PLC...
  71. pmc Endogenous cannabinoids mediate long-term synaptic depression in the nucleus accumbens
    David Robbe
    Actions Concertées Incitatives Jeunes Chercheurs Plasticité Synaptique et Toxicomanie, Centre National de la Recherche Scientifique, Unité Propre de Recherche 9023, 141 rue de la Cardonille, 34094 Montpellier Cedex 05, France
    Proc Natl Acad Sci U S A 99:8384-8. 2002
    ..These findings unveil the role of the eCB system in activity-dependent long-term synaptic plasticity and identify a mechanism by which marijuana can alter synaptic functions in the endogenous brain reward system...