GPCR Deorphanization Platform
EuroscreenFast give you access to a state-of-the-art GPCR deorphanization platform consisting of a large library of cellular tools, a unique collection of natural tissue extracts and our +20 years of expertise in the field. All these assets combined allowed us to become the CRO with the best scientific track record for GPCR deorphanization with 17 successful programs to this day.
Target Discovery
Our platform combines first-in-class cell lines, equipment and technologies to drive a deorphanization research program.
One of our competitive advantages comes from the wide collection of human and animal tissue extracts used for screening and identifying natural ligands for orphan GPCR. These extracts are processed using various protocols to enrich for peptides, proteins, biogenic amines, lipids (…) as sources of previously unknown receptor agonists.
We also have one of the largest library of orphan GPCR cell lines, verified for receptor expression by RT-PCR, FACS and/or constitutive signaling.
Last but not least, each program has to be strategically designed based on the latest knowledge of the target’s biology. For this you need a team of highly skilled and expert scientists, and you’ve come to the right place.
Deorphanization Track Record
| GPCR Target | Reference : patent application or publication |
| Undisclosed lipid receptor | to be published |
| GPR15 (Sponsored by Novartis) | WO 2015/069459A1 – Suply et al. Sci. Signal. 2017 |
| EBI2 (Sponsored by Novartis) | WO 2010/066689A2 – Hannedouche et al. Nature 2011 |
| GPR72 | EP1867994B1 & US7824866B2 |
| FPRL2 | EP1607745B1 – Migeotte et al. J. Exp. Med. 2005 |
| GPR43 | WO 2003/057730A1 – Le Poul et al. J. Biol. Chem. 2003 |
| GPR7 and GPR8 | WO 1995/12670A1 – Brézillon et al. J. Biol. Chem. 2003 |
| ChemR23 | WO 2003/006996A2 – Wittamer et al. J. Exp. Med. 2003 |
| P2Y13 | WO 2003/014731A2 – Communi et al. J. Biol. Chem. 2001 |
| NPFF2 | Kotani et al. Br. J. Pharmacol. 2001 |
| GPR54 | Kotani et al. J. Biol. Chem. 2001 |
| HCC1 | Detheux et al. J. Exp. Med. 2000 |
| P2Y11 | WO 1999/02675A1 – Communi et al. J. Biol. Chem. 1997 |
| CCR5 | WO 1997/32019A2 Samson et al. Biochemistry 1996 |
| ORL1 | WO 1997/07208A1 – Meunier et al. Nature 1995 |
| P2Y4 | WO 1997/19170A1 – Communi et al. Biochem. Biophys. Res. Commun. 1996 |
Publications
- A natural ligand for the orphan receptor GPR15 modulates lymphocyte recruitment to epithelia. T Suply, S Hannedouche, N Carte, J Li, B Grosshans, M Schaefer, L Raad, V Beck, S Vidal, A Hiou-Feige, N Beluch, S Barbieri, J Wirsching, N Lageyre, F Hillger, C Debon, J Dawson, P Smith, V Lannoy, M Detheux, F Bitsch, R Falchetto, T Bouwmeester, J Porter, B Baumgarten, K Mansfield, J M Carballido, K Seuwen and F Bassilina. (2017) Sci. Signal 10(496).
- Oxysterols direct immune cell migration via EBI2. S Hannedouche, J Zhang, T Yi, W Shen, D Nguyen, JP Pereira, D Guerini, BU Baumgarten, S Roggo, B Wen, R Knochenmuss, S Noel, F Gessier, LM Kelly, M Vanek, S Laurent, I Preuss, C Miault, I Christen, R Karuna, W Li, DI Koo, T Suply, C Schmedt, EC Peters, R Falchetto, A Katopodis, C Spanka, MO Roy, M Detheux, YA Chen, PG Schultz, CY Cho, K Seuwen, JG Cyster, and AW Sailer. (2011) Nature 475(7357): 524-7.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
