Euroscreen S.A.

Oxysterols direct immune cell migration via EBI2.  S. Hannedouche et al., 28 July 2011 Nature vol 475 p. 524.

Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor. H. R. Hoveyda, M-O Roy, S. Blanc, S. Noël, J. M. Salvino, M. A. Ator & G. Fraser., Bioorganic & Medicinal Chemistry Letters 21 (2011) 1991-1996.

Agonist-induced internalization of CCR5 as a mechanism to inhibit HIV replication.  Ferain T., Hoveyda HR., Ooms F., Schils D., Bernard J., Fraser G., J. Pharmacol. Exp. Ther. 2011 Mar 9.

Biological diversity from a structurally diverse library: systematically scanning conformational space using a pyranose scaffold.  Abbenante G et al., 2010. J Med Chem 53 (15):5576-86.

Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.  Dolusic E et al., Bioorg Med Chem 19 (2011) 1550-1561.

GPR43 agonist improves glucose tolerance and decreases NEFA levels in lean mice.  J. Bernard, M. Brait, G. Dutheuil, A.F. Hartiel, H. Hoveyda and G. Fraser, 70th Scientific Sessions of the American Diabetes Association (Orlando, FL), June 25-29th, 2010.

Identification of a small-molecule GPR43 agonist that increases glucose uptake and lipolysis in adipocytes.  J. Bernard, A.F. Hartiel, C. Brantis, H. Hoveyda and G. Fraser, 69th Scientific Sessions of the American Diabetes Association (New Orleans, LA), June 5-9th, 2009.

Free fatty acid receptor family: novel targets for the treatment of diabetes and dyslipidemia.  J. Bernard, 2008.  Curr Opin Invest Drug 9 (10) 1078-83.

ESN-196, a novel small-molecule CCR5 agonist inhibits R5 HIV infection.  T. Ferain, D. Scholes, J. Bernard, R. Sleigh, F. Ooms, J. Huck, V. Dupriez and G. Fraser, 15th Conference on Retroviruses and Opportunistic Infections (Boston, MA), Feb 3-6th, 2008.

Real-time monitoring of morphological changes in living cells by electronic cell sensor arrays: an approach to study G protein-coupled receptors. Yu N, Atienza JM, Bernard J, Blanc S, Zhu J, Wang X, Xu X, Abassi YA. (2005) Anal Chem. 78:35-43.

PTHrP fragments 1-16 and 1-23 do not bind to either the ETA or the ETB endothelin receptors. Langlois C, Letourneau M, Turcotte K, Detheux M, Fournier A. (2005) Peptides 26:1436-40.

Transmembrane domain V of the endothelin-A receptor is a binding domain of ETA-selective TTA-386-derived photoprobes. Tessier S, Boivin S, Aubin J, Lampron P, Detheux M, Fournier A. (2005) Biochemistry 44:7844-54.

Identification and characterization of an endogenous chemotactic ligand specific for FPRL2. Migeotte I, Riboldi E, Franssen JD, Gregoire F, Loison C, Wittamer V, Detheux M, Robberecht P, Costagliola S, Vassart G, Sozzani S, Parmentier M, Communi D. (2005) J. Exp. Med. 201:83-93.

Actions of tilidine and nortilidine on cloned opioid receptors. Thierry C, Boeynaems JM, Paolo M. (2005) Eur J Pharmacol. 506:205-8.

Identification of a binding domain of the endothelin-B receptor using a selective IRL-1620-derived photoprobe. Boivin S, Tessier S, Aubin J, Lampron P, Detheux M, Fournier A. (2004) Biochemistry 43:11516-25.

Substitution of conserved glycine residue by alanine in natural and synthetic neuropeptide ligands causes partial agonism at the stomoxytachykinin receptor. Poels J, Van Loy T, Franssens V, Detheux M, Nachman RJ, Oonk HB, Akerman KE, Vassart G, Parmentier M, De Loof A, Torfs H, Broeck JV. (2004) J. Neurochem. 90:472-8.

Functional analysis of chemically synthesized derivatives of the human CC chemokine CCL15/HCC-2, a high affinity CCR1 ligand. Escher SE, Forssmann U, Frimpong_Boateng A, Adermann K, Vakili J, Sticht H, Detheux M. (2004) J. Pept. Res. 63:6-47.

