Regular Article
G protein-coupled receptor adaptation mechanisms

https://doi.org/10.1006/scdb.1997.0216Get rights and content

Abstract

G protein-coupled receptors (GPCRs) transduce extracellular signals that modulate the activity of a wide variety of biological processes, such as neurotransmission, chemoattraction, cardiac function, olfaction, and vision. However, GPCR signalling desensitizes rapidly as the consequence of receptor phosphorylation. G protein-coupled receptor kinase-mediated receptor phosphorylation promotes the binding of β-arrestin proteins, which not only uncouple GPCRs from their cognate heterotrimeric G protein, but also target them for endocytosis. The sequestration (endocytosis) of desensitized GPCRs to endosomes is required for their dephosphorylation and subsequent resensitization to their pre-ligand exposed state. This review concentrates on the mechanisms underlying GPCR desensitization and resensitization.

References (0)

Cited by (161)

  • Association between common genetic variants of α2A-, α2B-, and α2C-adrenergic receptors and ischemic stroke

    2013, Clinical Neurology and Neurosurgery
    Citation Excerpt :

    Fifth, we could not study whole SNP markers of ADRA2 gene, their haplotypes or relevant receptor functions. However, the ADRA2B 301–303 I/D are known to be functional polymorphisms that can alter gene expression and receptor function [23]. Additionally, haplotype analysis using eight SNP markers of ADRA2B showed that two common haplotypes (one haplotype containing the D allele and another containing a non-D allele) could account for most of the total haplotypes (95% of Caucasians and 89% of African Americans) [16].

View all citing articles on Scopus

Unspecified

View full text