Publications

Chaptal V, Delolme F, Kilburg A, Magnard S, Montigny C, Picard M, Prier C, Monticelli L, Bornert O, Agez M, Ravaud S, Orelle C, Wagner R, Jawhari A, Broutin I, Pebay-Peyroula E, Jault JM, Kaback HR, le Maire M, Falson P (2017). Quantification of Detergents Complexed with Membrane Proteins. Sci Rep 7:41751.

Elhabazi K, Humbert JP, Bertin I, Quillet R, Utard V, Schmitt M, Bourguignon JJ, Laboureyras E, Simonnet G, Ancel C, Simonneaux V, Beltramo M, Bucher B, Sorg T, Meziane H, Schneider E, Petit-Demoulière B, Ilien B, Bihel F*, Simonin F* (2017). RF313:an orally bioavailable NPFF receptor antagonist, opposes effects of RF-amide-related peptide-3 and opioid-induced hyperalgesia in rodents. Neuropharmacol 118:188-198.

Hartmann L, Metzger E, Ottelard N, Wagner R (2017). Direct Extraction and Purification of Recombinant Membrane Proteins from Pichia pastoris Protoplasts. Methods Mol Biol 1635:45-56.

Roeckel LA, Utard V, Reiss D, Mouheiche J, Maurin H, Robé A, Audouard E, Wood JN, Goumon Y, Simonin F, Gaveriaux-Ruff C (2017). Morphine-induced hyperalgesia involves mu opioid receptors and the metabolite morphine-3-glucuronide. Sci Rep 7:10406.

Waqas SFS, Hoang AC, Lin YT, Ampem G, Azegrouz H, Balogh L, Thuróczy J, Chen JC, Gerling IC, Nam S, Lim JS, Martínez-Ibañez J, Real J T, Paschke S, Quillet R, Ayachi S, Simonin F, Schneider M, Brinkman JA, Lamming DW, Seroogy CM, Röszer T (2017). Neuropeptide-FF increases macrophage self-renewal and abrogates inflammation in adipose tissue. J Clin Invest 127:3559.

Guillemyn K, Starnowska J, Lagard C, Dyniewicz J, Rojewska E, Mika J, Chung NN, Utard V, Kosson P, Lipkowski AW, Chevillard L, Arranz-Gibert P, Teixidó M, Megarbane B, Tourwé D, Simonin F, Przewlocka B, Schiller PW, Ballet S (2016). Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain. J Med Chem 59:3777-3792.

Hartmann L, Kugler V, Wagner R (2016). Expression of Eukaryotic Membrane Proteins in Pichia pastoris. Methods Mol Biol 1432:143-62.

Logez C, Damian M, Legros C, Dupré C, Guéry M, Mary S, Wagner R, M'Kadmi C, Nosjean O, Fould B, Marie J, Fehrentz JA, Martinez J, Ferry G, Boutin JA, Banères JL (2016). Detergent-free Isolation of Functional G Protein-Coupled Receptors into Nanometric Lipid Particles. Biochemistry 55:38-48.

Quillet R, Ayachi S, Bihel F, Elhabazi K, Ilien B*, Simonin F* (2016). RF-amide neuropeptides and their receptors in Mammals : Pharmacological properties, drug development and main physiological functions. Pharmacol & Ther 160:84-132.

Roeckel LA*, Le Coz GM*, Gavériaux-Ruff C#, Simonin F# (2016). Opioid-induced hyperalgesia: cellular and molecular mechanisms. Neurosci 338:160-182.

Westh Hansen R, Wang X, Golab A, Bornert O, Oswald C, Wagner R, Martinez KL (2016). Functional Stability of the Human Kappa Opioid Receptor Reconstituted in Nanodiscs Revealed by a Time-Resolved Scintillation Proximity Assay. PLoS One 11:e0150658.

Abboud D, Daubeuf F, Do QT, Utard V, Villa P, Haiech J, Bonnet D, Hibert M, Bernard P, Galzi JL*, Frossard N* (2015). A strategy to discover decoy chemokine ligands with an anti-inflammatory activity. Sci Rep 5:14746.

