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GPCRs and Signal Transducers: Interaction Stoichiometry.

Gurevich VV, Gurevich EV
Trends Pharmacol Sci. 2018 39 (7): 672-684

PMID: 29739625 · PMCID: PMC6005764 · DOI:10.1016/j.tips.2018.04.002

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.

Copyright © 2018 Elsevier Ltd. All rights reserved.

MeSH Terms (6)

Animals Arrestins GTP-Binding Proteins Humans Receptors, G-Protein-Coupled Signal Transduction

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