Dernières Publications

Articles

• Novel Inhibitory Site Revealed by XAP044 Mode of Action on the Metabotropic Glutamate 7 Receptor Venus Flytrap Domain.
  Cristiano N, Cabayé A, Brabet I, Glatthar R, Tora A, Goudet C, Bertrand HO, Goupil-Lamy A, Flor PJ, Pin JP, McCort-Tranchepain I, Acher FC : J Med Chem, 2024
• Epitope Identification of an mGlu5 Receptor Nanobody Using Physics-Based Molecular Modeling and Deep Learning Techniques.
  Eshak F, Pion L, Scholler P, Nevoltris D, Chames P, Rondard P, Pin JP, Acher FC, Goupil-Lamy A : J Chem Inf Model, 2024
• Design, Synthesis, Pharmacology, and In Silico Studies of (1S,2S,3S)-2-((S)-Amino(carboxy)methyl)-3-(carboxymethyl)cyclopropane-1-carboxylic Acid (LBG30300): A Picomolar Potency Subtype-Selective mGlu(2) Receptor Agonist.
  Liu N, Eshak F, Malhaire F, Brabet I, Prézeau L, Renard E, Pin JP, Acher FC, Staudt M, Bunch L : J Med Chem, 2024
• Metabotropic glutamate receptor orthosteric ligands and their binding sites.
  Acher FC, Cabayé A, Eshak F, Goupil-Lamy A, Pin JP : Neuropharmacology, 2022
• A nanobody activating metabotropic glutamate receptor 4 discriminates between homo- and heterodimers.
  Haubrich J, Font J, Quast RB, Goupil-Lamy A, Scholler P, Nevoltris D, Acher F, Chames P, Rondard P, Prézeau L, Pin JP : Proc Natl Acad Sci U S A, 2021
• LSP2-9166, an orthosteric mGlu4 and mGlu7 receptor agonist, reduces cocaine self-administration under a progressive ratio schedule in rats.
  De Sa Nogueira D, Bourdy R, Filliol D, Quessada C, McCort-Tranchepain I, Acher F, Zwiller J, Romieu P, Befort K : Neurosci Lett, 2021
• Antidepressant efficacy of a selective organic cation transporter blocker in a mouse model of depression.
  Orrico-Sanchez A, Chausset-Boissarie L, Alves de Sousa R, Coutens B, Rezai Amin S, Vialou V, Louis F, Hessani A, Dansette PM, Zornoza T, Gruszczynski C, Giros B, Guiard BP, Acher F, Pietrancosta N, Gautron S : Mol Psychiatry, 2020
• Illuminating the allosteric modulation of the calcium-sensing receptor.
  Liu H, Yi P, Zhao W, Wu Y, Acher F, Pin JP, Liu J, Rondard P : Proc Natl Acad Sci U S A, 2020
• LSP5-2157 a new inhibitor of vesicular glutamate transporters.
  Poirel O, Mamer LE, Herman MA, Arnulf-Kempcke M, Kervern M, Potier B, Miot S, Wang J, Favre-Besse FC, Brabet I, Laras Y, Bertrand HO, Acher F, Pin JP, Puel JL, Giros B, Epelbaum J, Rosenmund C, Dutar P, Daumas S, El Mestikawy S, Pietrancosta N : Neuropharmacology, 2020
• Asc-1 Transporter (SLC7A10): Homology Models And Molecular Dynamics Insights Into The First Steps Of The Transport Mechanism.
  Mikou A, Cabayé A, Goupil A, Bertrand HO, Mothet JP, Acher FC : Sci Rep, 2020
• Amino Acids Bearing Aromatic or Heteroaromatic Substituents as a New Class of Ligands for the Lysosomal Sialic Acid Transporter Sialin.
  Dubois L, Pietrancosta N, Cabaye A, Fanget I, Debacker C, Gilormini PA, Dansette PM, Dairou J, Biot C, Froissart R, Goupil-Lamy A, Bertrand HO, Acher FC, McCort-Tranchepain I, Gasnier B, Anne C : J Med Chem, 2020
• Conformational pathway provides unique sensitivity to a synaptic mGluR.
  Habrian CH, Levitz J, Vyklicky V, Fu Z, Hoagland A, McCort-Tranchepain I, Acher F, Isacoff EY : Nat Commun, 2019
• Infiltrating Myeloid Cells Drive Osteosarcoma Progression via GRM4 Regulation of IL23.
  Kansara M, Thomson K, Pang P, Dutour A, Mirabello L, Acher F, Pin JP, Demicco EG, Yan J, Teng MWL, Smyth MJ, Thomas DM : Cancer Discov, 2019
• The mGlu7 receptor provides protective effects against epileptogenesis and epileptic seizures.
  Girard B, Tuduri P, Moreno MP, Sakkaki S, Barboux C, Bouschet T, Varrault A, Vitre J, McCort-Tranchepain I, Dairou J, Acher F, Fagni L, Marchi N, Perroy J, Bertaso F : Neurobiol Dis, 2019
• Chloride ions stabilize the glutamate-induced active state of the metabotropic glutamate receptor 3.
