Format

Send to

Choose Destination
Trends Pharmacol Sci. 2018 Jul;39(7):672-684. doi: 10.1016/j.tips.2018.04.002. Epub 2018 May 5.

GPCRs and Signal Transducers: Interaction Stoichiometry.

Author information

1
Department of Pharmacology, Vanderbilt University, Nashville, TN 37232, USA. Electronic address: vsevolod.gurevich@vanderbilt.edu.
2
Department of Pharmacology, Vanderbilt University, Nashville, TN 37232, USA.

Abstract

Until the late 1990s, class A G protein-coupled receptors (GPCRs) were believed to function as monomers. Indirect evidence that they might internalize or even signal as dimers has emerged, along with proof that class C GPCRs are obligatory dimers. Crystal structures of GPCRs and their much larger binding partners were consistent with the idea that two receptors might engage a single G protein, GRK, or arrestin. However, recent biophysical, biochemical, and structural evidence invariably suggests that a single GPCR binds G proteins, GRKs, and arrestins. Here we review existing evidence of the stoichiometry of GPCR interactions with signal transducers and discuss potential biological roles of class A GPCR oligomers, including proposed homo- and heterodimers.

KEYWORDS:

G proteins; GPCRs; GRKs; arrestins; oligomerization

PMID:
29739625
DOI:
10.1016/j.tips.2018.04.002
[Indexed for MEDLINE]
Free PMC Article

Supplemental Content

Full text links

Icon for Elsevier Science Icon for PubMed Central
Loading ...
Support Center