Research Topics
Genomes and Genes
| J BockaertSummaryCountry: France Publications
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Publications
5-HT4 receptors: gene, transduction and effects on olfactory memoryJ Bockaert
CNRS UPR 9023, Centre CNRS INSERM de Pharmacologie Endocrinologie CCIPE, Montpellier, France
Ann N Y Acad Sci 861:1-15. 1998....- [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... - 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... - Constitutively active mutants of 5-HT4 receptors are they in unique active states?S Claeysen
UPR CNRS 9023, Montpellier, France
EMBO Rep 2:61-7. 2001..However, the constitutive activity of the receptor mutated within the third intracellular loop was the result of both a change in the allosteric J constant and a change in the R* conformation... - Alternative splicing of the imprinted candidate tumor suppressor gene ZAC regulates its antiproliferative and DNA binding activitiesB Bilanges
Mecanismes Moleculaires des Communications Cellulaires, UPR 9023 CNRS, 141 rue de la Cardonille, F 34094 Montpellier Cedex 05, France
Oncogene 20:1246-53. 2001..Hence, these data further underline that ZAC gene is critically controlled, both at the transcriptional level through imprinting and at the functional level through alternative splicing... - 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... - Novel brain-specific 5-HT4 receptor splice variants show marked constitutive activity: role of the C-terminal intracellular domainS Claeysen
Centre National de la Recherche Scientifique, Unité Propre de Recherche 9023, Montpellier, France
Mol Pharmacol 55:910-20. 1999..Moreover, we further identified a sequence within the C-terminal tail upstream of L358, rich in serine and threonine residues, that played a crucial role in maintaining 5-HT4R under its inactive conformation... - Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclaseS Claeysen
CNRS UPR 9023, Centre CNRS INSERM de Pharmacologie Endocrinologie, Montpellier, France
Neuroreport 8:3189-96. 1997.... - Neurotransmitter regulation of MAP kinase signaling in striatal neurons in primary cultureS R Vincent
CNRS UPR 9023 CCIPE, Montpellier, France
Synapse 29:29-36. 1998..However, the signal transduction pathways mediating these responses appear to be distinct from those known to mediate MAP kinase activation by other stimuli... - PACAP-38 protects cerebellar granule cells from apoptosisL Journot
Centre National de la Recherche Scientifique, Centre CNRS INSERM de Pharmacologie Endocrinologie, Montpellier, France
Ann N Y Acad Sci 865:100-10. 1998..PD98059, an inhibitor of MEK (MAP kinase kinase), completely abolished the anti-apoptotic effect of PACAP-38, suggesting that MAP kinase pathway activation is necessary for PACAP-38 effect... - 5-HT4 receptors: cloning and expression of new splice variantsS Claeysen
CNRS UPR 9023, Centre CNRS INSERM de Pharmacologie Endocrinologie CCIPE, Montpellier, France
Ann N Y Acad Sci 861:49-56. 1998..Our data suggest that the differences in efficacy of 5-HT4 ligands on 5-HT4 receptor-mediated responses in several tissues is due to differences in coupling efficiency rather than to the presence of different 5-HT4 receptor isoforms... - PICK1 is required for the control of synaptic transmission by the metabotropic glutamate receptor 7J Perroy
UPR CNRS 9023, CCIPE, 141 rue de la Cardonille, 34094 Montpellier Cedex 05, France
EMBO J 21:2990-9. 2002..These results indicate that the scaffolding protein, PICK1, plays an essential role in the control of synaptic transmission by the mGlu7a receptor complex... - Alternative splicing in the N-terminal extracellular domain of the pituitary adenylate cyclase-activating polypeptide (PACAP) receptor modulates receptor selectivity and relative potencies of PACAP-27 and PACAP-38 in phospholipase C activationC Pantaloni
CNRS UPR 9023, Centre CNRS INSERM de Pharmacologie Endocrinologie, rue de la Cardonille, F 34094 Montpellier Cedex 05, France
J Biol Chem 271:22146-51. 1996..We demonstrate that this domain modulates receptor selectivity with respect to PACAP-27 and -38 binding and controls the relative potencies of the two agonists in phospholipase C stimulation... - 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.... - The 5-HT4 receptor subtype inhibits K+ current in colliculi neurones via activation of a cyclic AMP-dependent protein kinaseL Fagni
