Accéder directement au contenu

Jean-Philippe Pin

Directeur de Recherche de classe exceptionnelle au CNRS
66%
Libre accès
143
Documents
Affiliations actuelles
  • 1100822
  • 1087315
Identifiants chercheurs
Contact

Présentation

Jean-Philippe Pin got his PhD in Molecular Biology in 1987 at the University of Montpellier (France), working on excitatory amino acids receptors, at a time when glutamate was not yet fully accepted as a neurotransmitter. His studies led him to participate in 1985 in the discovery of G protein-coupled glutamate receptors, known as the metabotropic glutamate receptors. Since then, he has been concentrated on studying these fascinating dimeric and multidomain receptors. Using innovative tricks and assays co-developed with the CisBio company, he revealed any details of their original activation mechanism from the agonist-induced closure of the extracellular binding domain, to the relative movement of the two subunits, leading to a specific dimer interface of the active state allowing one subunit only to activate G proteins. These studies were extended to most class C GPCRs including the Calcium sensing and the GABAB receptor. Thanks to his collaborative laboratory established in China, he participated in the determination of the cryo-EM structure of some of these receptors, and revealed the original mode of G protein activation, different from that of all other GPCRs. Recently, he demonstrated the existence of heterodimeric mGluRs in the brain, adding sixteen possible new mGluRs in the brain. His studies were dedicated to the development of innovative molecules with the aim to decipher the therapeutic potential of these targets. Along these lines, he was among the first to report inverse agonists, as well as both negative and positive allosteric modulators for mGluRs. More recently, he has been developing original tools, including photoswitchable allosteric ligands that allowed him to demonstrate the role of central mGlu4 in the pain response, or allosteric nanobodies able to ameliorate the cognitive deficit in a mouse model of schizophrenia. In conclusion, over the recent years he developed innovative approaches to study cell surface receptors, including biosensors, photoswitchable ligands and nanobodies as pharmacological tools and potential therapeutic agents. His studies led to new concepts in the GPCR field, such as: the activation of cell surface receptors by intracellular proteins; the regulation of GPCRs by both negative and positive allosteric modulators, the asymmetric functioning of GPCR dimers.
Jean-Philippe Pin a obtenu son doctorat en biologie moléculaire en 1987 à l'université de Montpellier (France), en travaillant sur les récepteurs des acides aminés excitateurs, à une époque où le glutamate n'était pas encore pleinement accepté comme neurotransmetteur. Ses études l'ont amené à participer en 1985 à la découverte des récepteurs du glutamate couplés à la protéine G, connus sous le nom de récepteurs métabotropiques du glutamate. Depuis lors, il s'est concentré sur l'étude de ces fascinants récepteurs dimériques et multidomaines. À l'aide d'astuces et de tests innovants développés en collaboration avec la société CisBio, il a révélé tous les détails de leur mécanisme d'activation original, depuis la fermeture du domaine de liaison extracellulaire induite par l'agoniste jusqu'au mouvement relatif des deux sous-unités, conduisant à une interface dimérique spécifique de l'état actif permettant à une seule sous-unité d'activer les protéines G. Ces études ont été étendues à la plupart des récepteurs de la classe C. Ces études ont été étendues à la plupart des GPCRs de classe C, y compris la détection du calcium et le récepteur GABAB. Grâce à son laboratoire collaboratif établi en Chine, il a participé à la détermination de la structure cryo-EM de certains de ces récepteurs, et a révélé le mode original d'activation de la protéine G, différent de celui de tous les autres RCPG. Récemment, il a démontré l'existence de mGluR hétérodimériques dans le cerveau, ajoutant seize nouveaux mGluR possibles dans le cerveau. Ses études ont été consacrées au développement de molécules innovantes dans le but de décrypter le potentiel thérapeutique de ces cibles. Dans cette optique, il a été l'un des premiers à signaler l'existence d'agonistes inverses, ainsi que de modulateurs allostériques négatifs et positifs pour les mGluRs. Plus récemment, il a développé des outils originaux, notamment des ligands allostériques photoswitchables qui lui ont permis de démontrer le rôle du mGlu4 central dans la réponse à la douleur, ou des nanocorps allostériques capables d'améliorer le déficit cognitif dans un modèle murin de schizophrénie. En conclusion, au cours des dernières années, il a développé des approches innovantes pour étudier les récepteurs de la surface cellulaire, y compris les biocapteurs, les ligands photosensibles et les nanocorps en tant qu'outils pharmacologiques et agents thérapeutiques potentiels. Ses études ont débouché sur de nouveaux concepts dans le domaine des RCPG, tels que l'activation des récepteurs de surface cellulaire par des protéines intracellulaires, la régulation des RCPG par des modulateurs allostériques négatifs et positifs, le fonctionnement asymétrique des dimères de RCPG.

Domaines de recherche

Neurobiologie Biotechnologies Biochimie [q-bio.BM] Biologie moléculaire Biophysique Pharmacologie

Publications

Image document

Specific pharmacological and Gi/o protein responses of some native GPCRs in neurons

Chanjuan Xu , Yiwei Zhou , Yuxuan Liu , Li Lin , Peng Liu
Nature Communications, 2024, 15 (1), pp.1990. ⟨10.1038/s41467-024-46177-z⟩
Article dans une revue hal-04492538v1
Image document

TrkB receptor interacts with mGlu 2 receptor and mediates antipsychotic-like effects of mGlu 2 receptor activation in the mouse

Clémentine Eva Philibert , Candice Disdier , Pierre-André Lafon , Alexandre Bouyssou , Mathieu Oosterlaken
Science Advances , 2024, 10 (4), pp.eadg1679. ⟨10.1126/sciadv.adg1679⟩
Article dans une revue hal-04429823v1

Design, Synthesis, Pharmacology, and In Silico Studies of (1 S ,2 S ,3 S )-2-(( S )-Amino(carboxy)methyl)-3-(carboxymethyl)cyclopropane-1-carboxylic Acid (LBG30300): A Picomolar Potency Subtype-Selective mGlu 2 Receptor Agonist

Na Liu , Floriane Eshak , Fanny Malhaire , Isabelle Brabet , Laurent Prézeau
Journal of Medicinal Chemistry, 2024, 67 (2), pp.1314-1326. ⟨10.1021/acs.jmedchem.3c01811⟩
Article dans une revue hal-04385775v1

Synthesis and pharmacological characterization of conformationally restricted 2-amino-Adipic acid analogs and carboxycyclopropyl glycines as selective metabotropic glutamate 2 receptor agonists

Markus Staudt , Na Liu , Fanny Malhaire , Yasaman Doroudian , Laurent Prézeau
European Journal of Medicinal Chemistry, 2024, 266, pp.116157. ⟨10.1016/j.ejmech.2024.116157⟩
Article dans une revue hal-04415292v1
Image document

Different EGF ‐induced receptor dimer conformations for signaling and internalization

Jordi Haubrich , Jurriaan Zwier , Fabienne Charrier-Savournin , Laurent Prézeau , Jean‐philippe Pin
FASEB Journal, 2024, 38 (1), pp.e23356. ⟨10.1096/fj.202301209R⟩
Article dans une revue hal-04472295v1
Image document

Targeting the Brain with Single-Domain Antibodies: Greater Potential Than Stated So Far?

