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 …

Mechanisms of signalling and biased agonism in G protein-coupled receptors

D Wootten, A Christopoulos, M Marti-Solano… - … reviews Molecular cell …, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest group of cell surface receptors in
humans that signal in response to diverse inputs and regulate a plethora of cellular …

TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome

RHJ Olsen, JF DiBerto, JG English, AM Glaudin… - Nature chemical …, 2020 - nature.com
G-protein-coupled receptors (GPCRs) remain major drug targets, despite our incomplete
understanding of how they signal through 16 non-visual G-protein signal transducers …

Non-canonical β-adrenergic activation of ERK at endosomes

Y Kwon, S Mehta, M Clark, G Walters, Y Zhong, HN Lee… - Nature, 2022 - nature.com
G-protein-coupled receptors (GPCRs), the largest family of signalling receptors, as well as
important drug targets, are known to activate extracellular-signal-regulated kinase (ERK)—a …

β− Arrestins: structure, function, physiology, and pharmacological perspectives

J Wess, AB Oteng, O Rivera-Gonzalez… - Pharmacological …, 2023 - Elsevier
The two β-arrestins, β-arrestin-1 and-2 (systematic names: arrestin-2 and-3, respectively),
are multifunctional intracellular proteins that regulate the activity of a very large number of …

Conformational basis of G protein-coupled receptor signaling versatility

LM Wingler, RJ Lefkowitz - Trends in cell biology, 2020 - cell.com
G protein-coupled receptors (GPCRs) are privileged structural scaffolds in biology that have
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …

G-protein–coupled receptors in heart disease

J Wang, C Gareri, HA Rockman - Circulation research, 2018 - Am Heart Assoc
GPCRs (G-protein [guanine nucleotide-binding protein]–coupled receptors) play a central
physiological role in the regulation of cardiac function in both health and disease and thus …

[HTML][HTML] Membrane phosphoinositides regulate GPCR-β-arrestin complex assembly and dynamics

J Janetzko, R Kise, B Barsi-Rhyne, DH Siepe… - Cell, 2022 - cell.com
Binding of arrestin to phosphorylated G protein-coupled receptors (GPCRs) is crucial for
modulating signaling. Once internalized, some GPCRs remain complexed with β-arrestins …

Conformational transitions of a neurotensin receptor 1–Gi1 complex

HE Kato, Y Zhang, H Hu, CM Suomivuori, FMN Kadji… - Nature, 2019 - nature.com
Abstract Neurotensin receptor 1 (NTSR1) is a G-protein-coupled receptor (GPCR) that
engages multiple subtypes of G protein, and is involved in the regulation of blood pressure …

Mini G protein probes for active G protein–coupled receptors (GPCRs) in live cells

Q Wan, N Okashah, A Inoue, R Nehmé… - Journal of Biological …, 2018 - ASBMB
G protein–coupled receptors (GPCRs) are key signaling proteins that regulate nearly every
aspect of cell function. Studies of GPCRs have benefited greatly from the development of …