Centre de Pharmacologie et d Endocrinologie, Montpellier, France
Br J Pharmacol 105:973-9. 1992..The putative implication of 5-HT4 receptors in neuronal plasticity, via a blockade of K+ channels, is discussed... - The neuronal death induced by endotoxic shock but not that induced by excitatory amino acids requires TNF-alphaF de Bock
CNRS, UPR 9023, Laboratoire de Medecine Experimentale, Institut de Biologie, Montpellier, France
Eur J Neurosci 10:3107-14. 1998..In conclusion, although inflammation follows glutamate receptor-mediated neurotoxicity, the mechanisms by which an endotoxic insult triggers neuronal death are different from those involved in excitotoxicity... - Assignment of 5-hydroxytryptamine receptor (HTR4) to human chromosome 5 bands q31-->q33 by in situ hybridizationS Claeysen
CNRS-UPR 9023, Montpellier, France
Cytogenet Cell Genet 78:133-4. 1997 - A Go-like protein in Drosophila melanogaster and its expression in memory mutantsA Guillen
Centre CNRS INSERM de Pharmacologie Endocrinologie, Montpellier, France
EMBO J 9:1449-55. 1990..This report constitutes the first evidence for the participation of a Go protein in learning and memory... - 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... - Nitric oxide-induced blockade of NMDA receptorsO Manzoni
Centre CNRS INSERM de Pharmacologie Endocrinologie, Montpellier, France
Neuron 8:653-62. 1992..Since NMDA receptor activation induces NO synthesis, these results suggest a feedback inhibition of NMDA receptors by NO under physiological condition... - Impaired somatodendritic responses to pituitary adenylate cyclase-activating polypeptide (PACAP) of supraoptic neurones in PACAP type I -receptor deficient miceF Jamen
UPR 9023 CNRS and UMR 5101 CNRS, CCIPE, Montpellier, France
J Neuroendocrinol 15:871-81. 2003..In conclusion, the PAC1 receptor is solely responsible for the PACAP-induced [Ca2+]i signalling and secretion of vasopressin and oxytocin in the somatodendritic region of supraoptic neurones... - Group 2 metabotropic glutamate receptors induced long term depression in mouse striatal slicesL Kahn
CNRS UPR 9023, 141, rue de la Cardonille, 34094 Montpellier Cedex 05, France
Neurosci Lett 316:178-82. 2001..In contrast, MEK1-2 inhibitors reduced both mGlu2/3 initial depression and LTD suggesting the involvement of the mitogen activated kinase pathway in mGlu2/3-LTD... - 5-HT4 receptorsJ Bockaert
UPR CNRS 2580 CCIPE, 141 rue de la Cardonille, 34094 Montpellier Cedex 5, France
Curr Drug Targets CNS Neurol Disord 3:39-51. 2004..One 5-HT(4)R-directed drug (SL65.0155) is already in phase II to treat patients suffering from memory deficits or dementia... - 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... - Sequential expression of surface antigens and transcription factor NFkappaB by hippocampal cells in excitotoxicity and experimental epilepsyM Lerner-Natoli
CNRS UPR 9023, Laboratoire de Medecine Experimentale, Institute de Biologie, Montpellier, France
Epilepsy Res 41:141-54. 2000..Further clarification of the toxic or protective consequences of delayed inflammatory responses may be interesting in therapy of epilepsy... - hZAC encodes a zinc finger protein with antiproliferative properties and maps to a chromosomal region frequently lost in cancerA Varrault
Centre National de la Recherche Scientifique, UPR 9023, 141 rue de la Cardonille, F 34094 Montpellier Cedex 5, France
Proc Natl Acad Sci U S A 95:8835-40. 1998..quot; In view of these observations, the functional properties we report here provide further arguments to consider hZAC as a tumor suppressor gene candidate... - Cloning and functional expression of a Drosophila metabotropic glutamate receptor expressed in the embryonic CNSM L Parmentier
Unité Propre de Recherche Centre National de la Recherche Scientifique 9023, Mecanismes Moleculaires des Communications Cellulaires, Centre de Pharmacologie Endrocrinologie, 34094 Montpellier Cedex 5, France
J Neurosci 16:6687-94. 1996..These results indicate that the original structural features of both glutamate receptor types are conserved from insects to mammals and suggest that the functions of these receptors have been highly conserved during evolution... - Differential signal transduction by five splice variants of the PACAP receptorD Spengler
CNRS UPR 9023, Mecanismes Moleculaires des Communications Cellulaires, CCIPE, Montpellier, France
