Publications

GABAB PAM:

  1. Kalinichev M. , Donovan-Rodriguez T., Girard F., Rouillier M., Bournique B., Haddouk H., Mutel V., and Poli S. “Evaluation of peripheral versus central effects of GABAB receptor activation using novel, positive allosteric modulator of the GABAB receptor ADX71943, a pharmacological tool compound with a fully peripheral activity profile “ British Journal of Pharmacology 2014; 171 4941–4954
  2. M Kalinichev, S Palea, H Haddouk, I Royer-Urios, V Guilloteau, P Lluel, M Schneider, M Saporito, and S Poli “ADX71441, a novel, potent and selective positive allosteric modulator of GABAB receptor, shows efficacy in rodent models of overactive bladder” British journal of pharmacology 2014; 171(4):995-1006
  3. L. S. Hwa, M. Kalinichev, H. Haddouk, S. Poli, K. A. Miczek “Reduction of excessive alcohol drinking by a novel GABAB receptor positive allosteric modulator ADX71441 in mice.” Psychopharmacology 2014;231(2):333-343.
  4. M. H. Ayad, B. Bonnet, J. Quinton, M. Leigh, S. Poli “ Amorphous Solid Dispersion Successfully Improved Oral Exposure of ADX71943 in Support of Toxicology Studies” Drug Dev Ind Pharm. 2013;39(9):1300-5.

mGlu5 NAM:

  1. Sciamanna G., Ponterio G., Tassone A., Maltese M., Madeo G., Martella G., Poli S., Schirinzi T., Bonsi P., Pisani A. “Negative allosteric modulation of mGlu5 receptor rescues striatal D2 dopamine receptor dysfunction in rodent models of DYT1 dystonia” Neuropharmacology 2014 Oct;85:440-50
  2. Bezard E, Pioli EY, Li Q, Girard F, Mutel V, Keywood C, Tison F, Rascol O, Poli S “The mGluR5 negative allosteric modulator dipraglurant reduces dyskinesia in the MPTP macaque model. Movement disorders 2014 2014 Jul;29(8):1074-9.
  3. G. Duvey, B. Perry, E. Le Poul, S. Poli, B. Bonnet, N. Lambeng, D. Charvin, T. Donovan-Rodrigues, H. Haddouk, S. Gagliardi, and J.-P. Rocher “A Novel Series of Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators Based on a 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine Core” Bioorg Med Chem Lett. 2013; 23(16):4523-7.
  4. Rocher JPR, Bonnet B, Bolea C, Lutjens R, Le Poul E, Poli SM, Epping-Jordan M, Bessis A-S, Ludwig B, Mutel V “mGluR5 negative allosteric modulators overview: a medicinal chemistry approach towards a series of novel therapeutic agents” Curr Top Med Chem. 2011; 11(6):680-95
  5. Zerbib F, Bruley des Varannes S, Roman S, Tutuian R, Galmiche JP, Mion F, Tack J, Malfertheiner P, Keywood C. “Randomised clinical trial: effects of monotherapy with ADX10059, a mGluR5 inhibitor, on symptoms and reflux events in patients with gastro-oesophageal reflux disease.” Aliment Pharmacol Ther. 2011 Apr;33(8)
  6. Zerbib F, Keywood C, Strabach G. ”Efficacy, tolerability and pharmacokinetics of a modified release formulation of ADX10059, a negative allosteric modulator of metabotropic glutamate receptor 5: an esophageal pH-impedance study in healthy subjects.” Neurogastroenterol Motil. 2010 Aug;22(8)
  7. Marin JC, Goadsby PJ. “Glutamatergic fine tuning with ADX-10059: a novel therapeutic approach for migraine? Expert Opin Investig Drugs. 2010 Apr;19(4)
  8. Keywood C, Wakefield M, Tack J. “A proof-of-concept study evaluating the effect of ADX10059, a metabotropic glutamate receptor-5 negative allosteric modulator, on acid exposure and symptoms in gastro-oesophageal reflux disease.” Gut. 2009 Sep;58(9)

FSH NAM:

