title: G protein-coupled receptor deorphanizations.
abstract: G protein-coupled receptors (GPCRs) are major regulators of intercellular interactions. They initiate these actions by being activated by a wide variety of natural ligands. Historically, ligands were discovered first, but the advent of molecular biology reversed this trend. Most GPCRs are identified on the basis of their DNA sequences and thus are initially unmatched to known natural ligands. They are termed orphan GPCRs. Discovering their ligands-i.e., "deorphanizing" the GPCRs-gave birth to the field of reverse pharmacology. This review discusses the present status of GPCR deorphanization, presents a few examples of successes and surprises, and highlights difficulties encountered in these efforts.
authors.affiliation: Department of Pharmacology, University of California, Irvine, Irvine, California 92617, USA. ocivelli@uci.edu
authors.forename: Olivier
authors.initials: O
authors.lastname: Civelli
authors.forename: Rainer K
authors.initials: RK
authors.lastname: Reinscheid
authors.forename: Yan
authors.initials: Y
authors.lastname: Zhang
authors.forename: Zhiwei
authors.initials: Z
authors.lastname: Wang
authors.forename: Robert
authors.initials: R
authors.lastname: Fredriksson
authors.forename: Helgi B
authors.initials: HB
authors.lastname: Schiöth
mesh_terms: D000818:Animals; D006801:Humans; D008024:Ligands; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*
chemical_list: D008024:Ligands; D043562:Receptors, G-Protein-Coupled