Nature 365:170-5. 1993..Expression of these cDNAs revealed altered patterns of adenylyl cyclase and phospholipase C stimulation, suggesting a novel mechanism for fine tuning of signal transduction... - Cloning, expression and pharmacology of the mouse 5-HT(4L) receptorS Claeysen
CNRS UPR 9023, Centre CNRS INSERM de Pharmacologie Endocrinologie CCIPE, Montpellier, France
FEBS Lett 398:19-25. 1996..In contrast to the previously described distribution, we found that mRNA encoding for both the short (5-HT(4S))and the long form (5-HT(4L)) of 5-HT4 receptors are expressed in all mouse and rat brain areas... - Secretion of protease nexin-1 by C6 glioma cells is under the control of a heterotrimeric G protein, Go1A Lagriffoul
CNRS UPR 9023, Centre CNRS INSERM de Pharmacologie et Endocrinologie, 141 rue de la Cardonille, F 34094 Montpellier Cedex 5, France
J Biol Chem 271:31508-16. 1996..These results indicate, that in C6 glioma cells, PN-1 secretion could be regulated by both Go1alpha expression and activation... - Distribution of metabotropic glutamate receptor DmGlu-A in Drosophila melanogaster central nervous systemA Ramaekers
UPR CNRS 9023, Mecanismes Moleculaires des Communications Cellulaires, CCIPE, 34094 Montpellier Cedex 5, France
J Comp Neurol 438:213-25. 2001.... - GPCR-interacting proteins (GIPs): nature and functionsJ Bockaert
LGF, UPR CNRS 2580, 141 rue de la Cardonille, 34094 Montpellier, Cedex 5, France
Biochem Soc Trans 32:851-5. 2004.... - PAC1 null females display decreased fertilityF Jamen
CNRS UPR 9023, Centre CNRS INSERM de Pharmacologie Endocrinologie, 141 rue de la Cardonille, 34094 Montpellier, France Departamento de Bioquímica y Biología Molecular, Facultad de Medicina, Universidad de Alcala, E 28871 Alcala de Henares, Spain
Ann N Y Acad Sci 921:400-4. 2000..Moreover, the pituitary-gonadal axis responded properly to an acute fasting test in KO mice. Hence, the phenotype of PAC1 null mice provides clear evidence for the role of PAC1 receptor in reproduction process... - Hippocampal alterations of apolipoprotein E and D mRNA levels in vivo and in vitro following kainate excitotoxicityP Montpied
CNRS UPR 9023, CCIPE, Montpellier, France
Epilepsy Res 35:135-46. 1999.... - PAC1 receptor-deficient mice display impaired insulinotropic response to glucose and reduced glucose toleranceF Jamen
Unité Propre de Recherche UPR9023 Centre National de la Recherche Scientifique, Montpellier, France
J Clin Invest 105:1307-15. 2000..Thus, these results are consistent with a physiological role for the PAC1 receptor in glucose homeostasis, notably during food intake... - Localization of the human pituitary adenylate cyclase-activating polypeptide receptor (PACAP1-R) gene to 7p15-p14 by fluorescence in situ hybridizationP Brabet
CRBM du CNRS UPR 9008, INSERM U.249, Montpellier, France
Genomics 38:100-2. 1996 - Agonist-independent activation of metabotropic glutamate receptors by the intracellular protein HomerF Ango
CNRS UPR 9023, CCIPE, 141 rue de la Cardonille, 34000 Montpellier, France
Nature 411:962-5. 2001..Our results show that these glutamate GPCRs can be directly activated by intracellular proteins as well as by agonists... - A novel site on the Galpha -protein that recognizes heptahelical receptorsJ Blahos
Mecanismes Moleculaires des Communications Cellulaires, CNRS UPR9023, CCIPE, 141 rue de la Cardonille, F 34094 Montpellier, France
J Biol Chem 276:3262-9. 2001..Coupling of Galpha(16) protein to the metabotropic glutamate receptor 8 is partially modulated by each module alone, whereas both modules are needed to eliminate the coupling fully... - The metabotropic glutamate receptor types 2/3 inhibit L-type calcium channels via a pertussis toxin-sensitive G-protein in cultured cerebellar granule cellsP Chavis
Centre CNRS INSERM de Pharmacologie et d Endocrinologie, Montpellier, France
J Neurosci 14:7067-76. 1994..These results suggest that mGluR2 or mGluR3 receptors suppress the activity of L-type Ca2+ channels by a mechanism involving Gi or G(o) proteins. A likely direct effect of G-proteins on the channels is discussed... - BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activityF Y Carroll
, Montpellier, France