Bihel F, Humbert JP, Schneider S, Bertin I, Wagner P, Schmitt M, Laboureyras E, Petit-Demoulière B, Schneider E, Mollereau C, Simonnet G, Simonin F*, Bourguignon JJ* (2015). Development of a peptidomimetic antagonist of the neuropeptide FF receptors for the prevention of opioid-induced hyperalgesia. ACS Chem Neurosci 6:438-445.

Buffel I, Meurs A, Portelli J, Raedt R, De Herdt V, Poppe L, De Meulenaere V, Wadman W, Bihel F, Schmitt M, Vonck K, Bourguignon JJ, Simonin F, Smolders I, Boon P (2015). The effect of Neuropeptide FF in the amygdala kindling model. Acta Neurol Scand 134:181-188.

Buffel I, Meurs A, Portelli J, Raedt R, De Herdt V, Sioncke L, Wadman W, Bihel F, Schmitt M, Vonck K, Bourguignon JJ, Simonin F, Smolders I, Boon P (2015). Neuropeptide FF and prolactin releasing peptide decrease cortical excitability through activation of NPFF receptors. Epilepsia 56:489-498.

Galzi JL, Ruggiu F, Gizzi P, Didier B (2015). Quality control of chemical libraries. Med Sci 31:660-666.

Guilini C, Baehr C, Schaeffer E, Gizzi P, Rufi F, Haiech J, Weiss E, Bonnet D, Galzi JL (2015). New fluorescein precursors for live bacteria detection. Anal Chem 87:8858-8866.

Hounsou C, Margathe JF, Oueslati N, Belhocine A, Dupuis E, Thomas C, Mann A, Ilien B, Rognan D, Trinquet E, Hibert M, Pin JP, Bonnet D, Durroux T (2015). Time-resolved FRET binding assay to investigate hetero-oligomer binding properties: Proof of concept with dopamine D1/D3 heterodimer. ACS Chem Biol 10:466-474.

Lecat S, Belemnaba L, Galzi JL, Bucher B (2015). Neuropeptide Y receptor mediates activation of ERK1/2 via transactivation of the IGF receptor. Cell Signal 27:1297-1304.

Lecat S, Matthes HW, Pepperkok R, Simpson JC, Galzi JL (2015). A Fluorescent Live Imaging Screening Assay Based on Translocation Criteria Identifies Novel Cytoplasmic Proteins Implicated in G Protein-coupled Receptor Signaling Pathways. Mol Cell Proteomics 14:1385-1399.

Portelli J*, Meurs A*, Bihel F, Hammoud H, Schmitt, M De Kock J, Humbert JP , Bertin I, Utard V, Buffel I, Coppens J, Tourwe D, Maes V, Vanhaecke T, Massie A, Balasubramaniam A, Boon P, Michotte Y, Bourguignon JJ*, Simonin F*, Smolders I* (2015). Neuropeptide FF receptors as novel targets for limbic seizure attenuation. Neuropharmacol 95:415-423.

Rouméas L, Humbert JP, Schneider S, Doebelin C, Bertin I, Schmitt M, Bourguignon JJ, Simonin F*, Bihel F* (2015). Effects of systematic N-terminus deletions and benzoylations of endogenous RF-amide peptides on NPFF1R, NPFF2R, GPR10, GPR54 and GPR103 Peptides. Peptides 71:156-61.

Schneider S, Ftouni H, Niu S, Schmitt M, Simonin F, Bihel F (2015). Rapid and scalable synthesis of innovative unnatural α, β or γ-amino acids functionalized with tertiary amines on their side-chains. Org Biomol Chem 13:7020-7026.

Zirafi O, Kim KE, Ständker L, Mohr K, Sauter D, Heigele A, Kluge SF, Wiershinska E, Chudziak D, Richter R, Möpps B,Gierschik P, Vas V, Geiger H, Lamla M, Weil T, Burster T, Zgraja A, Daubeuf F, Frossard N, Hachet-Haas M, Heunisch F, Reichetzeder C, Galzi JL, Perez-Castells J, Canales-Mayordomo A, Jiménez-Barbero J,Giménez-Gallego G, Schneider M, Shorter J, Telenti A, Hocher B, Forssmann WG, Bonig H, Kirchhoff F, Münch J (2015). Discovery and characterization of an endogenous CXCR4 antagonist. Cell Rep 11:737-747.