Mireille Elodie Tsitokana , Pierre-André Lafon , Laurent Prézeau , Jean-Philippe Pin , Philippe Rondard
International Journal of Molecular Sciences, 2023, 24 (3), pp.2632. ⟨10.3390/ijms24032632⟩
Article dans une revue hal-03991195v1
Image document

Concerted conformational changes control metabotropic glutamate receptor activity

Nathalie Lecat-Guillet , Robert Quast , Hongkang Liu , Emmanuel Bourrier , Thor Møller
Science Advances , 2023, 9 (22), pp.eadf1378. ⟨10.1126/sciadv.adf1378⟩
Article dans une revue hal-04121751v1
Image document

Biased signaling due to oligomerization of the G protein-coupled platelet-activating factor receptor

Junke Liu , Hengmin Tang , Chanjuan Xu , Shengnan Zhou , Xunying Zhu
Nature Communications, 2022, 13 (1), pp.6365. ⟨10.1038/s41467-022-34056-4⟩
Article dans une revue hal-03837051v1
Image document

Structural basis of the activation of metabotropic glutamate receptor 3

Wei Fang , Fan Yang , Chanjuan Xu , Shenglong Ling , Li Lin
Cell Research, 2022, 32 (7), pp.695-698. ⟨10.1038/s41422-022-00623-z⟩
Article dans une revue hal-03603715v1
Image document

Nanobody-based sensors reveal a high proportion of mGlu heterodimers in the brain

Jiyong Meng , Chanjuan Xu , Pierre-André Lafon , Salomé Roux , Michaël Mathieu
Nature Chemical Biology, 2022, 18, pp.894-903. ⟨10.1038/s41589-022-01050-2⟩
Article dans une revue hal-03699580v1

( S )-2-Mercaptohistidine: A First Selective Orthosteric GluK3 Antagonist

Christian Poulie , Younes Larsen , Cindie Leteneur , Gaël Barthet , Walden Bjørn-Yoshimoto
ACS Chemical Neuroscience, 2022, 13 (10), pp.1580-1587. ⟨10.1021/acschemneuro.2c00162⟩
Article dans une revue hal-03659473v1
Image document

Chronic sodium bromide treatment relieves autistic-like behavioral deficits in three mouse models of autism

Cécile Derieux , Audrey Léauté , Agathe Brugoux , Déborah Jaccaz , Claire Terrier
Neuropsychopharmacology, 2022, 47 (9), pp.1680-1692. ⟨10.1038/s41386-022-01317-1⟩
Article dans une revue hal-03647444v1
Image document

SGIP1 modulates kinetics and interactions of the cannabinoid receptor 1 and G protein‐coupled receptor kinase 3 signalosome

Matej Gazdarica , Judith Noda , Oleh Durydivka , Vendula Novosadova , Ken Mackie
Journal of Neurochemistry, 2022, 160 (6), pp.625-642. ⟨10.1111/jnc.15569⟩
Article dans une revue hal-03761588v1
Image document

A nanobody activating metabotropic glutamate receptor 4 discriminates between homo- and heterodimers

Jordi Haubrich , Joan Font , Robert Quast , Anne Goupil-Lamy , Pauline Scholler
Proceedings of the National Academy of Sciences of the United States of America, 2021, 118 (33), pp.e2105848118. ⟨10.1073/pnas.2105848118⟩
Article dans une revue hal-03322348v1
Image document

G protein‐coupled receptors can control the Hippo/YAP pathway through Gq signaling

Diana Zindel , Patrick Mensat , Claire Vol , Zeinab Homayed , Fabienne Charrier‐savournin
FASEB Journal, 2021, 35 (7), pp.e21668. ⟨10.1096/fj.202002159R⟩
Article dans une revue hal-03263933v1
Image document

The GABA B receptor mediates neuroprotection by coupling to G 13

Yunyun Wang , Siyu Gai , Wenhua Zhang , Xuetao Huang , Shumin Ma
Science Signaling, 2021, 14 (705), pp.eaaz4112. ⟨10.1126/scisignal.aaz4112⟩
Article dans une revue hal-03394399v1
Image document

Structural basis of GABAB receptor–Gi protein coupling

Cangsong Shen , Chunyou Mao , Chanjuan Xu , Nan Jin , Huibing Zhang
Article dans une revue hal-03218736v1

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors

Stephen Alexander , Arthur Christopoulos , Anthony Davenport , Eamonn Kelly , Alistair Mathie
British Journal of Pharmacology, 2021, 178 (S1), pp.e0243333. ⟨10.1111/bph.15538⟩
Article dans une revue hal-03875300v1
Image document

GABAB1e promotes the malignancy of human cancer cells by targeting the tyrosine phosphatase PTPN12

Bo Wei , Yini Zhu , Peng Yang , Yong Han , Suyun Wang
iScience, 2021, 24 (11), pp.103311. ⟨10.1016/j.isci.2021.103311⟩
Article dans une revue hal-03432362v1
Image document

Structures of human mGlu2 and mGlu7 homo- and heterodimers

Juan Du , Dejian Wang , Hongcheng Fan , Chanjuan Xu , Linhua Tai
Nature, 2021, 594 (7864), pp.589-593. ⟨10.1038/s41586-021-03641-w⟩
Article dans une revue hal-03269110v1
Image document

Agonists and allosteric modulators promote signaling from different metabotropic glutamate receptor 5 conformations

Chady Nasrallah , Giuseppe Cannone , Julie Briot , Karine Rottier , Alice Berizzi
Cell Reports, 2021, 36 (9), pp.109648. ⟨10.1016/j.celrep.2021.109648⟩
Article dans une revue hal-03340751v1
Image document

Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state

Anne-Marinette Cao , Robert B Quast , Fataneh Fatemi , Philippe Rondard , Jean-Philippe Pin
Nature Communications, 2021, 12 (1), pp.5426. ⟨10.1038/s41467-021-25620-5⟩
Article dans une revue hal-03352901v2
Image document

Allosteric ligands control the activation of a class C GPCR heterodimer by acting at the transmembrane interface

Lei Liu , Zhiran Fan , Xavier Rovira , Li Xue , Salomé Roux
eLife, 2021, 10, pp.e70188. ⟨10.7554/eLife.70188⟩
Article dans une revue hal-03738955v1
Image document

Illuminating the allosteric modulation of the calcium-sensing receptor

Hongkang Liu , Ping Yi , Wenjing Zhao , Yuling Wu , Francine Acher
Proceedings of the National Academy of Sciences of the United States of America, 2020, 117 (35), pp.21711-21722. ⟨10.1073/pnas.1922231117⟩
Article dans une revue hal-02933760v1
Image document

Structural basis for distinct quality control mechanisms of Drosophila and mammalian GABAB receptor

Shenglan Zhang , Li Xue , Xuehui Liu , Xuejun Cai Zhang , Rui Zhou
FASEB Journal, 2020, 34 (12), pp.16348-16363. ⟨10.1096/fj.202001355RR⟩
Article dans une revue hal-03065658v1
Image document

D1-mGlu5 heteromers mediate noncanonical dopamine signaling in Parkinson’s disease