  Tora AS, Rovira X, Cao AM, Cabayé A, Olofsson L, Malhaire F, Scholler P, Baik H, Van Eeckhaut A, Smolders I, Rondard P, Margeat E, Acher F, Pin JP, Goudet C : Neuropharmacology, 2018
• Profiling of orthosteric and allosteric group-III metabotropic glutamate receptor ligands on various G protein-coupled receptors with Tag-lite assays.
  Belhocine A, Veglianese P, Hounsou C, Dupuis E, Acher F, Durroux T, Goudet C, Pin JP : Neuropharmacology, 2018
• Mutual activation of glutamatergic mGlu and muscarinic M receptors reverses schizophrenia-related changes in rodents.
  Cieślik P, Woźniak M, Rook JM, Tantawy MN, Conn PJ, Acher F, Tokarski K, Kusek M, Pilc A, Wierońska JM : Psychopharmacology (Berl), 2018
• Dynamic modulation of inflammatory pain-related affective and sensory symptoms by optical control of amygdala metabotropic glutamate receptor 4.
  Zussy C, Gómez-Santacana X, Rovira X, De Bundel D, Ferrazzo S, Bosch D, Asede D, Malhaire F, Acher F, Giraldo J, Valjent E, Ehrlich I, Ferraguti F, Pin JP, Llebaria A, Goudet C : Mol Psychiatry, 2018
• Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.
  Selvam C, Lemasson IA, Brabet I, Oueslati N, Karaman B, Cabaye A, Tora AS, Commare B, Courtiol T, Cesarini S, McCort-Tranchepain I, Rigault D, Mony L, Bessiron T, McLean H, Leroux FR, Colobert F, Daniel H, Goupil-Lamy A, Bertrand HO, Goudet C, Pin JP, Acher FC : J Med Chem, 2018
• Pharmacological activation of mGlu4 and mGlu7 receptors, by LSP2-9166, reduces ethanol consumption and relapse in rat.
  Lebourgeois S, Vilpoux C, Jeanblanc J, Acher F, Marie N, Noble F, Naassila M : Neuropharmacology, 2018
• Role of mGlu7 receptor in morphine rewarding effects is uncovered by a novel orthosteric agonist.
  Hajasova Z, Canestrelli C, Acher F, Noble F, Marie N : Neuropharmacology, 2018
• Neurochemical and behavioral studies on the 5-HT-dependent antipsychotic action of the mGlu receptor agonist LSP4-2022.
  Woźniak M, Gołembiowska K, Noworyta-Sokołowska K, Acher F, Cieślik P, Kusek M, Tokarski K, Pilc A, Wierońska JM : Neuropharmacology, 2017
• Involvement of GABAB Receptor Signaling in Antipsychotic-like Action of the Novel Orthosteric Agonist of the mGlu4 Receptor, LSP4-2022.
  Woźniak M, Acher F, Marciniak M, Lasoń-Tyburkiewicz M, Gruca P, Papp M, Pilc A, Wierońska JM : Curr Neuropharmacol, 2016
• Phasic and Tonic mGlu7 Receptor Activity Modulates the Thalamocortical Network.
  Tassin V, Girard B, Chotte A, Fontanaud P, Rigault D, Kalinichev M, Perroy J, Acher F, Fagni L, Bertaso F : Front Neural Circuits, 2016
• Determination of the absolute configuration of phosphinic analogues of glutamate
  Commare B, Rigault D, Lemasson IA, Deschamps P, Tomas A, Roussel P, Brabet I, Goudet C, Pin JP, Leroux FR, Colobert F, Acher FC : Org Biomol Chem, 2015
• Two-photon caging groups: effect of position isomery on the photorelease properties of aminoquinoline-derived photolabile protecting groups
  Tran C, Gallavardin T, Petit M, Slimi R, Dhimane H, Blanchard-Desce M, Acher FC, Ogden D, Dalko PI : Org Lett, 2015
• Design, synthesis and biological evaluation of small-azo-dyes as potent Vesicular Glutamate Transporters inhibitors.
  Favre-Besse FC, Poirel O, Bersot T, Kim-Grellier E, Daumas S, El Mestikawy S, Acher FC, Pietrancosta N : Eur J Med Chem, 2014
• Molecular determinants of agonist selectivity in glutamate-gated chloride channels which likely explain the agonist selectivity of the vertebrate glycine and GABAA-ρ receptors.
  Blarre T, Bertrand HO, Acher FC, Kehoe J : PLoS One, 2014
• Tandem triad systems based on FRET for two-photon induced release of glutamate.
  Picard S, Cueto-Diaz EJ, Genin E, Clermont G, Acher F, Ogden D, Blanchard-Desce M : Chem Commun (Camb), 2013
• Variations on glutamate binding in channel-gated receptors.
