title: G protein-coupled receptor adaptation mechanisms.
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 beta-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.
authors.affiliation: John P. Robarts Research Institute, London, Ontario, Canada.
authors.forename: S S
authors.initials: SS
authors.lastname: Ferguson
authors.forename: M G
authors.initials: MG
authors.lastname: Caron
mesh_terms: D000222:Adaptation, Physiological; D000818:Animals; D019390:Arrestins / Q000502:physiology; D019204:GTP-Binding Proteins / Q000502:physiology*; D006801:Humans; D020794:Receptor Protein-Tyrosine Kinases / Q000502:physiology; D011956:Receptors, Cell Surface / Q000502:physiology*
chemical_list: D019390:Arrestins; D011956:Receptors, Cell Surface; D020794:Receptor Protein-Tyrosine Kinases; D019204:GTP-Binding Proteins