Irene Sebastianutto , Elise Goyet , Laura Andreoli , Joan Font-Ingles , David Moreno-Delgado
Journal of Clinical Investigation, 2020, 130 (3), pp.1168 - 1184. ⟨10.1172/JCI126361⟩
Article dans une revue hal-02476033v1
Image document

Structural basis of metabotropic GABA receptor activation

Hamidreza Shaye , Andrii Ishchenko , Jordy Homing Lam , Gye Won Han , Li Xue
Nature, 2020, 584 (7820), pp.298-303. ⟨10.1038/s41586-020-2408-4⟩
Article dans une revue hal-03065675v1
Image document

LSP5-2157 a new inhibitor of vesicular glutamate transporters

Odile Poirel , Lauren E Mamer , Melissa A Herman , Marie Arnulf-Kempcke , Myriam Kervern
Neuropharmacology, 2019, 164, pp.107902. ⟨10.1016/j.neuropharm.2019.107902⟩
Article dans une revue hal-03043497v1
Image document

Rearrangement of the transmembrane domain interfaces associated with the activation 1 of a GPCR hetero-oligomer 2 3

Li Xue , Qian Sun , Han Zhao , Xavier Rovira , Siyu Gai
Nature Communications, 2019, 10 (1), pp.2765. ⟨10.1038/s41467-019-10834-5⟩
Article dans une revue hal-02398123v1
Image document

Infiltrating Myeloid Cells Drive Osteosarcoma Progression via GRM4 Regulation of IL23

Maya Kansara , Kristian Thomson , Puiyi Pang , Aurélie Dutour , Lisa Mirabello
Cancer Discovery, 2019, 9 (11), pp.1511-1519. ⟨10.1158/2159-8290.CD-19-0154⟩
Article dans une revue hal-02398127v1
Image document

GPCR interaction as a possible way for allosteric control between receptors

Jean-Philippe Pin , Julie Kniazeff , Laurent Prézeau , Jiang-Feng Liu , Philippe Rondard
Molecular and Cellular Endocrinology, 2019, ⟨10.1016/j.mce.2019.02.019⟩
Article dans une revue hal-02396289v1
Image document

Non-classical ligand-independent regulation of Go protein by an orphan Class C GPCR

Mariana Hajj , Teresa de Vita , Claire Vol , Charlotte Renassia , Jean-Charles Bologna
Molecular Pharmacology, 2019, 96 (2), pp.233-246. ⟨10.1124/mol.118.113019⟩
Article dans une revue hal-02396282v1
Image document

Context-Dependent Signaling of CXC Chemokine Receptor 4 and Atypical Chemokine Receptor 3

Joyce Heuninck , Cristina Perpiñá Viciano , Ali Işbilir , Birgit Caspar , Davide Capoferri
Molecular Pharmacology, 2019, 96 (6), pp.778-793. ⟨10.1124/mol.118.115477⟩
Article dans une revue hal-02389610v1
Image document

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein‐coupled receptors

Stephen Alexander , Arthur Christopoulos , Anthony P Davenport , Eamonn Kelly , Alistair Mathie
British Journal of Pharmacology, 2019, 176 (S1), pp.S21-S141. ⟨10.1111/bph.14748⟩
Article dans une revue hal-02388696v1

Profiling of orthosteric and allosteric group-III metabotropic glutamate receptor ligands on various G protein-coupled receptors with Tag-lite® assays

Abderazak Belhocine , Pietro Veglianese , Candide Hounsou , Elodie Dupuis , Francine C. Acher
Neuropharmacology, 2018, 140, pp.233-245. ⟨10.1016/j.neuropharm.2018.07.032⟩
Article dans une revue hal-02388698v1

Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites

Chelliah Selvam , Isabelle Lemasson , Isabelle Brabet , Nadia Oueslati , Berin Karaman
Journal of Medicinal Chemistry, 2018, 61 (5), pp.1969-1989. ⟨10.1021/acs.jmedchem.7b01438⟩
Article dans une revue hal-02018007v1
Image document

Allosteric interactions between GABA B1 subunits control orthosteric binding sites occupancy within GABA B oligomers

Gregory D Stewart , Laetitia Comps-Agrar , Lenea Blanc Nørskov-Lauritsen , Jean-Philippe Pin , Julie Kniazeff
Neuropharmacology, 2018, 136, pp.92-101. ⟨10.1016/j.neuropharm.2017.12.042⟩
Article dans une revue hal-02398132v1
Image document

Inhibition of neuronal FLT3 receptor tyrosine kinase alleviates peripheral neuropathic pain in mice

Cyril Rivat , Chamroeun Sar , Ilana Mechaly , J.P. Leyris , Lucie Diouloufet
Nature Communications, 2018, 9 (1), pp.1042. ⟨10.1038/s41467-018-03496-2⟩
Article dans une revue hal-02158159v1
Image document

Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs

Chady Nasrallah , Karine Rottier , Romain Marcellin , Vincent Compan , J. Font
Scientific Reports, 2018, 8 (1), pp.4407. ⟨10.1038/s41598-018-22729-4⟩
Article dans une revue hal-02073194v1
Image document

Dynamic modulation of inflammatory pain-related affective and sensory symptoms by optical control of amygdala metabotropic glutamate receptor 4

Charleine Zussy , X. Gomez-Santacana , Xavier Rovira , Dimitri de Bundel , S. Ferrazzo
Molecular Psychiatry, 2018, 23 (3), pp.509-520. ⟨10.1038/mp.2016.223⟩
Article dans une revue hal-02073218v1
Image document

Oligomerization of a G protein-coupled receptor in neurons controlled by its structural dynamics

Thor C Møller , Jérôme Hottin , Caroline Clerté , Jurriaan M. Zwier , Thierry Durroux
Scientific Reports, 2018, 8 (1), ⟨10.1038/s41598-018-28682-6⟩
Article dans une revue hal-02398134v1

Inhibition of neuronal FLT3 receptor tyrosine kinase alleviates peripheral neuropathic pain in mice

Cyril Rivat , Chamroeun Sar , Ilana Mechaly , Jean-Philippe Leyris , Lucie Diouloufet
Nature Communications, 2018, 9 (1), ⟨10.1038/s41467-018-03496-2⟩
Article dans une revue hal-03412426v1
Image document

Chloride ions stabilize the glutamate-induced active state of the metabotropic glutamate receptor 3

Amélie S. Tora , Xavier Rovira , Anne-Marinette Cao , Alexandre Cabaye , Linnea Olofsson
Neuropharmacology, 2018, 140, pp.275-286. ⟨10.1016/j.neuropharm.2018.08.011⟩
Article dans une revue hal-02346230v1
Image document

Analysis of positive and negative allosteric modulation in metabotropic glutamate receptors 4 and 5 with a dual ligand

James Dalton , Jean-Philippe Pin , Jesús Giraldo
Scientific Reports, 2017, 7 (1), pp.4944. ⟨10.1038/s41598-017-05095-5⟩
Article dans une revue hal-02058681v1

From the Promiscuous Asenapine to Potent Fluorescent Ligands Acting at a Series of Aminergic G-Protein-Coupled Receptors

Candide Hounsou , Corinne Baehr , Vincent Gasparik , Doria Alili , Abderazak Belhocine
Journal of Medicinal Chemistry, 2017, 61 (1), pp.174-188. ⟨10.1021/ACS.JMEDCHEM.7B01220⟩
Article dans une revue hal-02366277v1

