title: Postgenomic characterization of G-protein-coupled receptors.
abstract: G-protein-coupled receptors (GPCRs) constitute one of the largest families of membrane-spanning proteins. Their importance in drug development has been proven over and over again. Therefore, they remain one of the most significant groups of molecules to be characterized. In the postgenomic era, the methods used for the characterization of GPCRs have dramatically changed: the predicted orphan receptors are now often used to ascertain the ligands (reverse pharmacology), whereas, in the past, the bioactive ligand was used to identify the receptor (classic approach). In this review, we will give an overview of the recent postgenomic functional assays that are frequently used to link the orphan GPCR of both vertebrate and invertebrate organisms with their ligands.
authors.affiliation: Laboratory of Developmental Physiology, Genomics and Proteomics, Katholieke Universiteit Leuven, Naamsestraat 59, 3000 Leuven, Belgium. inge.mertens@bio.kuleuven.ac.be
authors.forename: Inge
authors.initials: I
authors.lastname: Mertens
authors.forename: Anick
authors.initials: A
authors.lastname: Vandingenen
authors.forename: Tom
authors.initials: T
authors.lastname: Meeusen
authors.forename: Arnold
authors.initials: A
authors.lastname: De Loof
authors.forename: Liliane
authors.initials: L
authors.lastname: Schoofs
mesh_terms: D000818:Animals; D001681:Biological Assay / Q000379:methods; D006801:Humans; D008024:Ligands; D043562:Receptors, G-Protein-Coupled / Q000235:genetics* / Q000378:metabolism
chemical_list: D008024:Ligands; D043562:Receptors, G-Protein-Coupled