New insights into the functional impact of G protein–coupled receptor oligomerization

Abstract The classical idea of a G protein–coupled receptor (GPCR) activating a single signal pathway has been superseded by the concept of functional pleiotropy for this receptor superfamily. One mechanism that has been shown to facilitate such multifaceted roles of GPCRs is the association of GPCRs to form dimers and oligomers, either with self (homomerization) or distinct GPCRs (heteromerization). This review explores the recent advances in our understanding of the structural and functional complexities of GPCR di/oligomerization, describing how our evolving models of these receptor complexes may provide novel and more selective modes of pharmacological tuning.