Ayachi S, Simonin F (2014). Involvement of Mammalian RF-Amide Peptides and Their Receptors in the Modulation of Nociception in Rodents. Front Endocrinol 5:158-170.

Elhabazi K, Ayachi S, Ilien B, Simonin F (2014). Assessment of morphine-induced hyperalgesia and analgesic tolerance in mice using thermal and mechanical nociceptive modalities. J Vis Exp e51264.

Logez C, Berger S, Legros C, Cohen W, Delagrange P, Boutin JA, Ferry G, Simonin F*, Wagner R* (2014). Recombinant human MT1 receptor purified in mixed detergents shows a similar pharmacology than in membranes from mammalian cells. PLoS One 9:e100616.

Michel G, Matthes HW, Hachet-Haas M, El Baghdadi K, de Mey J, Pepperkok R, Simpson JC, Galzi JL*, Lecat S* (2014). Plasma membrane translocation of REDD1 governed by GPCRs contributes to mTORC1 activation. J Cell Sci 127:773-87.

Romain B, Hachet-Haas M, Rohr S, Brigand C, Galzi JL, Gaub MP, Pencreach E, Guenot D (2014). Hypoxia differentially regulated CXCR4 and CXCR7 signaling in colon cancer. Mol Cancer 13:58.

Ruggiu F, Gizzi P, Galzi JL, Hibert M, Haiech J,  Baskin I, Horvath D, Marcou G, Varnek A (2014). Quantitative structure-property relationship modelling : a valuable support in high-throughput screening quality control. Anal Chem 86:2510–2520.

Bornert O, Møller TC, Bœuf J, Candusso MP, Wagner R, Martinez KL, Simonin F (2013). Identification of a novel protein-protein interaction motif mediating interaction of gpcr-associated sorting proteins with g protein-coupled receptors. PloS One 8:e56336.

Daubeuf F*, Hachet-Haas M*, Gizzi P, Gasparik V, Bonnet D, Hibert M, Frossard N, Galzi JL (2013). Antedrugs of the chemokine CXCL12 neutraligand show selectivity in an in vivo model of asthma. J Biol Chem 288:11865-11876.

Daval SB, Kellenberger E, Bonnet D, Utard V, Galzi JL, Ilien B (2013). Exploration of the orthosteric/allosteric interface in human M1 muscarinic receptors by bitopic fluorescent ligands. Mol Pharmacol 84:71-85.

Doebelin C, Wagner P, Bertin I, Simonin F, Schmitt M, Bihel F, Bourguignon JJ (2013). Trisubstitution of pyridine through sequential and regioselective palladium cross-coupling reactions affording analogs of known GPR54 antagonists. RSC Adv 3:10296-10300.

Elhabazi K, Humbert JP, Bertin I, Schmitt M, Bihel F, Bourguignon  JJ, Bucher B, Becker JAJ, Sorg T, Meziane H, Petit-Demoulière B, Ilien B, Simonin F (2013). Endogenous mammalian RF-amide peptides, including PrRP, kisspeptin and 26RFa, modulate nociception and morphine analgesia via NPFF receptors. Neuropharmacol 75:164-171.

Puglia AL, Rezende AG, Jorge SA, Wagner R, Pereira CA, Astray RM (2013). Quantitative RT-PCR for titration of replication-defective recombinant Semliki Forest virus. J Virol Methods 193:647-652.

Bouchery T, Dénécé G, Attout T, Eberhard K, Lhermitte-Vallarino N, Galzi JL, Bachelerie F, Brotin E, Gavotte L, Moulia C, Bain O, Martin C (2012). The development and the survival of the filarial Litomosoides sigmodontis in mouse is dependent on the CXCL12/CXCR4 axis. PLoS One 7:e34971.

Daval SB, Valant C, Bonnet D, Kellenberger E, Hibert M, Galzi JL, Ilien B (2012). Fluorescent Derivatives of AC-42 To Probe Bitopic Orthosteric/Allosteric Binding Mechanisms on Muscarinic M1 Receptors. J Med Chem 55:2125−2143.

