biostudies-literatureGaitonde SANIMH NIH HHS23-31https://www.ebi.ac.uk/biostudies/studies/S-EPMC5395348biostudies-literatureUnknown32G protein-coupled receptors (GPCRs) are a remarkably multifaceted family of transmembrane proteins that exert a variety of physiological effects. Although family A GPCRs are able to operate as monomers, there is increasing evidence that heteromerization represents a fundamental aspect of receptor function, trafficking and pharmacology. Most recently, it has been suggested that GPCR heteromers may play a crucial role as new molecular targets of heteromer-selective and bivalent ligands. The current review summarizes key recent developments in these topics.Current opinion in pharmacologyContribution of heteromerization to G protein-coupled receptor function.PMC5395348R01 MH084894Gonzalez-Maeso JGaitonde SAfalseContribution of heteromerization to G protein-coupled receptor function.G protein-coupled receptors (GPCRs) are a remarkably multifaceted family of transmembrane proteins that exert a variety of physiological effects. Although family A GPCRs are able to operate as monomers, there is increasing evidence that heteromerization represents a fundamental aspect of receptor function, trafficking and pharmacology. Most recently, it has been suggested that GPCR heteromers may play a crucial role as new molecular targets of heteromer-selective and bivalent ligands. The current review summarizes key recent developments in these topics.2017-01-01T00:00:00Z2017 Feb2024-11-21T00:02:29.998Z2019-03-26T22:59:39ZS-EPMC53953482783580010.1016/j.coph.2016.10.006