FRET-Based Sensors Unravel Activation and Allosteric Modulation of the GABA B Receptor

Nathalie Lecat-Guillet , Carine Monnier , Xavier Rovira , Julie Kniazeff , Laurent Lamarque
Cell Chemical Biology, 2017, 24 (3), pp.360-370. ⟨10.1016/j.chembiol.2017.02.011⟩
Article dans une revue hal-02072973v1

HTS-compatible FRET-based conformational sensors clarify membrane receptor activation

Pauline Scholler , David Moreno-Delgado , Nathalie Lecat-Guillet , Etienne Doumazane , Carine Monnier
Nature Chemical Biology, 2017, 13 (4), pp.372-380. ⟨10.1038/nchembio.2286⟩
Article dans une revue hal-02075211v1
Image document

Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator

Joan Font , Marc López-Cano , Serena Notartomaso , Pamela Scarselli , Paola Di Pietro
Article dans une revue hal-03549950v1
Image document

Allosteric nanobodies uncover a role of hippocampal mGlu2 receptor homodimers in contextual fear consolidation

Pauline Scholler , Damien Nevoltris , Dimitri de Bundel , Simon Bossi , David Moreno-Delgado
Nature Communications, 2017, 8 (1), pp.1967. ⟨10.1038/s41467-017-01489-1⟩
Article dans une revue hal-01672805v2
Image document

Class C G protein-coupled receptors: reviving old couples with new partners

Thor C Møller , David Moreno-Delgado , Jean-Philippe Pin , Julie Kniazeff
Biophysics Reports, 2017, 3 (4-6), pp.57-63. ⟨10.1007/s41048-017-0036-9⟩
Article dans une revue hal-02073162v1
Image document

Antibodies targeting G protein-coupled receptors: Recent advances and therapeutic challenges

Mohammed Akli Ayoub , Pascale Crépieux , Markus Koglin , Marc Parmentier , Jean-Philippe Pin
Article dans une revue hal-01604272v1
Image document

Pharmacological evidence for a metabotropic glutamate receptor heterodimer in neuronal cells

David Moreno-Delgado , Thor C Møller , Jeanne Ster , Jesús Giraldo , Damien Maurel
Article dans une revue hal-02073201v1
Image document

RgIA4 potently blocks mouse $\alpha$9$\alpha$10 nAChRs and provides long lasting protection against oxaliplatin-induced cold allodynia

Sean Christensen , Arik Hone , Isabelle Roux , Julie Kniazeff , Jean-Philippe Pin
Frontiers in Cellular Neuroscience, 2017, 11, pp.219. ⟨10.3389/fncel.2017.00219⟩
Article dans une revue hal-03363884v1

Positional isomers of bispyridine benzene derivatives induce efficacy changes on mGlu 5 negative allosteric modulation

Xavier Gómez-Santacana , James Dalton , Xavier Rovira , Jean-Philippe Pin , Cyril Goudet
European Journal of Medicinal Chemistry, 2017, 127, pp.567-576. ⟨10.1016/j.ejmech.2017.01.013⟩
Article dans une revue hal-02066019v1
Image document

Illuminating Phenylazopyridines To Photoswitch Metabotropic Glutamate Receptors: From the Flask to the Animals

Xavier Gómez-Santacana , Silvia Pittolo , Xavier Rovira , Marc Lopez , Charleine Zussy
ACS Central Science, 2017, 3 (1), pp.81-91. ⟨10.1021/acscentsci.6b00353⟩
Article dans une revue hal-02066097v1
Image document

Allosteric control of an asymmetric transduction in a G protein-coupled receptor heterodimer

Junke Liu , Zongyong Zhang , David Moreno-Delgado , James Ar Dalton , Xavier Rovira
Article dans une revue hal-02073040v1
Image document

OptoGluNAM4.1, a Photoswitchable Allosteric Antagonist for Real-Time Control of mGlu4 Receptor Activity

Xavier Rovira , Ana Trapero , Silvia Pittolo , Charleine Zussy , Adèle Faucherre
Cell Chemical Biology, 2016, 23 (8), pp.929--34. ⟨10.1016/j.chembiol.2016.06.013⟩
Article dans une revue hal-01941168v1
Image document

Identification of key phosphorylation sites in PTH1R that determine arrestin3 binding and fine-tune receptor signaling

Diana Zindel , S. Engel , A. R. Bottrill , Jean-Philippe Pin , Laurent Prézeau
Biochemical Journal, 2016, 473 (22), pp.4173--4192. ⟨10.1042/BCJ20160740⟩
Article dans une revue hal-01940960v1

Shining Light on an mGlu5 Photoswitchable NAM: A Theoretical Perspective

James Dalton , Isaias Lans , Xavier Rovira , Fanny Malhaire , Xavier Gómez-Santacana
Current Neuropharmacology, 2016, 14 (5), pp.441-454. ⟨10.2174/1570159x13666150407231417⟩
Article dans une revue hal-02448289v1

New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III

Tri H. V. Huynh , Mette N. Erichsen , Amélie S. Tora , Cyril Goudet , Emmanuelle Sagot
Journal of Medicinal Chemistry, 2016, 59, pp.914-924. ⟨10.1021/acs.jmedchem.5b01333⟩
Article dans une revue hal-01288609v1

Determination of the absolute configuration of phosphinic analogues of glutamate

Bruno Commare , Delphine Rigault , Isabelle Lemasson , Patrick Deschamps , Alain Tomas
Organic & Biomolecular Chemistry, 2015, 13 (4), pp.1106-1112. ⟨10.1039/C4OB01960A⟩
Article dans une revue hal-02268872v1

Overlapping binding sites drive allosteric agonism and positive cooperativity in type 4 metabotropic glutamate receptors

Xavier Rovira , Fanny Malhaire , Pauline Scholler , Jordi Rodrigo , P. Gonzalez-Bulnes
FASEB Journal, 2015, 29 (1), pp.116--30. ⟨10.1096/fj.14-257287⟩
Article dans une revue hal-01943324v1

Editorial overview: Neurosciences: Targeting glutamatergic signaling in CNS diseases: new hopes?