Elhabazi K, Trigo J M, Mollereau C, Moulédous L, Zajac JM, Bihel F, Schmitt M, Bourguignon JJ, Meziane H, Petit-demoulière B, Bockel F, Maldonado R, Simonin F (2012). Involvement of neuropeptide FF receptors in neuroadaptative responses to acute and chronic opiates treatments. Br J Pharmacol 165:424-435.

Galzi JL, Haas M, Frossard N, Hibert M (2012). Why and how to find neutraligands targeting chemokines? Drug Discov Today 9:e245-e251.

Galzi JL, Ilien B (2012). G protein-coupled receptors: allosteric regulators of cell metabolism. Med Sci 28:852-857.

Gasparik V, Daubeuf F Hachet-Haas M, Rohmer F, Gizzi P, Haiech J, Galzi JL, Hibert M, Bonnet D, Frossard N (2012). Prodrugs of a CXC Chemokine-12 (CXCL12) Neutraligand Prevent Inflammatory Reactions in an Asthma Model in Vivo. ACS Med Chem Lett 3:10-14.

Gealageas R, Schneider S, Humbert JP, Bertin I, Schmitt M, Laboureyras E, Dugave C, Mollereau C, Simonnet G, Bourguignon JJ, Bihel F*, Simonin F* (2012). Development of sub-nanomolar dipeptidic ligands of neuropeptide FF receptors. Bioorg Med Chem Lett 22:7471-7474.

Andersson DA, Gentry C, Alenmyr L, Killander D, Lewis SE, Andersson A, Bucher B, Galzi JL, Sterner O, Bevan S, Högestätt ED, Zygmunt PM (2011). TRPA1 mediates spinal antinociception induced by acetaminophen and the cannabinoid Δ(9)-tetrahydrocannabiorcol. Nat Commun 2:551.

Daubeuf F, Gasparik V, Hachet-Haas M, Rohmer F, Gizzi P, Haiech J, Galzi JL, Hibert M, Bonnet D, Frossard N (2011). Activity of soluble CXCL12 neutraligands in vivo in a short model of asthma.
Inflammation research 60:112-113

Elhabazi K, Trigo JM, Mollereau C, Moulédous L, Zajac JM, Bihel F, Schmitt M, Bourguignon JJ, Meziane H, Petit-demoulière B, Bockel F, Maldonado R, Simonin F (2011). Involvement of neuropeptide FF receptors in neuroadaptative responses to acute and chronic opiates treatments. Br J Pharmacol 165:424-35

Lecat S*, Ouédraogo M*, Cherrier T, Noulet F, Rondé P, Glasser N, Galzi JL, Mely Y, Takeda K, Bucher B (2011). Contribution of a tyrosine-based motif to cellular trafficking of wild-type and truncated NPY Y(1) receptors. Cell Signal 23:228-38.

Mathis C, Bott JB, Candusso MP, Cassel JC*, Simonin F* (2011). Impaired striatum-dependent behavior in GASP-1 knockout mice. Genes, Brain and Behavior 10:299-308.

Abu-Helo A, Simonin F (2010). Identification and biological significance of G protein-coupled receptor associated sorting proteins (GASP). Pharmacol Ther 126:244-250.

Galzi JL, Hachet-Haas M, Bonnet D, Daubeuf F, Hibert M, Haiech J, Frossard N (2010). Neutralising endogeneous chemokines with small molecules. Principles and potential therapeutic applications. Pharmacol Ther 126:39-55.

Iturrioz X, Alvear-Perez R, De Mota N, Franchet C, Guillier F, Leroux V, Dabire H, Le Jouan M, Chabane H, Gerbier R, Bonnet D, Berdeaux A, Maigret B, Galzi JL, Hibert M, Llorens-Cortes C (2010). Identification and pharmacological properties of E339-3D6, the first nonpeptidic apelin receptor agonist. FASEB J 24:1506-1517.

