Cell biology

Biology

Clathrin

Receptor

Signal transduction

Biochemistry

Endoplasmic reticulum

G protein

Endocytosis

Intracellular

Endosome

G protein-coupled receptor

Arrestin

Heterotrimeric G protein

Golgi apparatus

Chemistry

Trends in Pharmacological Sciences

G protein-coupled receptors (GPCRs) comprise a large and diverse class of signal-transducing receptors that undergo dynamic and isoform-specific membrane trafficking. GPCRs thus have an inherent potential to initiate or regulate signaling reactions from multiple membrane locations. This review discusses emerging insights into the subcellular organization of GPCR function in mammalian cells, focusing on signaling transduced by heterotrimeric G proteins and β-arrestins. We summarize recent evidence indicating that GPCR-mediated activation of G proteins occurs not only from the plasma membrane (PM) but also from endosomes and Golgi membranes and that β-arrestin-dependent signaling can be transduced from the PM by β-arrestin trafficking to clathrin-coated pits (CCPs) after dissociation from a ligand-activated GPCR.

Subcellular Organization of GPCR Signaling