G protein-coupled receptor heteromer identification technology: identification and profiling of GPCR heteromers.

Traditionally, G protein-coupled receptors (GPCRs) were thought to function as monomeric units activating linear signaling pathways to reach a single functional response. However, it is now recognized that GPCRs can exist as higher order structures, such as homomers or heteromers. The potential for unique pharmacology attributed to these GPCR complexes has opened up the possibility of a new class of targets that can be exploited for drug discovery. In this innovation brief, a novel technology developed to identify and profile GPCR heteromers and their ligands will be reviewed.