Two subtypes of ecdysis-triggering hormone receptor in Drosophila melanogaster. Park Y, Kim YJ, Dupriez V, Adams ME. (2003) J. Biol. Chem. 278:17710-5.

Specific recruitment of antigen-presenting cells by chemerin, a novel processed ligand from human inflammatory fluids. Wittamer V, Franssen JD, Vulcano M, Mirjolet JF, Le Poul E, Migeotte I, Brezillon S, Tyldesley R, Blanpain C, Detheux M, Mantovani A, Sozzani S, Vassart G, Parmentier M, Communi D. (2003) J. Exp. Med. 198:977-985 [PDF].

Functional Characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation. Le Poul E, Loison C, Strufy S, Springael JY, Lannoy V, Decobecq ME, Brezillon S, Dupriez V, Vassart G, Van Damme J, Parmentier M, Detheux M. (2003) J. Biol. Chem. 278:25481-25489 [PDF].

Identification of natural ligands for the orphan G protein-coupled receptors GPR7 and GPR8. Brezillon S, Lannoy V, Franssen JD, Le Poul E, Dupriez V, Lucchetti J, Detheux M, Parmentier M. (2003) J. Biol. Chem. 278:776-783 [PDF].

Serotonin 5-HT(2B) receptor loss of function mutation in a patient with fenfluramine-associated primary pulmonary hypertension. Blanpain C, Le Poul E, Parma J, Knoop C, Detheux M, Parmentier M, Vassart G, Abramowicz MJ. (2003) Cardiovasc Res 60:518-28.

Distinct recognition of OX1 and OX2 receptors by orexin peptides. Ammoun S, Holmqvist T, Shariatmadari R, Oonk HB, Detheux M, Parmentier M, Akerman KE, Kukkonen JP.(2003) J Pharmacol Exp Ther 305:507-14.

Multiple active states and oligomerization of CCR5 revealed by functional properties of monoclonal antibodies. Blanpain C, Vanderwinden JM, Cihak J, Wittamer V, Le Poul E, Issafras H, Stangassinger M, Vassart G, Marullo S, Schlndorff D, Parmentier M, Mack M. (2002) Mol Biol Cell. 13:723-37.

Aequorin-based functional assays for G-protein-coupled receptors, ion channels, and tyrosine kinase receptors. Dupriez VJ, Maes K, Le Poul E, Burgeon E, Detheux M. (2002) Receptors Channels 6:319-30.

Recombinant aequorin as a reporter for receptor-mediated changes of intracellular Ca2+ -levels in Drosophila S2 cells. Torfs H, Poels J, Detheux M, Dupriez V, Van Loy T, Vercammen L, Vassart G, Parmentier M, Vanden Broeck (2002) J. Invert Neurosci:3: 119-24.

Adaptation of aequorin functional assay to high throughput screening. Le Poul E, Hisada S, Mizuguchi Y, Dupriez VJ, Burgeon E, Detheux M. (2002) J Biomol Screen. 7:57-65.

Functional analysis of synthetic insectatachykinin analogs on recombinant neurokinin receptor expressing cell lines. Torfs H, Akerman KE, Nachman RJ, Oonk HB, Detheux M, Poels J, Loy TV, Loof AD, Meloen RH, Vassart G, Parmentier M, Broeck JV. (2002) Peptides 11: 1999-2005.

Pharmacological characterization of human NPFF(1) and NPFF(2) receptors expressed in CHO cells by using NPY Y(1) receptor antagonists. Mollereau C, Mazarguil H, Marcus D, Quelven I, Kotani M, Lannoy V, Dumont Y, Quirion R, Detheux M, Parmentier M, Zajac JM. (2002) Eur J Pharmacol 451:245-56.

Analysis of C-terminally substituted tachykinin-like peptide agonists by means of aequorin-based luminescent assays for human and insect neurokinin receptors. Torfs H, Detheux M, Oonk HB, Akerman KE, Poels J, Loy TV, Loof AD, Vassart G, Parmentier M, Broeck JV. (2002) Biochem Pharmacol 63:1675-82.

