Identifying orphan G protein coupled receptors in drug discovery

Authors: John Dunlop, Richard M Eglen
Publisher/Year: Drug Discovery Today: Technologies. 2004 Sep;1(1):61-68.
Pub Med ID/Journal ID:


G-protein coupled receptors (GPCRs) represent the most tractable family of drug targets. Those GPCRs identified by sequence only, but lacking an endogenous ligand, are defined as orphan GPCRs (oGPCRs) and might represent the next generation of targets for GPCR drug discovery. Drug discovery at oGPCRs is a resource intensive approach and frequently taken ‘at-risk’ without a clear understanding of the role in a disease. Identification of oGPCRs is, therefore, a prerequisite for the initiation of a drug discovery program.