Molecular mechanisms of fentanyl mediated β-arrestin biased signaling.
PLoS Computational Biology, 2020 The development of novel analgesics with improved safety profiles to combat the opioid epidemic represents a central question to G protein coupled receptor structural biology and pharmacology: What chemical features dictate G protein or β-arrestin ...
Parker W de Waal +7 more
doaj +1 more source
β-Arrestin1 and 2 differentially regulate PACAP-induced PAC1 receptor signaling and trafficking. [PDF]
PLoS ONE, 2018 A pituitary adenylate cyclase-activating polypeptide (PACAP)-specific receptor, PAC1R, is coupled with multiple signal transduction pathways including stimulation of adenylate cyclase, phospholipase C and extracellular-signal regulated kinase (ERK)1/2 ...
Yusuke Shintani +8 more
doaj +1 more source
The Effects of Apelin and Elabela Ligands on Apelin Receptor Distinct Signaling Profiles
Frontiers in Pharmacology, 2021 Apelin and Elabela are endogenous peptide ligands for Apelin receptor (APJ), a widely expressed G protein-coupled receptor. They constitute a spatiotemporal dual ligand system to control APJ signal transduction and function.
Yunlu Jiang +11 more
doaj +1 more source
Differential β-arrestin2 requirements for constitutive and agonist-induced internalization of the CB1 cannabinoid receptor [PDF]
, 2013 CB1 cannabinoid receptor (CB1R) undergoes both constitutive and agonist-induced internalization, but the underlying mechanisms of these processes and the role of beta-arrestins in the regulation of CB1R function are not completely understood.
Ahn +64 more
core +1 more source
Environmental Toxicology and Chemistry, EarlyView.Abstract There is increasing concern regarding pollutants disrupting the vertebrate thyroid hormone (TH) system, which is crucial for development. Thus, identification of TH system–disrupting chemicals (THSDCs) is an important requirement in the Organisation for Economic Co‐operation and Development (OECD) testing framework.
Lisa Gölz +9 more
wiley +1 more source
Lipids modulate the dynamics of GPCR:β-arrestin interaction
Nature Communicationsβ-arrestins are key molecular partners of G Protein-Coupled Receptors (GPCRs), triggering not only their desensitization but also intracellular signaling.
Antoniel A. S. Gomes +8 more
doaj +1 more source
Phosphorylation-induced conformation of beta(2)-adrenoceptor related to arrestin recruitment revealed by NMR [PDF]
, 2018 The C-terminal region of G-protein-coupled receptors (GPCRs), stimulated by agonist binding, is phosphorylated by GPCR kinases, and the phosphorylated GPCRs bind to arrestin, leading to the cellular responses.
Imai, Shunsuke +8 more
core +2 more sources
The Endothelial CXCR Family in Vascular Health and Disease
iNew Medicine, EarlyView.ABSTRACT Endothelial cells (ECs) form the dynamic interface between blood and tissue, serving as key regulators of vascular homeostasis, inflammation, and repair. Among the molecular systems governing endothelial behavior, the C‐X‐C motif chemokine receptor (CXCR) family—originally characterized in immunology for its roles in leukocyte trafficking and ...
Zhiming Wu +4 more
wiley +1 more source
ACKR3 Regulation of Neuronal Migration Requires ACKR3 Phosphorylation, but Not β-Arrestin
Cell Reports, 2019 Summary: Phosphorylation of heptahelical receptors is thought to regulate G protein signaling, receptor endocytosis, and non-canonical signaling via recruitment of β-arrestins.
Friederike Saaber +10 more
doaj +1 more source
Loss of biased signaling at a G protein-coupled receptor in overexpressed systems.
PLoS ONE, 2023 G protein-coupled receptors (GPCRs) regulate cellular signaling pathways by coupling to two classes of transducers: heterotrimeric G proteins and β-arrestins.
Angus Li +4 more
doaj +1 more source