Mol Pharmacol 59:965-73. 2001..BAY36-7620 will be useful to further delineate the functional importance of the mGlu1 receptor, including its putative agonist-independent activity... - Characterization of the methylation-sensitive promoter of the imprinted ZAC gene supports its role in transient neonatal diabetes mellitusA Varrault
UPR 9023 CNRS Centre CNRS INSERM de Pharmacologie Endocrinologie 141, rue de la Cardonille, 34094 Montpellier Cedex 05, France
J Biol Chem 276:18653-6. 2001..Our findings further strengthen the hypothesis that ZAC is the gene responsible for TNDM and suggest a novel mechanism for ZAC inactivation in breast tumors... - Cannabinoids inhibit GABAergic synaptic transmission in mice nucleus accumbensO J Manzoni
CNRS UPR 9023, 141 rue de la Cardonille, 34094 Cedex 05, Montpellier, France
Eur J Pharmacol 412:R3-5. 2001..WIN-2 modified paired-pulse ratio of evoked IPSCs and decreased miniature IPSC frequency indicating a presynaptic localization of cannabinoid CB(1) receptors... - Molecular events involved in neuronal death induced in the mouse hippocampus by in-vivo injection of kainic acidM Djebaili
CNRS UPR 9023, CCIPE, 34094 Montpellier 5, Cedex, France
Brain Res Mol Brain Res 93:190-8. 2001..Moreover, apoptosis (labeled by TUNEL) and the increase of bax and caspase-3 protein expression after the neurotoxic insult appeared to clearly depend on p53 expression... - Activation of 5-HT1A receptors expressed in NIH-3T3 cells induces focus formation and potentiates EGF effect on DNA synthesisA Varrault
Centre CNRS INSERM de Pharmacologie Endocrinologie, Montpellier, France
Mol Biol Cell 3:961-9. 1992..In conclusion, in transfected NIH-3T3 cells, transforming and mitogenic effects of 5-HT1A agonists involve a pertussis toxin-sensitive G protein but do not seem to be linked to adenylyl cyclase inhibition... - Cytokine signals propagate through the brainL Vitkovic
CNRS INSERM Centre de Pharmacologie Endocrinologie, Montpellier, France
Mol Psychiatry 5:604-15. 2000..This elucidation is a prerequisite for better understanding of reciprocal interactions between nervous, endocrine and immune systems... - The transduction signalling protein Go during embryonic development of Drosophila melanogasterA Guillen
Centre CNRS INSERM de Pharmacologie Endocrinologie, Montpellier, France
Cell Signal 3:341-52. 1991..The Go alpha protein expression was not altered in any of them but the pattern of labelling was disorganized as was the neuronal network. These results suggest a possible role for the Go protein during axonogenesis... - Regulation of apoptosis and cell cycle arrest by Zac1, a novel zinc finger protein expressed in the pituitary gland and the brainD Spengler
Max Planck Institute of Psychiatry, Molecular Neurobiology, Munich, Germany
EMBO J 16:2814-25. 1997..Zac1 is thus the first gene besides p53 which concurrently induces apoptosis and cell cycle arrest... - Up-regulation in late pregnancy of both Go1 alpha and Go2 alpha isoforms in human myometriumR Zumbihl
INSERM U65, Universite Montpellier II, France
Eur J Pharmacol 288:9-15. 1994.... - Ultrastructural localization of the GTP-binding protein Go in neuronsJ Gabrion
Laboratoire de Neurobiologie Endocrinologique, UA 1197 CNRS, Universite de Montpellier II, France
Cell Signal 1:107-23. 1989.... - Mild deficits in mice lacking pituitary adenylate cyclase-activating polypeptide receptor type 1 (PAC1) performing on memory tasksM Sauvage
Max Planck Institute of Psychiatry, Kraepelinstr 2 10, D 80804 Munich, Germany
Brain Res Mol Brain Res 84:79-89. 2000..Thus, the effects of PAC1 knock-out on modulating performance in these tasks were subtle and suggest that PAC1 only plays a limited role in learning and memory... - Interaction of serotonin 5-hydroxytryptamine type 2C receptors with PDZ10 of the multi-PDZ domain protein MUPP1C Becamel
Biofrontera Pharmaceuticals AG, Hemmelratherweg 201, 51377 Leverkusen, Germany
J Biol Chem 276:12974-82. 2001..We propose that MUPP1 may serve as a multivalent scaffold protein that selectively assembles and targets signaling complexes... - An alpha 40 subunit of a GTP-binding protein immunologically related to Go mediates a dopamine-induced decrease of Ca2+ current in snail neuronsR M Harris-Warrick
Laboratoire de Neurobiologie, , Paris, France
Neuron 1:27-32. 1988..We propose that this is a 40 kd alpha subunit of a molluscan G protein immunologically related to alpha o and that it mediates the effect of dopamine on Ca2+ currents in identified snail neurons...