Contribution of heteromerization to G protein-coupled receptor function

- Family A GPCRs can function as monomers but they also form higher order complexes.
- These complexes are involved in almost every step of the GPCR life cycle.
- They are also involved numerous neuropsychiatric conditions.
- GPCR heteromers represent novel targets for selective pharmacological treatments.

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.