Current Opinion in Pharmacology vol:12 issue:6 pages:647-652
GPR39 is an orphan GPCR receptor belonging to the ghrelin/motilin receptor subfamily. The receptor is constitutively active and Zn(2+) is a physiological agonist of GPR39. The receptor is emerging as an important regulator of gastrointestinal motility and secretion. Although GPR39 does not seem to be involved in the regulation of food intake, contradictory results are available on the role of GPR39 in the regulation of body weight. A well-established stimulatory role for GPR39 has been defined in insulin secretion which makes the receptor an attractive target for the treatment of type 1 or 2 diabetes. GPR39 signaling also inhibits apoptosis and mediates neural synaptic signaling. Novel ligands of GPR39 are warranted to reveal the main physiological role of this receptor.