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Publications
 Selvam, C. ; Oueslati, N ; Lemasson, I. A. ; Brabet, I. ; Rigault, D. ; Courtiol, T. ; Cesarini, S. ; Triballeau, N. ; Bertrand, H.-O. ; Goudet, C. ; Pin, JP. ; Acher, F.C. A virtual screening hit reveals new possibilities to develop group III metabotropic glutamate receptor agonists J.Med.Chem. 2010 in press.
Kehoe, J. ; Buldakova, S. ; Acher F. ; Dent, J. ; Bregestovski, P. ; Bradley, J. Aplysia cys-loop glutamate-gated chloride channels reveal convergent evolution of ligand specificity. J Mol Evol. 2009, 69, 125-141.
Beurrier, C. ; Lopez, S. ; Révy, D. ; Selvam, C. ; Goudet, C., Lhérondel, M., Gubellini, P., Kerkerian-LeGoff, L., Acher, F., Pin, JP., Amalric, M. Electrophysiological and behavioral evidences that modulation of metabotropic glutamate receptor 4 with a new agonist reverses experimental parkinsonism. FASEB J. 2009, Jun 12. [Epub ahead of print].
Cuomo, D., Martella, G., Barabino, E., Platania, P. ;Vita, D., Madeo, G., Selvam, C., Goudet, C., Oueslati, N., Pin, JP., Acher, F., Pisani, A., Beurrier, C., Melon, C., Kerkerian-Le Goff, L, Gubellini, P. Metabotropic glutamate receptor subtype 4 selectively modulates both glutamate and GABA transmission in the striatum : implications for Parkinson’s disease treatment. J.Neurochem. 2009, 109, 1096-1105.
Mony, L. ; Krzaczkowski, L. ; Léonetti, M. ; Le Goff, A. ; Alarcon, K. ; Neyton, J. ; Bertrand, H.-O. ; Acher, F. ; Paoletti, P. Structural basis of NR2B-selective antagonist recognition by NMDA receptors. Mol. Pharmacol. 2009, 75, 60-74.
Triballeau, N. ; Van Name, E. ; Laslier, G. ; Cai, D. ; Paillard, G. ; Sorensen, P. W. ; Hoffmann, R. ; Bertrand, H.-O. ; Ngai, J. ; Acher, F. C. High potency olfactory receptor agonists discovered by virtual high-throughput screening : molecular probes for receptor structure and olfactory function. Neuron, 2008, 60, 761-771.
Abitbol, K. ; Acher, F. ; Daniel, H. Depression of excitatory transmission at PF-PC synapse by group III metabotropic glutamate receptors is provided exclusively by mGluR4 in the rodent cerebellar cortex. J. Neurochem. 2008,105, 2069-2079.
Cottyn, B. ; Acher, F. ; Ramassamy, B. ; Alvey, L. ; Lepoivre, M. ; Frapart, Y. ; Stuehr, D. ; Mansuy, D. ; Boucher, J. ; Vichard, D. Inhibitory effects of a series of 7-substituted-indazoles toward nitric oxide synthases : Particular potency of 1H-indazole-7-carbonitrile. Bioorg. Med. Chem. 2008, 16, 5962-5975.
Goudet, C. ; Chapuy, E. ; Alloui, A. ; Acher, A. ; Pin, J.-P. ; Eschalier, A.
Group III metabotropic glutamate receptors inhibit hyperalgesia in animal models of inflammation and neuropathic pain.
Pain 2008, 137, 112-124.
Selvam, C. ; Goudet, C. ; Oueslati, N. ; Pin, J.-P. ; Acher, F. L(+)-2-amino-4-thiophosphonobutyric acid (L-thioAP4), a new potent agonist of group III metabotropic glutamate receptors : increased distal acidity affords enhanced potency. J.Med.Chem. 2007, 50, 4656-4664.
Lopez, S. ; Turle-Lorenzo, N. ; Acher, F. ; De Leonibus, E. ; Mele, A. ; Amalric, M. Targeting group III metabotropic glutamate receptors produces complex behavioural effects in rodent models of Parkinson’s disease. J. Neurosci. 2007, 27, 6701-6711.
Sibille, P. ; Lopez, S. ; Brabet, I. ; Valenti, O. ; Oueslati, N. ; Gaven, F. ; Goudet, C. ; Bertrand, H.-O. ; Neyton, J. ; Marino, M. J. ; Amalric, M. ; Pin, J.-P. ; Acher, F. C. Asymmetric synthesis and biological evaluation of 1-amino-2-phosphonomethylcyclopropane carboxylic acids, new group III metabotropic glutamate receptor agonists. J. Med. Chem. 2007, 50 ,3585-3595.
Frauli, M. ; Hubert, N. ; Schann, S. ; Triballeau, N. ; Bertrand, H.-O. ; Acher, F. ; Neuville, P. ; Pin, J.-P. ; Prézeau, L. Amino-pyrrolidine tricarboxylic acids (APTCs) give new insight into group III metabotropic glutamate receptor activation mechanism. Mol. Pharmacol. 2007, 71, 704-712.
