Understanding the physiological significance of GPCR dimers and oligomers

Abstract

The significance of G protein-coupled receptor (GPCR) oligomerization has been a subject of intense study which still remains controversial. Functional class C GPCRs are well accepted as obligate dimers but scepticism still remains with regards to the generalizability of this phenomenon when considering other classes of GPCRs. Here, we focus on understanding the organization and relationships between receptor equivalents in oligomeric receptor complexes. We discuss receptor properties such as ligand binding cooperativity which can be best explained in the context of functional oligomeric entities, and the asymmetries in receptor structure and function created by oligomers as well as their implications for drug discovery.