  Acher FC : Structure, 2013
• The antipsychotic-like effects of the mGlu group III orthosteric agonist, LSP1-2111, involves 5-HT1A signalling.
  Wierońska JM, Acher FC, Sławińska A, Gruca P, Lasoń-Tyburkiewicz M, Papp M, Pilc A : Psychopharmacology, 2013
• Substitution effect on the one- and two-photon sensitivity of DMAQ
  Petit M, Tran C, Roger T, Gallavardin T, Dhimane H, Palma-Cerda F, Blanchard-Desce M, Acher FC, Ogden D, Dalko PI : Org Lett, 2012
• Opposing efficacy of group III mGlu receptor activators, LSP1-2111 and AMN082, in animal models of positive symptoms of schizophrenia.
  Wierońska JM, Stachowicz K, Acher F, Lech T, Pilc A : Psychopharmacology, 2012
• A novel selective metabotropic glutamate receptor 4 agonist reveals new possibilities for developing subtype selective ligands with therapeutic potential.
  Goudet C, Vilar B, Courtiol T, Deltheil T, Bessiron T, Brabet I, Oueslati N, Rigault D, Bertrand HO, McLean H, Daniel H, Amalric M, Acher F, Pin JP : FASEB J, 2012
• Cinnabarinic acid, an endogenous metabolite of the kynurenine pathway, activates type 4 metabotropic glutamate receptors.
  Fazio F, Lionetto L, Molinaro G, Bertrand HO, Acher F, Ngomba RT, Notartomaso S, Curini M, Rosati O, Scarselli P, Di Marco R, Battaglia G, Bruno V, Simmaco M, Pin JP, Nicoletti F, Goudet C : Mol Pharmacol, 2012
• Successful prediction of substrate-binding pocket in SLC17 transporter sialin. (PDF)
  Pietrancosta N, Anne C, Prescher H, Ruivo R, Sagné C, Debacker C, Bertrand HO, Brossmer R, Acher F, Gasnier B : J Biol Chem, 2012
• Orthosteric versus allosteric GPCR activation: the great challenge of group-III mGluRs.
  Flor PJ, Acher FC : Biochem Pharmacol, 2012
• Group III and subtype 4 metabotropic glutamate receptor agonists: discovery and pathophysiological applications in Parkinson’s disease.
  Amalric M, Lopez S, Goudet C, Fisone G, Battaglia G, Nicoletti F, Pin JP, Acher FC : Neuropharmacology, 2012
• Role of mGluR4 in acquisition of fear learning and memory.
  Davis MJ, Iancu OD, Acher FC, Stewart BM, Eiwaz MA, Duvoisin RM, Raber J : Neuropharmacology, 2012
• Synthesis of quinoline dicarboxylic esters as biocompatible fluorescent tags.
  Laras Y, Hugues V, Chandrasekaran Y, Blanchard-Desce M, Acher FC, Pietrancosta N : J Org Chem, 2012
• A critical pocket close to the glutamate binding site of mGlu receptors opens new possibilities for agonist design.
  Acher FC, Selvam C, Pin JP, Goudet C, Bertrand HO : Neuropharmacology, 2011
• Rose Bengal analogs and vesicular glutamate transporters (VGLUTs)
  Pietrancosta N, Kessler A, Favre-Besse F-C, Triballeau N, Quentin T, Giros B, El Mestikawy S, Acher F C : Bioorganic \& medicinal chemistry, 2010
• Identification of a novel NR2B-selective NMDA receptor antagonist using a virtual screening approach
  Mony L, Triballeau N, Paoletti P, Acher F C, Bertrand H-O : Bioorganic \& medicinal chemistry letters, 2010
• A virtual screening hit reveals new possibilities for developing group III metabotropic glutamate receptor agonists
  Selvam C, Oueslati N, Lemasson IA, Brabet I, Rigault D, Courtiol T, Cesarini S, Triballeau N, Bertrand HO, Goudet C, Pin JP, Acher FC : J Med Chem, 2010
• Aplysia cys-loop glutamate-gated chloride channels reveal convergent evolution of ligand specificity
  Kehoe J, Buldakova S, Acher F, Dent J, Bregestovski P, Bradley J : J Mol Evol, 2009
• High-potency olfactory receptor agonists discovered by virtual high-throughput screening: molecular probes for receptor structure and olfactory function
  Triballeau N, Van Name E, Laslier G, Cai D Paillard G Sorensen PW, Hoffmann R, Bertrand HO, Ngai J, Acher FC : Neuron, 2008

Chapitre

• Modulation of Metabotropic Glutamate Receptors by Orthosteric, Allosteric, and Light-Operated Ligands
  Goudet C, Rovira X, Rondard P, Pin J-P, Llebaria A, Acher F : extrait de Structure and Function of GPCRs Guillaume Lebon – Springer, pages 253–284, ISBN:978-3-030-24589-4, 2019