BioCentury
ARTICLE | Translation in Brief

Pickpocketed orphans

How a new GPCR matching technique could identify ligands for orphan receptors

January 26, 2017 8:03 PM UTC

While G protein-coupled receptors (GPCRs) make good drug targets when the ligand is known, about 100 of the roughly 800-member family are orphan receptors, representing an untapped reservoir of potential drug targets. Now, researchers from the University of California San Diego and Australia have developed a computational model to match the orphan receptors with ligands that could serve as starting points for drug development.

The system, dubbed GPCR-CoINPocket (GPCR contact-informed neighboring pocket), was described last month in a Nature Chemical Biology paper from the UCSD team and their partners at the Victor Chang Cardiac Research Institute in New South Wales, who wrote that the system can find relationships, “even those undetected by phylogeny.” ...