title: Alternative drug discovery approaches for orphan GPCRs.
abstract: G protein-coupled receptors (GPCRs) are well-known drug targets. However, a question mark remains for the more than 100 orphan GPCRs as current deorphanisation strategies failed to identify specific ligands for these receptors. Recent advances have shown that orphan GPCRs may have important functions that are ligand-independent. Orphan GPCRs can modulate the function of well-defined drug targets such as GPCRs with identified ligands and neurotransmitter transporters though physical association with those molecules. Thus, compounds that bind to orphan GPCRs and allosterically regulate the function of the interacting partner or even disrupt the interaction with the latter could become new drugs.
authors.affiliation: Institut Cochin, Université Paris Descartes, CNRS (UMR 8104), Department of Cell Biology, Paris, France.
authors.forename: Angélique
authors.initials: A
authors.lastname: Levoye
authors.forename: Ralf
authors.initials: R
authors.lastname: Jockers
mesh_terms: D015195:Drug Design; D004345:Drug Industry; D008024:Ligands; D043562:Receptors, G-Protein-Coupled / Q000502:physiology*; D015398:Signal Transduction; D013678:Technology, Pharmaceutical / Q000379:methods*
chemical_list: D008024:Ligands; D043562:Receptors, G-Protein-Coupled