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Orphan GPCR research
Author(s) -
Chung S,
Funakoshi T,
Civelli O
Publication year - 2008
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1038/sj.bjp.0707606
Subject(s) - g protein coupled receptor , receptor , molecular pharmacology , endogeny , orphan receptor , computational biology , neuropeptide , biology , pharmacology , bioinformatics , neuroscience , gene , biochemistry , transcription factor
Orphan G protein‐coupled receptors (GPCRs) are receptors lacking endogenous ligands. Found by molecular biological analyses, they became the roots of reverse pharmacology, in which receptors are attempted to be matched to potential transmitters. Later, when high‐throughput screening technology was applied to reverse pharmacology, dozens of orphan GPCRs became deorphanized. Furthermore, novel neuropeptides were discovered. This review retraces the history of the orphan GPCRs and of the discoveries of their endogenous ligands, it also discusses the difficulties that the search for new ligands is presently encountering. British Journal of Pharmacology (2008) 153 , S339–S346; doi: 10.1038/sj.bjp.0707606 ; published online 10 December 2007