Pierre Paoletti , Jean-Philippe Pin
Current Opinion in Pharmacology, 2015, 20, pp.iv-vi. ⟨10.1016/j.coph.2015.01.001⟩
Article dans une revue hal-02065120v1

Dynamics and modulation of metabotropic glutamate receptors

Philippe Rondard , Jean-Philippe Pin
Current Opinion in Pharmacology, 2015, 20, pp.95--101. ⟨10.1016/j.coph.2014.12.001⟩
Article dans une revue hal-01943325v1

Major ligand-induced rearrangement of the heptahelical domain interface in a GPCR dimer

Li Xue , Xavier Rovira , Pauline Scholler , Han Zhao , Jianfeng Liu
Nature Chemical Biology, 2015, 11 (2), pp.134--40. ⟨10.1038/nchembio.1711⟩
Article dans une revue hal-01943326v1

Allosteric modulation of metabotropic glutamate receptors by chloride ions

Amélie S. Tora , Xavier Rovira , Ibrahima Dione , Hugues-Olivier Bertrand , Isabelle Brabet
FASEB Journal, 2015, 29 (10), pp.4174-4188. ⟨10.1096/fj.14-269746⟩
Article dans une revue hal-02065116v1

Time-resolved FRET binding assay to investigate hetero-oligomer binding properties: proof of concept with dopamine D1/D3 heterodimer

Candide Hounsou , Jean-François Margathe , Nadia Oueslati , Abderazak Belhocine , Elodie Dupuis
ACS Chemical Biology, 2015, 10 (2), pp.466--74. ⟨10.1021/cb5007568⟩
Article dans une revue hal-01950133v1

Synthesis and studies on the mGluR agonist activity of FAP4 stereoisomers

Pavel Ivashkin , Gérald Lemonnier , Amélie S. Tora , Jean-Philippe Pin , Cyril Goudet
Bioorganic and Medicinal Chemistry Letters, 2015, 25 (12), pp.2523-2526. ⟨10.1016/j.bmcl.2015.04.043⟩
Article dans une revue hal-01180138v1
Image document

Untangling dopamine-adenosine receptor-receptor assembly in experimental parkinsonism in rats

V. Fernandez-Duenas , J. J. Taura , Martin Cottet , M. Gomez-Soler , M. Lopez-Cano
Disease Models & Mechanisms, 2015, 8 (1), pp.57--63. ⟨10.1242/dmm.018143⟩
Article dans une revue hal-01950131v1

Introduction

J. Bousquet , R. Bourret , T. Camuzat , P Augé , P. Domy
La Presse Médicale, 2015, 44, ⟨10.1016/j.lpm.2015.07.014⟩
Article dans une revue hal-02565513v1
Image document

Fine tuning of sub-millisecond conformational dynamics controls metabotropic glutamate receptors agonist efficacy

Linnea Olofsson , S. Felekyan , Etienne Doumazane , Pauline Scholler , Ludovic Fabre
Nature Communications, 2014, 5, pp.5206. ⟨10.1038/ncomms6206⟩
Article dans une revue hal-01943332v1
Image document

Homogeneous time-resolved fluorescence-based assay to monitor extracellular signal-regulated kinase signaling in a high-throughput format

Mohammed Akli Ayoub , Julien Trebaux , Julie Vallaghe , Fabienne Charrier-Savournin , Khaled Al-Hosaini
Frontiers in Endocrinology, 2014, 5, pp.94. ⟨10.3389/fendo.2014.00094⟩
Article dans une revue hal-01943335v1

The chemokine CXC4 and CC2 receptors form homo- and heterooligomers that can engage their signaling G-protein effectors and betaarrestin

Sylvain Armando , Julie Quoyer , Viktorya Lukashova , Arhamatoulaye Maiga , Yann Percherancier
FASEB Journal, 2014, 28 (10), pp.4509--23. ⟨10.1096/fj.13-242446⟩
Article dans une revue hal-01950128v1
Image document

G protein-coupled receptor oligomerization revisited: functional and pharmacological perspectives.

Sergi Ferré , Vicent Casadó , Lakshmi A. Devi , Marta Filizola , Ralf Jockers
Pharmacological Reviews, 2014, 66 (2), pp.413-34. ⟨10.1124/pr.113.008052⟩
Article dans une revue inserm-01067990v1

An allosteric modulator to control endogenous G protein-coupled receptors with light

S. Pittolo , X. Gomez-Santacana , K. Eckelt , Xavier Rovira , J. Dalton
Nature Chemical Biology, 2014, 10 (10), pp.813--5. ⟨10.1038/nchembio.1612⟩
Article dans une revue hal-01942934v1

Exploring the active conformation of cyclohexane carboxylate positive allosteric modulators of the type 4 metabotropic glutamate receptor

Xavier Rovira , Youssef Harrak , Ana Trapero , Patricia Gonzalez-Bulnes , Fanny Malhaire
ChemMedChem, 2014, 9 (12), pp.2685--98. ⟨10.1002/cmdc.201402190⟩
Article dans une revue hal-01943327v1
Image document

Complex GABAB receptor complexes: how to generate multiple functionally distinct units from a single receptor

Chanjuan Xu , Wenhua Zhang , Philippe Rondard , Jean-Philippe Pin , Jianfeng Liu
Frontiers in Pharmacology, 2014, 5, pp.12. ⟨10.3389/fphar.2014.00012⟩
Article dans une revue hal-01942936v1

Biased signaling through G-protein-coupled PROKR2 receptors harboring missense mutations

Oualid Sbai , Carine Monnier , Catherine Dode , Jean-Philippe Pin , Jean-Pierre Hardelin
FASEB Journal, 2014, 28 (8), pp.3734--44. ⟨10.1096/fj.13-243402⟩
Article dans une revue hal-01942940v1

Sensing of amino acids in a dopaminergic circuitry promotes rejection of an incomplete diet in Drosophila.

Marianne Bjordal , Nathalie Arquier , Julie Kniazeff , Jean-Philippe Pin , Pierre Léopold
Cell, 2014, 156 (3), pp.510-21. ⟨10.1016/j.cell.2013.12.024⟩
Article dans une revue hal-00968719v1
Image document

Alleviating Pain Hypersensitivity through Activation of Type 4 Metabotropic Glutamate Receptor

Bruno Vilar , Jérôme Busserolles , Bing Ling , Sophie Laffray , Lauriane Ulmann
Journal of Neuroscience, 2013, 33 (48), pp.18951-18965. ⟨10.1523/JNEUROSCI.1221-13.2013⟩
Article dans une revue hal-02448295v1

Group III and subtype 4 metabotropic glutamate receptor agonists: Discovery and pathophysiological applications in Parkinson's disease

Marianne Amalric , S. Lopez , C. Goudet , G. Fisone , G. Battaglia
Neuropharmacology, 2013, 66 (SI), pp.53-64. ⟨10.1016/j.neuropharm.2012.05.026⟩
Article dans une revue hal-01384098v1
Image document

Interaction of Protease-Activated Receptor 2 with G Proteins and beta-Arrestin 1 Studied by Bioluminescence Resonance Energy Transfer

Mohammed Akli Ayoub , Jean-Philippe Pin
Frontiers in Endocrinology, 2013, 4, pp.196. ⟨10.3389/fendo.2013.00196⟩
Article dans une revue hal-01984750v1

A novel selective metabotropic glutamate receptor 4 agonist reveals new possibilities for developing subtype selective ligands with therapeutic potential.

Cyril Goudet , Bruno Vilar , Tiphanie Courtiol , Thierry Deltheil , Thomas Bessiron
FASEB Journal, 2012, 26 (4), pp.1682-93. ⟨10.1096/fj.11-195941⟩
Article dans une revue hal-01182946v1

Structure and functional interaction of the extracellular domain of human GABAB receptor GBR2

Yong Geng , Dazhi Xiong , Lidia Mosyak , David Malito , Julie Kniazeff
Nature Neuroscience, 2012, 15 (7), pp.970-978. ⟨10.1038/nn.3133⟩
Article dans une revue hal-03363943v1

Des dimères et des oligomères de récepteurs couplés aux protéines G, oui mais pourquoi ?