Acher, F. C. Target validation : othogonal ligand-receptor pairs.in Comprehensive Medicinal Chemistry II vol3 : Drug Discovery Technologies ; Triggle, D. J., Taylor, J. B., Kubinyi, H. eds. ; Elsevier : Oxford (U.K.), 2006 ; pp 215-234.
Schann, S. ; Menet, C. ; Arvault, P. ; Mercier, G. ; Frauli, M. ; Mayer, S. ; Hubert, N. ; Triballeau, N. ; Bertrand, H.-O. ; Acher, F. ; Neuville, P. Design and synthesis of APTCs (AminoPyrrolidine Tricarboxylic Acids) : Identification of a new group III metabotropic glutamate receptor selective agonist. Bioorg. Med. Chem. Lett. 2006, 16, 4856-4860.
Triballeau, N. ; Acher, F. ; Brabet, I. ; Pin, J.-P. ; Bertrand, H.-O. Virtual screening workflow development guided by the ROC curve approach. Application to high-throughput docking on metabotropic glutamate receptor subtype 4. J.Med.Chem. 2005, 48, 2534-2547.
Luu, P. ; Acher, F. ; Bertrand, H.-O. ; Ngai, J. Odorant receptor specificities and receptor combinatorials : implications for olfactory coding. Chem Senses. 2005, 30 Suppl 1, i97-i98.
Goudet, C. ; Kniazeff, J. ; Hlavackova, V. ; Malhaire, F. ; Maurel, D. ; Acher, F. ; Blahos, J. ; Prezeau, L. ; Pin, J.-P. Asymmetric functioning of dimeric metabotropic glutamate receptors disclosed by positive allosteric modulators. J Biol Chem. 2005, 280, 24380-24385.
Conti, P. ; De Amici, M. ; Grazioso, G. ; Roda, G. ; Pinto, A. ; Hansen, K. B. ; Nielsen, B. ; Madsen, U. ; Brauner-Osborne, H. ; Egebjerg, J. ; Vestri, V. ; Pellegrini-Giampietro, D. E. ; Sibille, P. ; Acher, F. C. ; De Micheli, C. Synthesis, Binding Affinity at Glutamic Acid Receptors, Neuroprotective Effects, and Molecular Modeling Investigation of Novel Dihydroisoxazole Amino Acids. J. Med. Chem. 2005, 48, 6315-6325.
Acher, F. ; Bertrand, H.-O. Amino acid recognition by Venus Flytrap domains is encoded in an 8 residue motif. Biopolymers 2005, 80, 357-366.
Pin, J.-P. ; Kniazeff, J. ; Goudet, C. ; Bessis, A.-S. ; Rondard, P. ; Liu, J. ; Acher, F. C. ; Galvez, T. ; Prézeau, L. The activation mechanism of class-III G-protein coupled receptors. Med Chem Res 2004, 13, 38-51.
Pin, J.-P. ; Kniazeff, J. ; Goudet, C. ; Bessis, A.-S. ; Liu, J. ; Galvez, T. ; Acher, F. ; Rondard, P. ; Prézeau, L. The activation mechanism of class-C G-protein coupled receptors. Biol. Cell 2004, 96, 335-342.
Luu, P. ; Acher, F. ; Bertrand, H.-O. ; Fan, J. ; Ngai, J. Molecular determinants of ligand selectivity in a vertebrate odorant receptor. J. Neurosci. 2004, 24, 10128-10137.
Goudet, C. ; Gaven, F. ; Kniazeff, J. ; Vol, C. ; Liu, J. ; Cohen-Gonsaud, M. ; Acher, F. ; Prézeau, L. ; Pin, J.-P. Heptahelical domain of metabotropic glutamate receptor 5 behaves like rhodopsin-like receptors. Proc Nat Acad. Sci. USA 2004, 101, 378-383.
Binet, V. ; Brajon, C. ; Le Corre, L. ; Acher, F. ; Pin, J.-P. ; Prézeau, L. The heptahelical domain of GABAB2 is directly activated by CGP7930,a positive allosteric modulator of the GABAB receptor. J. Biol. Chem. 2004, 279, 29085-29091.
Mutucumarana, V. P. ; Acher, F. ; Straight, D. L. ; Jin, D. Y. ; Stafford, D. W. A Conserved Region of Human Vitamin K-dependent Carboxylase between Residues 393 and 404 Is Important for Its Interaction with the Glutamate Substrate. J Biol Chem. 2003 2003, 278, 46488-44693.
Bessis, A.-S. ; Vadesne, G. ; Bourrat, E. ; Bertho, G. ; Pin, J.-P. ; Acher, F. 3-Carboxy-4-phosphonocyclopentane amino acids : new metabotropic glutamate receptor ligands. Amino Acids 2003, 24, 303-310.
