ArticleCommunications biology2018
Conformational signatures in β-arrestin2 reveal natural biased agonism at a G-protein-coupled receptor.
Article in Communications biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
What it found
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The trial behind it
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Who cites it
32 citing papers in PubMed, 59 citations in OpenAlex.
- Galanin Receptors: G Protein-Dependent Signaling and Beyond.Biomolecules · 2026Review
- A novel long-galanin peptide from non-mammalian vertebrates mitigates the inflammatory response in IBD models via the biased GALR2/β-arrestin2 pathway.Nature communications · 2025Article
- Inhibition of constitutive activity of the atypical chemokine receptor 3 by the small-molecule inverse agonist VUF16840.Molecular pharmacology · 2025Article
- Is FAM19A5 an adipokine? Peripheral FAM19A5 in wild-type, FAM19A5 knockout, and LacZ knockin mice.Molecules and cells · 2024Article
- Multiplex Detection of Fluorescent Chemokine Binding to CXC Chemokine Receptors by NanoBRET.International journal of molecular sciences · 2024Article
- Exploring the Potential Link between Acute Central Serous Chorioretinopathy and Trimethylamine N-Oxide, Phoenixin, Spexin, and Alarin Molecules.Biomolecules · 2023Article
- Structural snapshots uncover a key phosphorylation motif in GPCRs driving β-arrestin activation.Molecular cell · 2023Article
- β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the same GPCR in living cells.Nature communications · 2022Article
- Finding the Perfect Fit: Conformational Biosensors to Determine the Efficacy of GPCR Ligands.ACS pharmacology & translational science · 2022Review
- The Neuropeptide Spexin Promotes the Osteoblast Differentiation of MC3T3-E1 Cells via the MEK/ERK Pathway and Bone Regeneration in a Mouse Calvarial Defect Model.Tissue engineering and regenerative medicine · 2022Article
- Characterization of the chicken melanocortin 5 receptor and its potential role in regulating hepatic glucolipid metabolism.Frontiers in physiology · 2022Article
- Article
- The Association of Serum Circulating Neuropeptide Q and Chemerin Levels with Cardiometabolic Risk Factors among Patients with Metabolic Syndrome.Biomolecules · 2021Article
- Novel insights on the role of spexin as a biomarker of obesity and related cardiometabolic disease.International journal of obesity (2005) · 2021Review
- Dopamine regulates pancreatic glucagon and insulin secretion via adrenergic and dopaminergic receptors.Translational psychiatry · 2021Article
- Functions of galanin, spexin and kisspeptin in metabolism, mood and behaviour.Nature reviews. Endocrinology · 2021Review
- NanoLuc-Based Methods to Measure β-Arrestin2 Recruitment to G Protein-Coupled Receptors.Methods in molecular biology (Clifton, N.J.) · 2021Article
- Mouse Spexin: (III) Differential Regulation by Glucose and Insulin in Glandular Stomach and Functional Implication in Feeding Control.Frontiers in endocrinology · 2021Article
- Luciferase Complementation Approaches to Measure GPCR Signaling Kinetics and Bias.Methods in molecular biology (Clifton, N.J.) · 2021Article
- Mouse Spexin: (II) Functional Role as a Satiety Factor inhibiting Food Intake by Regulatory Actions Within the Hypothalamus.Frontiers in endocrinology · 2021Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Discovery of biased ligands and receptor mutants allows characterization of G-protein- and β-arrestin-mediated signaling mechanisms of G-protein-coupled receptors (GPCRs). However, the structural mechanisms underlying biased agonism remain unclear for many GPCRs. We show that while Galanin induces the activation of the galanin receptor 2 (Galr2) that leads to a robust stimulation toward Gαq-protein and β-arrestin1/2, an alternative ligand Spexin and its analog have biased agonism toward G-protein signaling relative to Galanin. We used intramolecular fluorescein arsenical hairpin bioluminescence resonance energy transfer-based biosensors of β-arrestin2 combined with NanoBit technology to measure β-arrestin2-Galr2 interactions in real-time living systems. We found that Spexin and Galanin induce specific active conformations of Galr2, which may lead to different internalization rates of the receptor as well as different signaling outputs. This work represents an additional pharmacological evidence of endogenous G-protein-biased agonism at a GPCR.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.