Julie Kniazeff , Jean-Philippe Pin
Médecine/Sciences, 2012, 28 (10), pp.858-863. ⟨10.1051/medsci/20122810014⟩
Article dans une revue hal-03363918v1

Cinnabarinic Acid, an Endogenous Metabolite of the Kynurenine Pathway, Activates Type 4 Metabotropic Glutamate Receptors

F. Fazio , L. Lionetto , G. Molinaro , H. Bertrand , F. Acher
Molecular Pharmacology, 2012, 81 (5), pp.643-656. ⟨10.1124/mol.111.074765⟩
Article dans une revue hal-02448364v1

Α-amino-β-fluorocyclopropanecarboxylic acids as a new tool for drug development: synthesis of glutamic acid analogs and agonist activity towards metabotropic glutamate receptor 4.

Gérald Lemonnier , Cédric Lion , Jean-Charles Quirion , Jean-Philippe Pin , Cyril Goudet
Bioorganic and Medicinal Chemistry, 2012, 20 (15), pp.4716-26. ⟨10.1016/j.bmc.2012.06.006⟩
Article dans une revue hal-00996602v1

Stability of GABA B receptor oligomers revealed by dual TR‐FRET and drug‐induced cell surface targeting

Laëtitia Comps‐agrar , Julie Kniazeff , Carsten Brock , Eric Trinquet , Jean-Philippe Pin
FASEB Journal, 2012, 26 (8), pp.3430-3439. ⟨10.1096/fj.12-203646⟩
Article dans une revue hal-03363950v1
Image document

G Protein Activation by Serotonin Type 4 Receptor Dimers: evidence that turning on two protomers is more efficient.

Lucie P. Pellissier , Gaël Barthet , Florence Gaven , Elisabeth Cassier , Eric Trinquet
Journal of Biological Chemistry, 2011, 286 (12), pp.9985-9997. ⟨10.1074/jbc.M110.201939⟩
Article dans une revue hal-02482879v1

A new Selective Metabotropic Glutamate Receptor type 4 Agonist Reveals New ways to Develop Subtype Selective Orthosteric Ligands with Potential Therapeutic Effects

Cyril Goudet , Bruno Vilar , Tiphanie Courtiol , Thierry Deltheil , Thomas Bessiron
Current Neuropharmacology, 2011, 9 (1), pp.26
Article dans une revue hal-01384798v1
Image document

IUPHAR-DB: the IUPHAR database of G protein-coupled receptors and ion channels

Anthony J. Harmar , Rebecca A. Hills , Edward M. Rosser , Martin Jones , O. Peter Buneman
Nucleic Acids Research, 2009, 37, pp.D680-D685. ⟨10.1093/nar/gkn728⟩
Article dans une revue hal-02667062v1

Metabotropic glutamate receptor subtype 4 selectively modulates both glutamate and GABA transmission in the striatum: implications for Parkinson's disease treatment

D. Cuomo , G. Martella , E. Barabino , P. Platania , D. Vita
Journal of Neurochemistry, 2009, 109, pp.1096-1105
Article dans une revue hal-00409236v1

A novel series of group III metabotropic glutamate receptor (mGluR) agonists

Francine C. Acher , C. Selvam , N. Triballeau , N. Oueslati , I. Lemasson
Abstracts of Papers of the American Chemical Society, 2009, 237
Article dans une revue hal-01384834v1

Is metabotropic glutamate receptor mGlu4R a good target to treat Parkinson's disease symptoms? Design and evaluation of potent and selective agonists

Isabelle A. Lemasson , Chelliah Selvam , Nadia Oueslati , Isabelle Brabet , Tiphanie Courtiol
Abstracts of Papers of the American Chemical Society, 2009, 238
Article dans une revue hal-01384832v1

Electrophysiological and behavioral evidence that modulation of metabotropic glutamate receptor 4 with a new agonist reverses experimental parkinsonism

C. Beurrier , S. Lopez , D. Revy , C. Selvam , C. Goudet
FASEB Journal, 2009, 23, pp.3619-3628
Article dans une revue hal-00582954v1
Image document

Cell surface protein-protein interaction analysis with combined time-resolved FRET and snap-tag technologies: application to GPCR oligomerization

Damien Maurel , Laetitia Comps-Agrar , Carsten Brock , Marie-Laure Rives , Emmanuel Bourrier
Nature Methods, 2008, 5 (6), pp.561. ⟨10.1038/nmeth.1213⟩
Article dans une revue hal-00318856v1
Image document

Functioning of the dimeric GABA(B) receptor extracellular domain revealed by glycan wedge scanning.

Philippe Rondard , Siluo Huang , Carine Monnier , Haijun Tu , Bertrand Blanchard
EMBO Journal, 2008, 27 (9), pp.1321-1332. ⟨10.1038/emboj.2008.64⟩
Article dans une revue hal-00318880v1
Image document

Modeling the binding and function of metabotropic glutamate receptors.

Xavier Rovira , David Roche , Juan Serra , Julie Kniazeff , Jean-Philippe Pin
Journal of Pharmacology and Experimental Therapeutics, 2008, 325 (2), pp.443-56. ⟨10.1124/jpet.107.133967⟩
Article dans une revue hal-00319020v1

N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors.

Yelin Chen , Cyril Goudet , Jean-Philippe Pin , P Jeffrey Conn
Molecular Pharmacology, 2008, 73 (3), pp.909-18. ⟨10.1124/mol.107.040097⟩
Article dans une revue inserm-00318958v1
Image document

Surface expression of metabotropic glutamate receptor variants mGluR1a and mGluR1b in transfected HEK293 cells.

Jiri Kumpost , Zdenka Syrova , Lenka Kulihova , Daniela Frankova , Jean-Charles Bologna
Neuropharmacology, 2008, 55 (4), pp.409-18. ⟨10.1016/j.neuropharm.2008.06.073⟩
Article dans une revue inserm-00319023v1
Image document

Amino-pyrrolidine tricarboxylic acids give new insight into group III metabotropic glutamate receptor activation mechanism.

Mélanie Frauli , Nadia Hubert , Stephan Schann , Nicolas Triballeau , Hugues-Olivier Bertrand
Molecular Pharmacology, 2007, 71 (3), pp.704-12. ⟨10.1124/mol.106.030254⟩
Article dans une revue inserm-00318866v1
Image document

Dominant role of GABAB2 and Gbetagamma for GABAB receptor-mediated-ERK1/2/CREB pathway in cerebellar neurons.

Haijun Tu , Philippe Rondard , Chanjuan Xu , Federica Bertaso , Fangli Cao
Cellular Signalling, 2007, 19 (9), pp.1996-2002. ⟨10.1016/j.cellsig.2007.05.004⟩
Article dans une revue hal-00319022v1
Image document

Real-time analysis of agonist-induced activation of protease-activated receptor 1/Galphai1 protein complex measured by bioluminescence resonance energy transfer in living cells.

Mohammed Akli Ayoub , Damien Maurel , Virginie Binet , Michel Fink , Laurent Prézeau
Molecular Pharmacology, 2007, 71 (5), pp.1329-40. ⟨10.1124/mol.106.030304⟩
Article dans une revue hal-00318930v1
Image document

L-(+)-2-Amino-4-thiophosphonobutyric acid (L-thioAP4), a new potent agonist of group III metabotropic glutamate receptors: increased distal acidity affords enhanced potency.