  1. J. A. Dias, B. A. Weaver, J. Watts, K. Kluetzman, R. M. Thomas, B. Campo, B. Bonnet, and S. Poli ” Inhibition of FSH Induced Rat Oocyte Production by a Non-Steroidal Negative Allosteric Modulator of Follicle Stimulating Hormone Receptor” Biolreprod. 2014;90(1):19
  2. Dias JA, Bonnet B, Weaver BA, Watts J, Kluetzman K, Thomas RM, Poli S, Mutel V, Campo B. “A negative allosteric modulator demonstrates biased antagonism of the follicle stimulating hormone receptor.” Mol Cell Endocrinol. 2011;333(2):143-50.

mGlu7 NAM:

  1. M. Kalinichev, M. Rouillier, F. Girard, I. Royer-Urios, B. Bournique, T. Finn, D. Charvin, B. Campo, E. Le Poul, V. Mutel, S. Poli, S. A. Neale, T. E. Salt, and R. Lutjens “ADX71743, a potent and selective negative allosteric modulator of metabotropic glutamate receptor 7 (mGlu7): in vitro and in vivo characterization” JPET 2013;344(3):624-36.

mGlu5 PAM:

  1. S. Parmentier-Batteur, P.H. Hutson, K. Menzel, J.M. Uslaner, B.A. Mattson, J.A O’Brien, B.C. Magliaro, C.A. Stump, R.M. Tynebor, N.J. Anthony, T.J. Tucker, X.F. Zhang, R. Gomez, S.L. Huszar, S. Doran, T. Forest, J.P. Rocher*, N. Lambeng*, H. Fauré*, E. Le Poul*, S. Poli*, T.W. Rosahl, M.A. Jacobson, R. Hargreaves, T.M. Williams.” Mechanism Based Neurotoxicity of mGlu5 Positive Allosteric Modulators - development challenges for a promising novel antipsychotic target” Neuropharmacology 2014;82C:161-173.

mGlu4 PAM:

  1. Kalinichev M, Le Poul E, Boléa C, Girard F, Campo B, Fonsi M, Royer-Urios I, Browne SE, Uslaner JM, Davis MJ, Raber J, Duvoisin R, Bate ST, Reynolds IJ, Poli S, Célanire S “Characterization of the novel positive allosteric modulator of the metabotropic glutamate receptor 4 ADX88178 in rodent models of neuropsychiatric disorders” JPET, 2014 Sep;350(3):495-505.
  2. Le Poul E., Boléa C., Girard F., Poli S., Charvin D., Campo B., Bortoli J., Bessif A., Luo B., Koser A.J., Hodge L.M. Smith K.M., DiLella A. G.,Liverton N., Hess F., Brown S.E. Reynolds I. J. “A potent and selective mGluR4 positive allosteric modulator improves movement in rodent models of Parkinson’s disease” JPET 2012 343:1–11.

mGlu2 PAM:

