Arrestin interactions with G protein-coupled receptors

Handbook of Experimental Pharmacology
M J Lohse, Carsten Hoffmann

Abstract

G-protein-coupled receptors (GPCRs) are the primary interaction partners for arrestins. The visual arrestins, arrestin1 and arrestin4, physiologically bind to only very few receptors, i.e., rhodopsin and the color opsins, respectively. In contrast, the ubiquitously expressed nonvisual variants β-arrestin1 and 2 bind to a large number of receptors in a fairly nonspecific manner. This binding requires two triggers, agonist activation and receptor phosphorylation by a G-protein-coupled receptor kinase (GRK). These two triggers are mediated by two different regions of the arrestins, the "phosphorylation sensor" in the core of the protein and a less well-defined "activation sensor." Binding appears to occur mostly in a 1:1 stoichiometry, involving the N-terminal domain of GPCRs, but in addition a second GPCR may loosely bind to the C-terminal domain when active receptors are abundant.Arrestin binding initially uncouples GPCRs from their G-proteins. It stabilizes receptors in an active conformation and also induces a conformational change in the arrestins that involves a rotation of the two domains relative to each other plus changes in the polar core. This conformational change appears to permit the interaction with further downstre...Continue Reading

Citations

May 11, 2017·Journal of Medicinal Chemistry·Barbara MännelPeter Gmeiner
Feb 22, 2017·Nature Communications·Ciara C M LallyMartha E Sommer
Jun 16, 2017·Molecular Biology of the Cell·Yukari Okamoto, Sojin Shikano
Jul 22, 2014·Nature·Arun K ShuklaRobert J Lefkowitz
Sep 22, 2015·Acta Pharmacologica Sinica·Yuan-jing GuWei Wei
Jul 23, 2015·Journal of Molecular Medicine : Official Organ of the Gesellschaft Deutscher Naturforscher Und Ärzte·Martin J Lohse
Jul 1, 2014·Journal of Cellular and Molecular Medicine·Jing ZhaoDeling Yin
Jul 18, 2015·Molecular Pharmacology·Martin J Lohse, Klaus Peter Hofmann
Jun 25, 2017·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Fang ZhangQin Wang
Jan 27, 2019·Scientific Reports·Raphael S HaiderMartin K Ostermaier
Apr 2, 2019·Frontiers in Endocrinology·Flavie LandomielEric Reiter
Jun 17, 2020·Nature Chemical Biology·Jan MöllerMartin J Lohse
Jan 31, 2016·Archives of Pharmacal Research·Ji Young ParkKa Young Chung
Jun 28, 2017·Proceedings of the National Academy of Sciences of the United States of America·Seung-Ryoung JungBertil Hille
Jan 10, 2021·Biochimica Et Biophysica Acta. Proteins and Proteomics·Yaejin YunHyung Ho Lee
Mar 9, 2021·The Journal of Biological Chemistry·Maria Hauge PedersenJonathan A Javitch
Apr 20, 2021·The FEBS Journal·Daniel Hilger
Aug 6, 2021·Scientific Reports·Nuttawadee NgamlertwongTaka-Aki Koshimizu
Sep 12, 2021·Proceedings of the National Academy of Sciences of the United States of America·Changxiu QuKa Young Chung
Mar 4, 2022·Cell Communication and Signaling : CCS·Hao ChenHuirong Liu
Feb 18, 2014·Current Opinion in Cell Biology·Martin J LohseDavide Calebiro

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.