Chelliah Selvam , Cyril Goudet , Nadia Oueslati , Jean-Philippe Pin , Francine C. Acher
Journal of Medicinal Chemistry, 2007, 50 (19), pp.4656-64. ⟨10.1021/jm070400y⟩
Article dans une revue inserm-00318965v1
Image document

Group III metabotropic glutamate receptors inhibit hyperalgesia in animal models of inflammation and neuropathic pain

Cyril Goudet , Eric Chapuy , Abdelkrim Alloui , Francine Acher , Jean-Philippe Pin
Pain, 2007, 137 (1), pp.112-124. ⟨10.1016/j.pain.2007.08.020⟩
Article dans une revue inserm-00318859v1
Image document

Common structural requirements for heptahelical domain function in class A and class C G protein-coupled receptors.

Virginie Binet , Béatrice Duthey , Jennifer Lecaillon , Claire Vol , Julie Quoyer
Journal of Biological Chemistry, 2007, 282 (16), pp.12154-63. ⟨10.1074/jbc.M611071200⟩
Article dans une revue inserm-00318820v1
Image document

Synthesis and biological evaluation of 1-amino-2-phosphonomethylcyclopropanecarboxylic acids, new group III metabotropic glutamate receptor agonists.

Pauline Sibille , Sébastien Lopez , Isabelle Brabet , Ornella Valenti , Nadia Oueslati
Journal of Medicinal Chemistry, 2007, 50 (15), pp.3585-95. ⟨10.1021/jm070262c⟩
Article dans une revue inserm-00318976v1

Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses.

Yelin Chen , Yi Nong , Cyril Goudet , Kamondanai Hemstapat , Tomas de Paulis
Molecular Pharmacology, 2007, 71 (5), pp.1389-98. ⟨10.1124/mol.106.032425⟩
Article dans une revue inserm-00319012v1
Image document

Activation of a Dimeric Metabotropic Glutamate Receptor by Inter-Subunit Rearrangement

Carsten Brock , Nadia Oueslati , Stéphan Soler , Laure Boudier , Philippe Rondard
Journal of Biological Chemistry, 2007, 282 (45), pp.33000. ⟨10.1074/jbc.M702542200⟩
Article dans une revue hal-00318871v1

D-myo-inositol 1-phosphate as a surrogate of D-myo-inositol 1,4,5-tris phosphate to monitor G protein-coupled receptor activation.

Eric Trinquet , Michel Fink , Hervé Bazin , Florence Grillet , Fabrice Maurin
Analytical Biochemistry, 2006, 358 (1), pp.126-35. ⟨10.1016/j.ab.2006.08.002⟩
Article dans une revue inserm-00318996v1
Image document

Among the twenty classical L-amino acids, only glutamate directly activates metabotropic glutamate receptors.

Mélanie Frauli , Pascal Neuville , Claire Vol , Jean-Philippe Pin , Laurent Prézeau
Neuropharmacology, 2006, 50 (2), pp.245-53. ⟨10.1016/j.neuropharm.2005.09.016⟩
Article dans une revue inserm-00318879v1

Identification and characterization of Hedgehog modulator properties after functional coupling of Smoothened to G15.

Christelle Masdeu , Hélène Faure , Josée Coulombe , Angèle Schoenfelder , André Mann
Biochemical and Biophysical Research Communications, 2006, 349 (2), pp.471-9. ⟨10.1016/j.bbrc.2006.07.216⟩
Article dans une revue hal-00105551v1

Asymmetry conformational changes in a GPCR dimer controlled by G-proteins

Marjorie Damian , Aimée Martin , Danielle Mesnier , Jean-Philippe Pin , Jean-Louis Banères
EMBO Journal, 2006, 25 (24), pp.5693-5702. ⟨10.1038/sj.emboj.7601449⟩
Article dans une revue hal-00176784v1
Image document

Assembly-dependent surface targeting of the heterodimeric GABAB Receptor is controlled by COPI but not 14-3-3.

Carsten Brock , Laure Boudier , Damien Maurel , Jaroslav Blahos , Jean-Philippe Pin
Molecular Biology of the Cell, 2005, 16 (12), pp.5572-8. ⟨10.1091/mbc.E05-05-0400⟩
Article dans une revue hal-00318967v2
Image document

Asymmetric functioning of dimeric metabotropic glutamate receptors disclosed by positive allosteric modulators.

Cyril Goudet , Julie Kniazeff , Veronika Hlavackova , Fanny Malhaire , Damien Maurel
Journal of Biological Chemistry, 2005, 280 (26), pp.24380-5. ⟨10.1074/jbc.M502642200⟩
Article dans une revue inserm-00318925v1

Allosteric functioning of dimeric class C G-protein-coupled receptors.

Jean-Philippe Pin , Julie Kniazeff , Jianfeng Liu , Virginie Binet , Cyril Goudet
FEBS Journal, 2005, 272, pp.2947-55. ⟨10.1111/j.1742-4658.2005.04728.x⟩
Article dans une revue inserm-00094959v1
Image document

Evidence for a single heptahelical domain being turned on upon activation of a dimeric GPCR.

Veronika Hlavackova , Cyril Goudet , Julie Kniazeff , Alice Zikova , Damien Maurel
EMBO Journal, 2005, 24 (3), pp.499-509. ⟨10.1038/sj.emboj.7600557⟩
Article dans une revue inserm-00318934v1
Image document

Locking the dimeric GABA(B) G-protein-coupled receptor in its active state.

Julie Kniazeff , Pierre-Philippe Saintot , Cyril Goudet , Jianfeng Liu , Annie Charnet
Journal of Neuroscience, 2004, 24 (2), pp.370-7. ⟨10.1523/JNEUROSCI.3141-03.2004⟩
Article dans une revue hal-00319013v1
Image document

Cell surface detection of membrane protein interaction with homogeneous time-resolved fluorescence resonance energy transfer technology.

Damien Maurel , Julie Kniazeff , Gérard Mathis , Eric Trinquet , Jean-Philippe Pin
Analytical Biochemistry, 2004, 329 (2), pp.253-62. ⟨10.1016/j.ab.2004.02.013⟩
Article dans une revue hal-00318979v1
Image document

Molecular determinants involved in the allosteric control of agonist affinity in the GABAB receptor by the GABAB2 subunit.

Jianfeng Liu , Damien Maurel , Sébastien Etzol , Isabelle Brabet , Hervé Ansanay
Journal of Biological Chemistry, 2004, 279 (16), pp.15824-30. ⟨10.1074/jbc.M313639200⟩
Article dans une revue hal-00319008v1
Image document

The heptahelical domain of GABA(B2) is activated directly by CGP7930, a positive allosteric modulator of the GABA(B) receptor.

Virginie Binet , Carole Brajon , Laurent Le Corre , Francine Acher , Jean-Philippe Pin
Journal of Biological Chemistry, 2004, 279 (28), pp.29085-91. ⟨10.1074/jbc.M400930200⟩
Article dans une revue inserm-00318926v1
Image document

Heptahelical domain of metabotropic glutamate receptor 5 behaves like rhodopsin-like receptors.