  1. Lavreysen H, Langlois X, Donck LV, Nuñez JM, Pype S, Lütjens R, Megens A. “Preclinical evaluation of the antipsychotic potential of the mGlu2-positive allosteric modulator JNJ-40411813”. Pharmacol Res Perspect. 2015 Mar;3(2)
  2. Lavreysen H, Ahnaou A, Drinkenburg W, Langlois X, Mackie C, Pype S, Lütjens R, Le Poul E, Trabanco AA, Nuñez JM. “Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor.” Pharmacol Res Perspect. 2015 Feb;3(1)
  3. Cid, Jose; Tresadern, Gary; Duvey, Guillaume; Lütjens, Robert; Finn, Terry; Rocher, Jean-Philippe; Imogai, Hassan; Poli, Sonia; Vega, Juan; de Lucas, Ana; Matesanz, Encarnación; Linares, María; Andrés, José-Ignacio; Alcazar, Jesús; MacDonald, Gregor; Oelhrich, Daniel; Lavreysen, Hilde; Ahnaou, Abdellah; Drinkerburg, Wilhelmus; Mackie, Claire; Gallacher, David; Pype, Stefan; Trabanco, Andrés “Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): A Novel Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor" J Med Chem 2014 Aug 14;57(15):6495-512
  4. Jose María Cid, Guillaume Duvey, Andrés A. Trabanco, Gary Tresadern, Vanthea Nhem, Rocco Furnari, Philippe Cluzeau, Juan Antonio Vega, Ana Isabel de Lucas, Encarnación Matesanz, José Manuel Alonso, María Lourdes Linares, José Ignacio Andrés, Sonia M. Poli, Robert Lütjens, Hassan Himogai, Jean-Philippe Rocher, Gregor J. Macdonald, Daniel Oehlrich, Hilde Lavreysen, Abdelah Ahnaou, Wilhelmus Drinkenburg, Claire Mackie “Discovery of 1,4-Disubstituted-3-Cyano-2-pyridones: a New Class of Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor” J Med Chem. 2012;55(5):2388-405.
  5. Trabanco AA, Duvey G, Cid JM, Macdonald GJ, Cluzeau P, Nhem V, Furnari R, Behaj N, Poulain G, Finn T, Lavreysen H, Poli S, Raux A, Thollon Y, Poirier N, D'Addona D, Andrés JI, Lütjens R, Le Poul E, Imogai H, Rocher JP “New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): identification and synthesis of N-propyl-8-chloro-6-substituted isoquinolones.” Bioorg Med Chem Lett. 2011;21(3):971-6
  6. Mara Cid J, Duvey G, Cluzeau P, Nhem V, Macary K, Raux A, Poirier N, Muller J, Bolea C, Finn T, Poli S, Epping-Jordan M, Chamelot E, Derouet F, Girard F, Macdonald GJ, Vega JA, de Lucas AI, Matesanz E, Lavreysen H, Linares ML, Oehlrich D, Oyarzbal J, Tresadern G, Trabanco AA, Ignacio J, Le Poul E, Imogai H, Lütjens R, and Rocher JP “Discovery of 1,5-Disubstituted Pyridones: a New Class of Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor” ACS Chem. Neurosci. 2010, 1, 788

mGlu2 NAM:

  1. Campo B, Kalinichev M, Lambeng N, El Yacoubi M, Royer-Urios I, Schneider M, Legrand C, Parron D, Girard F, Bessif A, Poli S, Vaugeois JM, Le Poul E and Célanire S “Characterization of an mGluR2/3 negative allosteric modulator in rodent models of depression and comparison with the reference mGluR2/3 orthosteric antagonist LY341495” J. Neurogenetics, 2011; 25(4): 152–166

GLP1 PAM:

  1. Schelshorn D, Joly F, Mutel S, Hampe C, Breton B, Mutel V, Lütjens R. “Lateral allosterism in the glucagon receptor family: glucagon-like peptide 1 induces G-protein-coupled receptor heteromer formation”. Mol Pharmacol. 2012 Mar;81(3):309-18

Editorial work

  1. “Small Molecule Therapeutics for Schizophrenia” in Topics in medicinal chemistry – Springer 2014; Editor: Sylvain Célanire; Co-Editor: Sonia Poli

Book chapters & reviews:

  1. S. Célanire, B. Perry, R. Lutjens, S. Poli and I. J. Reynolds: “Glutamate Receptor Modulators as Emergent Therapeutic Agents in the Treatment of Parkinson’s Disease” chapter in Emerging Drugs and Targets for Parkinson's Disease, RSC drug discovery series vol 34 – Chapter 10, 237-265.
  2. Lütjens R, Perry B, Schelshorn D, Rocher JP.: “New technologies enabling the industrialization of allosteric modulator discovery.” Drug Discov Today Technol. 2013 Summer;10(2)
  3. Célanire S, Campo B. “Recent advances in the drug discovery of metabotropic glutamate receptor 4 (mGluR4) activators for the treatment of CNS and non-CNS disorders.” Expert Opin Drug Discov. 2012 Mar;7(3)
  4. Célanire S., Duvey G., Poli S., Rocher J.-P. “mGluR2 Activators and mGluR5 Blockers Advancing in the Clinic for Major CNS Disorders” Annual Reports in Medicinal Chemistry 2012 vol 47, Chapter 6, 71-88.