Postgenomic characterization of G-protein-coupled receptors.
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.
Mertens
Inge
I
Laboratory of Developmental Physiology, Genomics and Proteomics, Katholieke Universiteit Leuven, Naamsestraat 59, 3000 Leuven, Belgium. inge.mertens@bio.kuleuven.ac.be
Vandingenen
Anick
A
Meeusen
Tom
T
De Loof
Arnold
A
Schoofs
Liliane
L
D000818:Animals; D001681:Biological Assay / Q000379:methods; D006801:Humans; D008024:Ligands; D043562:Receptors, G-Protein-Coupled / Q000235:genetics* / Q000378:metabolism
D008024:Ligands; D043562:Receptors, G-Protein-Coupled