Cyril Goudet , Florence Gaven , Julie Kniazeff , Claire Vol , Jianfeng Liu
Proceedings of the National Academy of Sciences of the United States of America, 2004, 101 (1), pp.378-83. ⟨10.1073/pnas.0304699101⟩
Article dans une revue inserm-00319003v1
Image document

Closed state of both binding domains of homodimeric mGlu receptors is required for full activity.

Julie Kniazeff , Anne-Sophie Bessis , Damien Maurel , Hervé Ansanay , Laurent Prézeau
Nature Structural and Molecular Biology, 2004, 11 (8), pp.706-13. ⟨10.1038/nsmb794⟩
Article dans une revue hal-00318999v1
Image document

Divergent Evolution in Metabotropic Glutamate Receptors

Christian Mitri , Marie-Laure Parmentier , Jean-Philippe Pin , Joël Bockaert , Yves Grau
Journal of Biological Chemistry, 2004, 279 (10), pp.9313-9320. ⟨10.1074/jbc.M310878200⟩
Article dans une revue hal-02506712v1

Homer-dependent cell surface expression of metabotropic glutamate receptor type 5 in neurons

Fabrice Ango , David Robbe , J.C. Tu , B. Xiao , P.F. Worley
Molecular and Cellular Neuroscience, 2002, 20, pp.323-329. ⟨10.1006/mcne.2002.1100⟩
Article dans une revue hal-00016884v1

A single olfactory receptor specifically binds a set of odorant molecules

Isabelle Gaillard , Sylvie Rouquier , Jean-Philippe Pin , Patrice Mollard , Sylvain Richard
European Journal of Neuroscience, 2002, 15 (3), pp.409-418. ⟨10.1046/j.0953-816x.2001.01871.x⟩
Article dans une revue hal-02948481v1
Image document

A single subunit (GB2) is required for G-protein activation by the heterodimeric GABA(B) receptor.

Béatrice Duthey , Sara Caudron , Julie Perroy , Bernhard Bettler , Laurent Fagni
Journal of Biological Chemistry, 2002, 277 (5), pp.3236-41. ⟨10.1074/jbc.M108900200⟩
Article dans une revue inserm-00318936v1

Agonist-independent activation of metabotropic glutamate receptors by the intracellular protein Homer.

Fabrice Ango , Laurent Prézeau , Thomas Muller , Jian C. Tu , Bo Xiao
Nature, 2001, 411 (6840), pp.962-5. ⟨10.1038/35082096⟩
Article dans une revue inserm-00318959v1
Image document

The C terminus of the metabotropic glutamate receptor subtypes 2 and 7 specifies the receptor signaling pathways

Julie Perroy , G. J. Gutierrez , V. Coulon , Joël Bockaert , Jean-Philippe Pin
Journal of Biological Chemistry, 2001, 276 (49), pp.45800--45805. ⟨10.1074/jbc.M106876200⟩
Article dans une revue hal-02197463v1
Image document

BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity.

Fiona Y. Carroll , Andreas Stolle , Philip M. Beart , Arnd Voerste , Isabelle Brabet
Molecular Pharmacology, 2001, 59 (5), pp.965-73. ⟨10.1124/mol.59.5.965⟩
Article dans une revue inserm-00319007v1

Aminobicyclo (2.2.1.)heptane dicarboxylic acids (ABHD), rigid analogs of ACPD and glutamic acid: synthesis and pharmacological activity on metabotropic receptors mGluR1 and mGluR2

Frederique Tellier , Francine Acher , I. Brabet , J.-P. Pin
Bioorganic and Medicinal Chemistry, 1998, 6, pp.195-208
Article dans une revue hal-02691001v1

Conformational analysis of glutamic acid analogues as probes of glutamate receptors using molecular modelling and NMR methods. Comparison with specific agonists

Nathalie Todeschi , Josyane Gharbi-Benarous , Francine Acher , Valery Laure , Jean-Philippe Pin
Bioorganic and Medicinal Chemistry Letters, 1997, 5 (2), pp.335-352. ⟨10.1016/s0968-0896(96)00252-0⟩
Article dans une revue hal-02356241v1

Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids : new tools to discriminate between metabotropic glutamate receptor subtypes

Francine C. Acher , Frédérique Tellier , Robert Azerad , Isabelle N. Brabet , Laurent Fagni
Journal of Medicinal Chemistry, 1997, 40, pp.3119-3129
Article dans une revue hal-02694452v1

Synthesis of conformationally-constrained analogs of glutamic acid as structural probes of glutamatergic receptors

Frederique Tellier , Francine Acher , I. Brabet , J.-P. Pin , J. Bockaert
Comptes rendus de l’Académie des sciences. Série 2, 1995, 321, pp.385-392
Article dans une revue hal-02705357v1

Synthesis of conformationally-constrained stereospecific analogs of glutamic acid as antagonists of metabotropic receptors

Frederique Tellier , Francine Acher , I. Brabet , J.-P. Pin , J. Bockaert
Bioorganic and Medicinal Chemistry Letters, 1995, 5 (22), pp.2627-2632
Article dans une revue hal-02705336v1
Image document

HTRF® total and phospho-YAP(Ser127) cellular assays

Diana Zindel , Claire Vol , Odile Lecha , Isabelle Bourquignon , Merve Bilgic
The Hippo pathway: Methods and Protocols, 1893, pp.153-166, 2019, Methods in Molecular Biology, ⟨10.1007/978-1-4939-8910-2_13⟩
Chapitre d'ouvrage hal-02396286v1
Image document

Time-resolved FRET based assays to characterize hetero-oligomer pharmacology

Joyce Heuninck , Candide Hounsou , Elodie Dupuis , Eric Trinquet , Bernard Mouillac
Mario Tiberi. G Protein-Coupled Receptor Signaling: Methods and Protocols, 1947, Springer New York, pp.151-168, 2019, Methods in Molecular Biology, 978-1-4939-9120-4. ⟨10.1007/978-1-4939-9121-1_8⟩
Chapitre d'ouvrage hal-03563498v1

Fluorescent-Based Strategies to Investigate G Protein-Coupled Receptors: Evolution of the Techniques to a Better Understanding

Orestis Faklaris , Joyce Heuninck , Amandine Falco , Elise Goyet , Jurriaan M. Zwier
Structure and Function of GPCRs, pp.217-252, 2017, ⟨10.1007/7355_2017_2⟩
Chapitre d'ouvrage hal-02391215v1

Time-Resolved FRET Strategy to Screen GPCR Ligand Library

Nadia Oueslati , Candide Hounsou , Abderazak Belhocine , Thieric Rodriguez , Elodie Dupuis
Methods in Molecular Biology, 1272, pp.23-36, 2015, ⟨10.1007/978-1-4939-2336-6_2⟩
Chapitre d'ouvrage hal-02068533v1

Time-Resolved Förster Resonance Energy Transfer-Based Technologies to Investigate G Protein-Coupled Receptor Machinery

Pauline Scholler , Jurriaan Zwier , Eric Trinquet , Philippe Rondard , Jean-Philippe Pin
Fluorescence-Based Biosensors - From Concepts to Applications, 113, Elsevier, pp.275-312, 2013, Progress in Molecular Biology and Translational Science, ⟨10.1016/B978-0-12-386932-6.00007-7⟩
Chapitre d'ouvrage hal-03363917v1