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Opposing functions of β-arrestin 1 and 2 in Parkinson’s disease via microglia inflammation and Nprl3
Although β-arrestins (ARRBs) regulate diverse physiological and pathophysiological processes, their functions and regulation in Parkinson’s disease...
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Exendin-4 Attenuates Remodeling in the Remote Myocardium of Rats After an Acute Myocardial Infarction by Activating β-Arrestin-2, Protein Phosphatase 2A, and Glycogen Synthase Kinase-3 and Inhibiting β-Catenin
PurposeThis study tested if the protective anti-remodeling effect of GLP-1 agonist Exendin-4 after an acute myocardial infarction (MI) in rats...
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Structure of the M2 muscarinic receptor–β-arrestin complex in a lipid nanodisc
After activation by an agonist, G-protein-coupled receptors (GPCRs) recruit β-arrestin, which desensitizes heterotrimeric G-protein signalling and...
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Structure of the neurotensin receptor 1 in complex with β-arrestin 1
Arrestin proteins bind to active, phosphorylated G-protein-coupled receptors (GPCRs), thereby preventing G-protein coupling, triggering receptor...
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Identification of 5-HT2A receptor signaling pathways associated with psychedelic potential
Serotonergic psychedelics possess considerable therapeutic potential. Although 5-HT 2A receptor activation mediates psychedelic effects, prototypical...
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The mechanism of 25-hydroxycholesterol-mediated suppression of atrial β1-adrenergic responses
25-Hydroxycholesterol (25HC) is a biologically active oxysterol, whose production greatly increases during inflammation by macrophages and dendritic...
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Profiling of basal and ligand-dependent GPCR activities by means of a polyvalent cell-based high-throughput platform
Representing the most attractive and successful druggable receptors of the proteome, GPCRs regulate a myriad of physiological and pathophysiological...
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Correction to: In vitro structure–activity relationship determination of 30 psychedelic new psychoactive substances by means of β-arrestin 2 recruitment to the serotonin 2A receptor
It has been brought to the authors’ attention that Fig. 1 of “In vitro structure–activity relationship determination of 30 psychedelic new...
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β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the same GPCR in living cells
β-arrestins mediate regulatory processes for over 800 different G protein-coupled receptors (GPCRs) by adopting specific conformations that result...
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β-Arrestin inhibition induces autophagy, apoptosis, G0/G1 cell cycle arrest in agonist-activated V2R receptor in breast cancer cells
Non-visual arrestins (β-arrestins) are endocytic proteins that mediate agonist-activated GPCRs internalization and signaling pathways in an...
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Chemoproteomics reveals microbiota-derived aromatic monoamine agonists for GPRC5A
The microbiota generates diverse metabolites to modulate host physiology and disease, but their protein targets and mechanisms of action have not...
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Structural and dynamic insights into supra-physiological activation and allosteric modulation of a muscarinic acetylcholine receptor
The M2 muscarinic receptor (M2R) is a prototypical G-protein-coupled receptor (GPCR) that serves as a model system for understanding GPCR regulation...
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RETRACTED ARTICLE: β adrenergic receptor modulated signaling in glioma models: promoting β adrenergic receptor-β arrestin scaffold-mediated activation of extracellular-regulated kinase 1/2 may prove to be a panacea in the treatment of intracranial and spinal malignancy and extra-neuraxial carcinoma
Neoplastically transformed astrocytes express functionally active cell surface β adrenergic receptors (βARs). Treatment of glioma models in vitro and...
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Biased signaling due to oligomerization of the G protein-coupled platelet-activating factor receptor
G protein-coupled receptors (GPCRs) are important drug targets that mediate various signaling pathways by activating G proteins and engaging...
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Structure of an endosomal signaling GPCR–G protein–β-arrestin megacomplex
Classically, G-protein-coupled receptors (GPCRs) are thought to activate G protein from the plasma membrane and are subsequently desensitized by...
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Nanomolar range of FAM237B can activate receptor GPR83
Our recent study confirmed that the mature neuropeptide FAM237A, also known as neurosecretory protein GL (NPGL), is an efficient agonist for GPR83....
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The Influence of β-Arrestin-2 Gene Knockout in Mice on Survival of Cultured Astrocytes Exposed to Thrombin and on the Cerebral Thrombosis Aftereffects In Vivo
Abstract —Thrombin is a multifunctional serine protease that attracts the attention of many researchers in particular in connection with a wide range...
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Ligand efficacy modulates conformational dynamics of the µ-opioid receptor
The µ-opioid receptor (µOR) is an important target for pain management
1 and molecular understanding of drug action on µOR will facilitate the...
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St. John's wort extract Ze 117 alters the membrane fluidity of C6 glioma cells by influencing cellular cholesterol metabolism
Chronic stress is associated with major depressive disorder (MDD). Increased glucocorticoid levels caused by uncontrolled release through the...
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Proinflammatory chemokine CXCL14 activates MAS-related G protein-coupled receptor MRGPRX2 and its putative mouse ortholog MRGPRB2
Patients with idiopathic pulmonary fibrosis show a strongly upregulated expression of chemokine CXCL14, whose target is still unknown. Screening of...