Amino-terminal truncation of CXCR3 agonists impairs receptor signaling and lymphocyte chemotaxis, while preserving antiangiogenic properties. Proost P, Schutyser E, Menten P, Struyf S, Wuyts A, Opdenakker G, Detheux M, Parmentier M, Durinx C, Lambeir AM, Neyts J, Liekens S, Maudgal PC, Billiau A, Van Damme J. (2001) Blood.;98:3554-61.

Distribution of an orphan G-protein coupled receptor (JP05) mRNA in the human brain. Brezillon S, Detheux M, Parmentier M, Hokfelt T, Hurd YL. (2001) Brain Res.;921(1-2):21-30.

Identification of a novel human ADP receptor coupled to G(i). Communi D, Gonzalez NS, Detheux M, Brezillon S, Lannoy V, Parmentier M, Boeynaems JM. (2001) J Biol Chem. 276:41479-85.

Urokinase plasminogen activator and plasmin efficiently convert hemofiltrate CC chemokine 1 into its active. Vakili J, Standker L, Detheux M, Vassart G, Forssmann WG, Parmentier M. (2001) J Immunol.;167:3406-13.

The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. Kotani M, Detheux M, Vandenbogaerde A, Communi D, Vanderwinden JM, Le Poul E, Brezillon S, Tyldesley R, Suarez-Huerta N, Vandeput F, Blanpain C, Schiffmann SN, Vassart G, Parmentier M. (2001) J Biol Chem. 276:34631-6.

Palmitoylation of CCR5 is critical for receptor trafficking and efficient activation of intracellular signaling pathways. Blanpain C, Wittamer V, Vanderwinden JM, Boom A, Renneboog B, Lee B, Le Poul E, El Asmar L, Govaerts C, Vassart G, Doms RW, Parmentier M (2001) J Biol Chem 276:23795-804.

Functional characterization of a human receptor for neuropeptide FF and related peptides. Kotani M, Mollereau C, Detheux M, Le Poul E, Brézillon S, Vakili J, Mazarguil H, Vassart G, Zajac JM, Parmentier M. (2001) Br J Pharmacol. 133:138-44.

Agonist and antagonist activities on human NPFF(2) receptors of the NPY ligands GR231118 and BIBP3226. Mollereau C, Gouardères C, Dumont Y, Kotani M, Detheux M, Doods H, Parmentier M, Quirion R, Zajac JM. (2001) Br J Pharmacol. 133:1-4.

Natural proteolytic processing of hemofiltrate CC chemokine 1 generates a potent CC chemokine receptor (CCR)1 and CCR5 agonist with anti-HIV properties. Detheux M, Ständker L, Vakili J, Münch J, Forssmann U, Adermann K, Pöhlmann S, Vassart G, Kirchhoff F, Parmentier M, Forssmann WG. (2000) J Exp Med 192:1501-8.

The orexin OX1 receptor activates a novel Ca2+ influx pathway necessary for coupling to phospholipase C. Lund PE, Shariatmadari R, Uustare A, Detheux M, Parmentier M, Kukkonen JP, Akerman KE. (2000) J Biol Chem 275:30806-12.

Extracellular cysteines of CCR5 are required for chemokine binding, but dispensable for HIV-1 coreceptor activity. Blanpain C, Lee B, Vakili J, Doranz BJ, Govaerts C, Migeotte I, Sharron M, Dupriez V, Vassart G, Doms RW, Parmentier M. (1999) J Biol Chem 274:18902-8.

CD26/dipeptidyl-peptidase IV down-regulates the eosinophil chemotactic potency, but not the anti-HIV activity of human eotaxin by affecting its interaction with CC chemokine receptor 3. Struyf S, Proost P, Schols D, De Clercq E, Opdenakker G, Lenaerts JP, Detheux M, Parmentier M, De Meester I, Scharpé S, Van Damme J. (1999) J Immunol 162:4903-9.

Distribution of a glucocorticoid-induced orphan receptor (JP05) mRNA in the central nervous system of the mouse. Pesini P, Detheux M, Parmentier M, Hökfelt T. (1998) Brain Res Mol Brain Res 57:281-300.

The second extracellular loop of CCR5 is the major determinant of ligand specificity. Samson M, LaRosa G, Libert F, Paindavoine P, Detheux M, Vassart G, Parmentier M. (1997) J Biol Chem 272:24934-41.