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β-Arrestin-independent endosomal cAMP signaling by a polypeptide hormone GPCR
Many G protein-coupled receptors (GPCRs) initiate a second phase of stimulatory heterotrimeric G protein (G s )-coupled cAMP signaling after...
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Characterization of genetic variants of GIPR reveals a contribution of β-arrestin to metabolic phenotypes
Incretin-based therapies are highly successful in combatting obesity and type 2 diabetes
1 . Yet both activation and inhibition of the...
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Computational insights into ligand–induced G protein and β-arrestin signaling of the dopamine D1 receptor
The dopamine D1 receptor (D1R), is a class A G protein coupled-receptor (GPCR) which has been a promising drug target for psychiatric and...
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MiR-150 blunts cardiac dysfunction in mice with cardiomyocyte loss of β1-adrenergic receptor/β-arrestin signaling and controls a unique transcriptome
The β 1 -adrenergic receptor (β 1 AR) is found primarily in hearts (mainly in cardiomyocytes [CMs]) and β-arrestin-mediated β 1 AR signaling elicits...
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Noradrenergic consolidation of social recognition memory is mediated by β-arrestin–biased signaling in the mouse prefrontal cortex
Social recognition memory (SRM) is critical for maintaining social relationships and increasing the survival rate. The medial prefrontal cortex...
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Stabilization of pre-existing neurotensin receptor conformational states by β-arrestin-1 and the biased allosteric modulator ML314
The neurotensin receptor 1 (NTS 1 ) is a G protein-coupled receptor (GPCR) with promise as a drug target for the treatment of pain, schizophrenia,...
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The Effects of Piracetam and Noopept on NMDA- and 5-HT2A-Receptors in the Brains of Mice with Congenital β-Arrestin Deficiency
Abstract —Based on the special role of the β-arrestin signal protein in the processes of neuronal plasticity and receptor activation, the effects of...
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Cellular Assay to Study β-Arrestin Recruitment by the Cannabinoid Receptors 1 and 2
Cannabinoid receptor 1 (CB1R) and cannabinoid receptor 2 (CB2R) are G protein-coupled receptors (GPCRs) that activate a variety of pathways upon...
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Platelet P2Y1 receptor exhibits constitutive G protein signaling and β-arrestin 2 recruitment
BackgroundPurinergic P2Y 1 and P2Y 12 receptors (P2Y 1 -R and P2Y 12 -R) are G protein-coupled receptors (GPCR) activated by adenosine diphosphate (ADP)...
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Islet MC4R Regulates PC1/3 to Improve Insulin Secretion in T2DM Mice via the cAMP and β-arrestin-1 Pathways
Melanocortin-4 receptor (MC4R) plays an important role in energy balance regulation and insulin secretion. It has been demonstrated that in the...
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A novel β2-AR agonist, Higenamine, induces β-arrestin-biased signaling
The biased ligands in G protein-coupled receptors (GPCRs) have opened new avenues for develo** safer and more effective drugs. However, the...
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Systematic assessment of chemokine ligand bias at the human chemokine receptor CXCR2 indicates G protein bias over β-arrestin recruitment and receptor internalization
BackgroundThe human CXC chemokine receptor 2 (CXCR2) is a G protein-coupled receptor (GPCR) interacting with multiple chemokines ( i.e. , CXC...
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Functionality of Melatonin Receptors: Recruitment of β-Arrestin at MT1
The main process of downregulation of G protein-coupled receptors is desensitization by which the receptor is extruded from the plasma membrane and...
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Heterotrimeric Gq proteins act as a switch for GRK5/6 selectivity underlying β-arrestin transducer bias
Signaling-biased ligands acting on G-protein-coupled receptors (GPCRs) differentially activate heterotrimeric G proteins and β-arrestins. Although a...
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LSD-stimulated behaviors in mice require β-arrestin 2 but not β-arrestin 1
Recent evidence suggests that psychedelic drugs can exert beneficial effects on anxiety, depression, and ethanol and nicotine abuse in humans....
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β‐arrestin 2 negatively regulates lung cancer progression by inhibiting the TRAF6 signaling axis for NF-κB activation and autophagy induced by TLR3 and TLR4
β‐arrestin 2 (ARRB2) is functionally implicated in cancer progression via various signaling pathways. However, its role in lung cancer remains...
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Agonist dependency of the second phase access of β-arrestin 2 to the heteromeric µ-V1b receptor
During the development of analgesic tolerance to morphine, the V1b vasopressin receptor has been proposed to bind to β-arrestin 2 and the µ-opioid...
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Design and discovery of a high affinity, selective and β-arrestin biased 5-HT7 receptor agonist
Compound 1c , 5-chloro-2-(2-(3,4-dihydroisoquinolin-2(1H)-yl)ethyl)-2,3-dihydro-1H-inden-1-one was previously reported from our laboratory showing...
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Atypical chemokine receptor 3 induces colorectal tumorigenesis in mice by promoting β-arrestin-NOLC1-fibrillarin-dependent rRNA biogenesis
Atypical chemokine receptor 3 (ACKR3) has emerged as a key player in various biological processes. Its atypical “intercepting receptor” properties...
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Novel interaction between neurotrophic factor-α1/carboxypeptidase E and serotonin receptor, 5-HTR1E, protects human neurons against oxidative/neuroexcitotoxic stress via β-arrestin/ERK signaling
Protecting neurons from death during oxidative and neuroexcitotoxic stress is key for preventing cognitive dysfunction. We uncovered a novel...
