GPCR signaling regulation: the role of GRKs and arrestins

VV Gurevich, EV Gurevich - Frontiers in pharmacology, 2019 - frontiersin.org
Every animal species expresses hundreds of different G protein-coupled receptors (GPCRs)
that respond to a wide variety of external stimuli. GPCRs-driven signaling pathways are …

Biased signalling: from simple switches to allosteric microprocessors

JS Smith, RJ Lefkowitz, S Rajagopal - Nature reviews Drug discovery, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …

Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD

C Cao, X Barros-Álvarez, S Zhang, K Kim, MA Dämgen… - Neuron, 2022 - cell.com
Summary Serotonin (5-hydroxytryptamine [5-HT]) 5-HT2-family receptors represent essential
targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs. Although the …

Structure of the neurotensin receptor 1 in complex with β-arrestin 1

W Huang, M Masureel, Q Qu, J Janetzko, A Inoue… - Nature, 2020 - nature.com
Arrestin proteins bind to active, phosphorylated G-protein-coupled receptors (GPCRs),
thereby preventing G-protein coupling, triggering receptor internalization and affecting …

GPCR dynamics: structures in motion

NR Latorraca, AJ Venkatakrishnan, RO Dror - Chemical reviews, 2017 - ACS Publications
The function of G protein-coupled receptors (GPCRs) which represent the largest class of
both human membrane proteins and drug targets depends critically on their ability to …

Regulation, signaling, and physiological functions of G-proteins

V Syrovatkina, KO Alegre, R Dey, XY Huang - Journal of molecular biology, 2016 - Elsevier
Heterotrimeric guanine-nucleotide-binding regulatory proteins (G-proteins) mainly relay the
information from G-protein-coupled receptors (GPCRs) on the plasma membrane to the …

GPCR-G protein-β-arrestin super-complex mediates sustained G protein signaling

ARB Thomsen, B Plouffe, TJ Cahill, AK Shukla… - Cell, 2016 - cell.com
Classically, G protein-coupled receptor (GPCR) stimulation promotes G protein signaling at
the plasma membrane, followed by rapid β-arrestin-mediated desensitization and receptor …

The diverse roles of arrestin scaffolds in G protein–coupled receptor signaling

YK Peterson, LM Luttrell, MC Michel - Pharmacological reviews, 2017 - Elsevier
The visual/β-arrestins, a small family of proteins originally described for their role in the
desensitization and intracellular trafficking of G protein–coupled receptors (GPCRs), have …

Distinct conformations of GPCR–β-arrestin complexes mediate desensitization, signaling, and endocytosis

TJ Cahill III, ARB Thomsen… - Proceedings of the …, 2017 - National Acad Sciences
β-Arrestins (βarrs) interact with G protein-coupled receptors (GPCRs) to desensitize G
protein signaling, to initiate signaling on their own, and to mediate receptor endocytosis …

[HTML][HTML] Rhodopsin, light-sensor of vision

KP Hofmann, TD Lamb - Progress in Retinal and Eye Research, 2023 - Elsevier
The light sensor of vertebrate scotopic (low-light) vision, rhodopsin, is a G-protein-coupled
receptor comprising a polypeptide chain with bound chromophore, 11-cis-retinal, that …