scholarly journals Seeing β-arrestin in action: The role of β-arrestins in Histamine 1 Receptor signaling

2019 ◽  
Author(s):  
A Pietraszewska-Bogiel ◽  
J Goedhart
Keyword(s):  
G Protein ◽  
Live Cell ◽  
Chemical Mediator ◽  
Intracellular Location ◽  
Erk Activation ◽  
Class A ◽  
Transient Interactions ◽  
Major Chemical ◽  
G Protein Coupled

ABSTRACTß-arrestins regulate G protein-coupled receptor functions by influencing their signaling activity and intracellular location. Histamine is a major chemical mediator of allergic reactions, and its action is mainly mediated by the Gq/11- and Gi-coupled H1R. Contrary to accumulating insights into G protein-mediated signaling downstream of H1R, very little is known about the function of ß-arrestins in H1R signaling. Here, we describe dynamic, live cell measurements of ß-arrestin recruitment upon H1R activation in HEK293TN cells. Our observations classify H1R as a class A receptor, undergoing transient interactions with ß-arrestin. To investigate the relative contributions of G proteins and ß-arrestins to H1R signaling, we use specific G protein inhibitors, as well as ß-arrestin overexpression and depletion, and quantify various signaling outcomes in a panel of dynamic, live cell biosensor assays. Overall, we link ß-arrestins to desensitization of H1R-mediated signaling and show that ERK activation downstream of endogenous (HeLa, HUVEC) or transiently expressed (HEK293TN) H1R is largely Gq-mediated.

scholarly journals Interaction of class A G protein-coupled receptors with G proteins.

2004 ◽  
Vol 51 (1) ◽  
pp. 129-136 ◽  
Author(s):  
Rafał Slusarz ◽  
Jerzy Ciarkowski
Keyword(s):  
G Protein ◽  
G Proteins ◽  
G Protein Coupled Receptors ◽  
Alpha Subunit ◽  
Protein Activation ◽  
Class A ◽  
G Protein Activation ◽  
G Protein Coupled ◽  
Receptor Dimer

A model for interaction of class A G protein-coupled receptor with the G protein G(alpha) subunit is proposed using the rhodopsin-transducin (RD/Gt) prototype. The model combines the resolved interactions/distances, essential in the active RD*/Gt system, with the structure of Gt(alpha) C-terminal peptide bound to RD* while stabilizing it. Assuming the interactions involve conserved parts of the partners, the model specifies the conserved Helix 2 non-polar X- - -X, Helix 3 DRY and Helix 7/8 NP- -Y- - F RD* motifs interacting with the Gt(alpha) C-terminal peptide, in compliance with the structure of the latter. A concomitant role of Gt(alpha) and Gt(gamma) C-termini in stabilizing RD* could possibly be resolved assuming a receptor dimer as requisite for G protein activation.

Marijuana and β-estradiol interactions on spatial learning and memory in young female rats: Lack of role of the G protein-coupled estrogen receptor (GPR30)

Life Sciences ◽  
2021 ◽  
pp. 119723
Author(s):  
Mohadeseh Chahkandi ◽  
Gholamreza Komeili ◽  
Gholamreza Sepehri ◽  
Mohammad Khaksari ◽  
Sedigheh Amiresmaili
Keyword(s):  
Estrogen Receptor ◽  
Learning And Memory ◽  
G Protein ◽  
Spatial Learning ◽  
Young Female ◽  
Female Rats ◽  
Spatial Learning And Memory ◽  
G Protein Coupled

scholarly journals Constitutive Activity among Orphan Class-A G Protein Coupled Receptors

PLoS ONE ◽  
2015 ◽  
Vol 10 (9) ◽  
pp. e0138463 ◽  
Author(s):  
Adam L. Martin ◽  
Michael A. Steurer ◽  
Robert S. Aronstam
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptors ◽  
Constitutive Activity ◽  
Class A ◽  
G Protein Coupled

scholarly journals The apelin receptor: physiology, pathology, cell signalling, and ligand modulation of a peptide-activated class A GPCR

2014 ◽  
Vol 92 (6) ◽  
pp. 431-440 ◽  
Author(s):  
Nigel A. Chapman ◽  
Denis J. Dupré ◽  
Jan K. Rainey
Keyword(s):  
G Protein ◽  
Cell Signalling ◽  
Wide Distribution ◽  
Peptide Ligand ◽  
Cellular Effects ◽  
Class A ◽  
Promising Therapeutic Target ◽  
Apelin Receptor ◽  
Obesity And Cancer ◽  
G Protein Coupled

The apelin receptor (AR or APJ) is a class A (rhodopsin-like) G-protein-coupled receptor with wide distribution throughout the human body. Activation of the AR by its cognate peptide ligand, apelin, induces diverse physiological effects including vasoconstriction and dilation, strengthening of heart muscle contractility, angiogenesis, and regulation of energy metabolism and fluid homeostasis. Recently, another endogenous peptidic activator of the AR, Toddler/ELABELA, was identified as having a crucial role in zebrafish (Danio rerio) embryonic development. The AR is also implicated in pathologies including cardiovascular disease, diabetes, obesity, and cancer, making it a promising therapeutic target. Despite its established importance, the precise roles of AR signalling remain poorly understood. Moreover, little is known about the mechanisms of peptide–AR activation. Additional complexity arises from modulation of the AR by 2 endogenous peptide ligands, both with multiple bioactive isoforms of variable length and distribution. The various apelin and Toddler/ELABELA isoforms may also produce distinct cellular effects. Further complexity arises through formation of functionally distinct heterodimers between the AR and other G-protein-coupled receptors. This minireview outlines key (patho)physiological actions of the AR, addresses what is known about signal transduction downstream of AR activation, and concludes by discussing unique properties of the endogenous peptidic ligands of the AR.

Role of the endogenous obestatin/G-protein coupled receptor 39 (GPR39) system in the regulation of proliferation and migration of activated human pancreatic stellate cells

Pancreatology ◽  
2018 ◽  
Vol 18 (4) ◽  
pp. S118
Author(s):  
Lara Estévez-Perez ◽  
Saul Leal-lopez ◽  
Agustin Sanchez-Temprano ◽  
Begoña Otero-Alen ◽  
Carlos Seoane-Mosteiro ◽  
...  
Keyword(s):  
G Protein ◽  
Stellate Cells ◽  
Pancreatic Stellate Cells ◽  
G Protein Coupled Receptor ◽  
Regulation Of Proliferation ◽  
And Migration ◽  
G Protein Coupled ◽  
Proliferation And Migration

G-protein-coupled receptor regulation: role of G-protein-coupled receptor kinases and arrestins

1996 ◽  
Vol 74 (10) ◽  
pp. 1095-1110 ◽  
Author(s):  
SSG Ferguson ◽  
L S Barak ◽  
J Zhang ◽  
M G Caron
Keyword(s):  
G Protein ◽  
Receptor Regulation ◽  
G Protein Coupled Receptor ◽  
Receptor Kinases ◽  
G Protein Coupled
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