Pin, J.-P. ; Acher, F. The metabotropic glutamate receptors : structure, activation mechanism and pharmacology. Curr. Drug Targets - CNS & Neur. Dis. 2002, 1, 297-317.
Houben, R. J. T. J. ; Rijkers, D. T. S. ; Stanley, T. B. ; Acher, F. ; Azerad, R. ; Käkönen, S. M. ; Vermeer, C. ; Soute, B. A. M. Characteristics and composition of the vitamin K-dependent gamma-glutamyl carboxylase binding domain on osteocalcin. Biochem. J. 2002, 364, 323.
Bessis, A.-S. ; Rondard, P. ; Gaven, F. ; Brabet, I. ; Triballeau, N. ; Prézeau, L. ; Acher, F. ; Pin, J.-P. Closure of the Venus Flytrap module of mGlu8 receptor and the activation process : insights from mutations converting antagonists into agonists. Proc. Nat. Acad. Sci. USA 2002, 99, 11097-11102.
Bertrand, H.-O. ; Bessis, A.-S. ; Pin, J.-P. ; Acher, F. Common and selective molecular determinants involved in metabotropic glutamate receptor agonist activity. J. Med. Chem. 2002, 45, 3171-3183.
Bessis, A.-S. ; Acher, F. ; Pin, J.-P. Metabotropic glutamate receptors : exciting possibilities in excitatory transmission. Cell Transmission 2001, 17, 3-10.
Bessis, A.-S. ; Bolte, J. ; Pin, J.-P. ; Acher, F. New probes of the agonist binding site of metabotropic glutamate receptors. Bioorg. Med. Chem. Lett. 2001, 11, 1569-1572.
Parmentier, M.-L. ; Galvez, T. ; Acher, F. ; Peyre, B. ; Pellicciari, R. ; Grau, Y. ; Bockaert, J. ; Pin, J.-P. Conservation of the ligand recognition site of metabotropic glutamate receptors during evolution. Neuropharmacology 2000, 39, 1119-1131.
De Colle, C. ; Bessis, A.-S. ; Bockaert, J. ; Acher, F. ; Pin, J.-P. Pharmacological characterization of the rat metabotropic glutamate receptor type 8a revealed strong similarities and slight differences with the type 4a receptor. Eur. J. Pharmacol. 2000, 394, 17-26.
Dauban, P. ; de Saint-Fuscien, C. ; Acher, F. ; Prézeau, L. ; Brabet, I. ; Pin, J.-P. ; Dodd, R. H. First enantiospecific synthesis of a 3,4-dihydroxy-L-Glutamic acid, a new mGluR1 agonist. Bioorg. Med. Chem. Lett. 2000, 10, 129-133.
Chesnoy-Marchais, D. ; Lévi, S. ; Acher, F. Glycinergic potentiation by some 5-HT3 antagonists : insight into selectivity. Eur. J. Pharmacol. 2000, 402, 205-213.
Bessis, A.-S. ; Bertrand, H.-O. ; Galvez, T. ; De Colle, C. ; Pin, J.-P. ; Acher, F. Three-dimensional model of the extracellular domain of the type 4a metabotropic glutamate receptor : new insights into the activation process. Protein Sci. 2000, 9, 2200-2209.
Jullian, N. ; Brabet, I. ; Pin, J.-P. ; Acher, F. Agonist selectivity of mGluR1 and mGluR2 metabotropic receptors : a different environment but similar recognition of an extended glutamate conformation. J. Med. Chem. 1999, 42, 1546-1555.
Bessis, A.-S. ; Jullian, N. ; Coudert, E. ; Pin, J.-P. ; Acher, F. Extended glutamate activates metabotropic receptor types 1, 2 and 4 : selective features at mGluR4 binding site. Neuropharmacology 1999, 38, 1543-1551.
Tellier, F. ; Acher, F. ; Brabet, I. ; Pin, J.-P. ; Azerad, R. 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. Bioorg. Med. Chem. 1998, 6, 195-208.
Brabet, I. ; Parmentier, M.-L. ; Bockaert, J. ; Acher, F. ; Pin, J.-P. Effect of -carboxy-L-glutamate and DCG-IV on metabotropic glutamate receptor types 1, 2 and 4. Neuropharmacology 1998, 37, 1043-1051.
Acher, F. ; Tellier, F. ; Brabet, I. ; Fagni, L. ; Azerad, R. ; Pin, J.-P. Synthesis and pharmacological characterization of aminocyclopentane tricarboxylic acids (ACPT) : new tools to discriminate between metabotropic glutamate receptor subtypes. J. Med. Chem. 1997, 40, 3119-3129.
Tellier, F. ; Acher, F. ; Brabet, I. ; Pin, J. P. ; Bockaert, J. ; Azerad, R. Synthesis of conformationally-constrained stereospecific analogs of glutamic acid as antagonists of metabotropic receptors. Bioorg. Med. Chem. Lett. 1995, 5, 2627-2632.
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