Biomol Ther.  2017 Jan;25(1):26-43. 10.4062/biomolther.2016.186.

Multifactorial Regulation of G Protein-Coupled Receptor Endocytosis

• Zhang X
• Kim KM

• KMID: 2367617
• DOI: http://doi.org/10.4062/biomolther.2016.186

Abstract

Endocytosis is a process by which cells absorb extracellular materials via the inward budding of vesicles formed from the plasma membrane. Receptor-mediated endocytosis is a highly selective process where receptors with specific binding sites for extracellular molecules internalize via vesicles. G protein-coupled receptors (GPCRs) are the largest single family of plasma-membrane receptors with more than 1000 family members. But the molecular mechanisms involved in the regulation of GPCRs are believed to be highly conserved. For example, receptor phosphorylation in collaboration with β-arrestins plays major roles in desensitization and endocytosis of most GPCRs. Nevertheless, a number of subsequent studies showed that GPCR regulation, such as that by endocytosis, occurs through various pathways with a multitude of cellular components and processes. This review focused on i) functional interactions between homologous and heterologous pathways, ii) methodologies applied for determining receptor endocytosis, iii) experimental tools to determine specific endocytic routes, iv) roles of small guanosine triphosphate-binding proteins in GPCR endocytosis, and v) role of post-translational modification of the receptors in endocytosis.

Keyword

G protein-coupled receptor; Endocytosis; Ral; ARF6; Glycosylation; Palmitoylation

MeSH Terms

Binding Sites
Cell Membrane
Cooperative Behavior
Endocytosis*
Glycosylation
Guanosine
Humans
Lipoylation
Phosphorylation
Protein Processing, Post-Translational
Guanosine