Bœuf J, Trigo JM, Moreau PH, Lecourtier L, Vogel E, Cassel JC, Mathis C, Klosen P, Maldonado R, Simonin F (2009). Attenuated behavioural responses to acute and chronic cocaine in GASP-1 deficient mice. Eur J Neurosci 30:860-868.

Ilien B, Glasser N, Clamme JP, Didier P, Piemont E, Chinnappan R, Daval SB, Galzi JL, Mély Y (2009). Pirenzepine promotes the dimerization of muscarinic M1 receptors through a three-step binding process. J Biol Chem 284:19533-19543.

Ma L, MacTavish D, Simonin F, Bourguignon JJ, Watanabe T, Jhamandas JH (2009). Prolactin-releasing peptide effects in the rat brain are mediated through the Neuropeptide FF receptor. Eur J Neurosci 30:1585-1593.

Valant C, Maillet EL, Bourguignon JJ, Bucher B, Utard V, Galzi JL, Hibert M (2009). Allosteric functional switch of neurokinin A-mediated signalling at the neurokinin NK2 receptor : structural exploration. J Med Chem 52:5999-6011.

Hachet-Haas M, Balabanian K, Rohmer F, Pons F, Franchet C, Lecat S, Chow KYC, Dagher R, Gizzi P, Didier B, Lagane B, Kellenberger E, Bonnet D, Baleux F, Haiech J, Parmentier M, Frossard N, Arenzana-Seisdedos F, Hibert M, Galzi JL (2008). Small neutralizing molecules to inhibit actions of the chemokine CXCL12. J Biol Chem 283:23189-23499.

Ouédraogo M, Lecat S, Rochdi MD, Hachet-Haas M, Matthes H, Gicquiaux H, Verrier S, Gaire M, Glasser N, Mély Y, Takeda K, Bouvier M, Galzi JL, Bucher B (2008). Distinct motifs of neuropeptide Y receptors differentially regulate trafficking and desensitization. Traffic 9:305-324.

Kellenberger E, Springael JY, Parmentier M, Hachet-Haas M, Galzi JL, Rognan D (2007). Identification of nonpeptide CCR5 receptor agonists by structure-based virtual screening. J Med Chem 50:1294-303.

Jhamandas JH, Simonin F, Bourguignon JJ, Harris KH (2007). Neuropeptide FF and neuropeptide VF inhibit GABAergic neurotransmission in parvocellular neurons of the rat hypothalamic paraventricular nucleus. Am J Physiol Regul Integr Comp Physiol 292:R1872-80

Maillet EL, Pellegrini N, Valant C, Bucher B, Hibert M, Bourguignon JJ, Galzi JL (2007). A novel, conformation-specific allosteric inhibitor of the tachykinin NK2 receptor (NK2R) with functionally selective properties. FASEB J 21:2124-34.

Zoffmann S, Bertrand S, Do QT, Bertrand D, Rognan D, Hibert M, Galzi JL (2007). Topological analysis of the complex formed between neurokinin A and the NK2 tachykinin receptor. J Neurochem 101:506-16.

Bonnet D, Ilien B, Galzi JL, Riche S, Antheaune C, Hibert M (2006). A rapid and versatile method to label receptor ligands using "click" chemistry : Validation with the muscarinic M1 antagonist pirenzepine. Bioconjug Chem 17:1618-23.

Bourguignon JJ, Simonnet G, Simonin F (2006). RF9, a powerful and selective antagonist of the neuropeptide FF receptors, prevents the development of the tolerance to opioids. Med Sci 22:579-80.

Hachet-Haas M, Converset N, Marchal O, Matthes H, Gioria S, Galzi JL, Lecat S (2006). FRET and colocalization analyzer : a method to validate measurements of sensitized emission FRET acquired by confocal microscopy and available as an ImageJ plug-in. Microsc Res Tech 69:941-56.

Simonin F (2006). Neuropeptide FF receptors as therapeutic targets. Drugs of the Future 31:603-609.

Simonin F, Schmitt M, Laulin JP, Laboureyras E, Jhamandas JH, MacTavish D, Matifas A, Mollereau C, Laurent P, Parmentier M, Kieffer BL, Bourguignon JJ, Simonnet G (2006). RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia. Proc Natl Acad Sci USA 103:466-71.