Institut de Recherche Interdisciplinaire en Biologie Humaine et Moléculaire

G protein-coupled receptors (GPCRs)

[ JM Boeynaems, David Communi, Didier Communi, S.Costagliola, Langer Ingrid, C.Ledent, F.Libert, M.Parmentier, I.Pirson, B.Robaye, G.Vassart]

After having pioneered the cloning by homology of rhodopsin-like GPCRs, the Institute has built expertise in the study of a variety of GPCR subfamilies. These include mainly the glycoprotein hormone receptors, receptors for chemokines and other leucocyte chemoattractants, adenosine receptors, P2Y nucleotide receptors, cannabinoid receptors and neuropeptide receptors. Current studies concentrate on structure-function relationships, regulation of downstream regulatory cascades and gene expression by microarrays, in vivo phenotypic studies of mice wgith invalidated receptor genes, role of GPCRs in tumorigenesis, role of homo- and hetero-dimerization of GPCRs. A strong emphasis is put on the identification of the natural agonists of a diversity of orphan GPCRs

Gilbert VASSART group

Isabelle Garcia

Roxana Mustata

Tom Van Loy

Sandra Strollo




Main recent publications

Blanpain C, Vanderwinden JM, Cihak J, Wittamer V, Le Poul E, Issafras H, Stangassinger M, Vassart G, Marullo S, Schlondorff D, Parmentier M, Mack M.

Multiple active states and oligomerization of CCR5 revealed by functional properties of monoclonal antibodies.
Mol. Biol. Cell. 13:723-37 ( 2002).

Costagliola S, Panneels V, Bonomi M, Koch J, Many MC, Smits G, Vassart G.

Tyrosine sulfation is required for agonist recognition by glycoprotein hormone receptors.
EMBO J. 21:504-13 (2002).

Vlaeminck-Guillem V, Ho SC, Rodien P, Vassart G, Costagliola S.

Activation of the cAMP Pathway by the TSH Receptor Involves Switching of the Ectodomain from a Tethered Inverse Agonist to an Agonist.
Mol.Endocrinol. 16:736-46 (2002).

Robaye B,   Ghanem E, Wilkin F, Fokan D, Van Driessche W, Schurmans S, Boeynaems J-M, Beauwens R

Loss of nucleotide regulation of epithelial chloride transport in the jejunum of P2Y 4 -null mice
Mol Pharmacol, 63:777-783 (2003).

Smits G, Olatunbosun O, Delbaere A, Pierson R, Vassart G, Costagliola S.

Ovarian hyperstimulation syndrome due to a mutation in the follicle-stimulating hormone receptor.
New England Journal of Medicine 349:760-6 (2003).

Smits G, Campillo M, Govaerts C, Janssens V, Richter C, Vassart G, Pardo L, Costagliola S.

Glycoprotein hormone receptors: determinants in leucine-rich repeats responsible for ligand specificity.
EMBO J 22:2692-703 (2003).

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.

Specific Recruitment of Antigen-presenting Cells by Chemerin, a Novel Processed Ligand from Human Inflammatory Fluids.
J.Exp.Med. 198:977-85 (2003).

Vassart G, Pardo L, Costagliola S.

A molecular dissection of the glycoprotein hormone receptors.
Trends Biochem.Sci. 29:119-26 (2004).

Marteau F, Suarez Gonzalez N, Communi D, Goldman M, Boeynaems J-M, Communi D.

Thrombospondin-1 and indoleamine 2,3-dioxygenase are major targets of extracellular ATP in human dendritic cells
Blood, 106 :3860-3866 (2005).

Ledent C, Demeestere I, Blum D, Petermans J, Hamalainen T, Smits G, Vassart G.

Premature ovarian aging in mice deficient for Gpr3.
Proc.Natl.Acad.Sci.U.S A 102:8922-6 (2005).

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.

Identification and characterization of an endogenous chemotactic ligand specific for FPRL2
J Exp Med. 201:83-93 (2005).

Urizar E, Montanelli L, Loy T, Bonomi M, Swillens S, Gales C, Bouvier M, Smits G, Vassart G, Costagliola S.

Glycoprotein hormone receptors: link between receptor homodimerization and negative cooperativity. EMBO J. 24:1954-64 (2005).

Laurent P, Becker JAJ, Valverde O, Ledent C, de Kerchove d’Exaerde A, Schiffmann SN, Maldonado R, Vassart G and Parmentier M.

The prolactin-releasing peptide acts as a functional antagonist of the opioid system through its receptor GPR10.
Nature Neurosciences, 8:1735-1741 (2005).

El-Asmar L, Springael JY, Ballet S, Urizar Andrieu E, Vassart G, Parmentier M.

Evidence for negative binding cooperativity within CCR5-CCR2b heterodimers.
Mol Pharmacol. 67:460-469 (2005).


Bar I, Guns PJ, Metallo J, Cammarata D, Wilkin F, Boeynams JM, Bult H, Robaye B.

Knockout mice reveal a role for P2Y6 receptor in macrophages, endothelial cells, and vascular smooth muscle cells.
Mol Pharmacol. 2008;74(3):777-84.

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