ORPHAN G-PROTEIN-COUPLED RECEPTORS - A NEGLECTED OPPORTUNITY FOR PIONEER DRUG DISCOVERY

Access to DNA databases has introduced an exciting new dimension to th e way biomedical research is conducted. 'Genomic research' offers trem endous opportunity for accelerating the identification of the cause of disease at the molecular level and thereby foster the discovery of mo re selective medicines to improve human health and longevity. The curr ent challenge is to close the gap rapidly between gene identification and clinical development of efficacious therapeutics. In the present r eview, Jeffrey Stadel, Shelagh Wilson and Derk Bergsma outline the rat ionale and describe strategies for converting one large class of novel genes, orphan G protein-coupled receptors (GPCRs), into therapeutic t argets. Historically, the superfamily of GPCRs has proven to be among the most successful drug targets and consequently these newly isolated orphan receptors have great potential for pioneer drug discovery.