ArticleThe EMBO journal2010
Molecular organization and dynamics of the melatonin MT₁ receptor/RGS20/G(i) protein complex reveal asymmetry of receptor dimers for RGS and G(i) coupling.
Article in The EMBO journal, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 65 citations in OpenAlex.
- Phylogenetic and Structural Insights into Melatonin Receptors in Plants: Case Study inPlants (Basel, Switzerland) · 2025Article
- Orphan GPR50 Restrains Neurite Outgrowth and Cell Migration by Activating the GJournal of pineal research · 2025Article
- The genomic response of human granulosa cells (KGN) to melatonin and specific agonists/antagonists to the melatonin receptors.Scientific reports · 2022Article
- Article
- Melatonin decreases androgen-sensitive prostate cancer growth by suppressing SENP1 expression.Translational andrology and urology · 2022Article
- Class A and C GPCR Dimers in Neurodegenerative Diseases.Current neuropharmacology · 2022Review
- Structure of the class C orphan GPCR GPR158 in complex with RGS7-Gβ5.Nature communications · 2021Article
- Negative regulation of melatonin secretion by melatonin receptors in ovine pinealocytes.PloS one · 2021Article
- Regulators of G-protein signaling, RGS2 and RGS4, inhibit protease-activated receptor 4-mediated signaling by forming a complex with the receptor and Gα in live cells.Cell communication and signaling : CCS · 2020Article
- Characterization of the various functional pathways elicited by synthetic agonists or antagonists at the melatonin MTPharmacology research & perspectives · 2020Article
- Melatonin in type 2 diabetes mellitus and obesity.Nature reviews. Endocrinology · 2019Review
- Melatonin receptors: molecular pharmacology and signalling in the context of system bias.British journal of pharmacology · 2018Review
- Importance of the second extracellular loop for melatonin MTBritish journal of pharmacology · 2018Article
- The orphan GPR50 receptor promotes constitutive TGFβ receptor signaling and protects against cancer development.Nature communications · 2018Article
- Systematic protein-protein interaction mapping for clinically relevant human GPCRs.Molecular systems biology · 2017Article
- Article
- Valproic Acid Influences MTNR1A Intracellular Trafficking and Signaling in a β-Arrestin 2-Dependent Manner.Molecular neurobiology · 2016Article
- Understanding melatonin receptor pharmacology: latest insights from mouse models, and their relevance to human disease.BioEssays : news and reviews in molecular, cellular and developmental biology · 2014Review
- G protein-coupled receptor oligomerization revisited: functional and pharmacological perspectives.Pharmacological reviews · 2014Review
- Melatonin receptor genes in vertebrates.International journal of molecular sciences · 2013Review
Corrections and comments
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Authors and funding
12 authors at 7 institutions in 3 countries.
Funding
Abstract
Functional asymmetry of G-protein-coupled receptor (GPCR) dimers has been reported for an increasing number of cases, but the molecular architecture of signalling units associated to these dimers remains unclear. Here, we characterized the molecular complex of the melatonin MT₁ receptor, which directly and constitutively couples to G(i) proteins and the regulator of G-protein signalling (RGS) 20. The molecular organization of the ternary MT₁/G(i)/RGS20 complex was monitored in its basal and activated state by bioluminescence resonance energy transfer between probes inserted at multiple sites of the complex. On the basis of the reported crystal structures of G(i) and the RGS domain, we propose a model wherein one G(i) and one RGS20 protein bind to separate protomers of MT₁ dimers in a pre-associated complex that rearranges upon agonist activation. This model was further validated with MT₁/MT₂ heterodimers. Collectively, our data extend the concept of asymmetry within GPCR dimers, reinforce the notion of receptor specificity for RGS proteins and highlight the advantage of GPCRs organized as dimers in which each protomer fulfils its specific task by binding to different GPCR-interacting proteins.
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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.