ArticleThe Journal of biological chemistry2011
G protein activation by serotonin type 4 receptor dimers: evidence that turning on two protomers is more efficient.
Article in The Journal of biological chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers, 1 of them a synthesis that pooled it.
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Who cites it
39 citing papers in PubMed, 1 synthesis or guideline pooled it, 74 citations in OpenAlex.
- The C825T Polymorphism of the G-Protein β3 Gene as a Risk Factor for Depression: A Meta-Analysis.PloS one · 2015Pooled it
- amyloid-predict and LLPS-predict: Predicting phase separation propensities in the intrinsically disordered proteome.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- The Benzoylpiperidine Fragment as a Privileged Structure in Medicinal Chemistry: A Comprehensive Review.Molecules (Basel, Switzerland) · 2024Review
- Functional Dimerization of Serotonin Receptors: Role in Health and Depressive Disorders.International journal of molecular sciences · 2023Review
- Evolutionary Couplings and Molecular Dynamic Simulations Highlight Details of GPCRs Heterodimers' Interfaces.Molecules (Basel, Switzerland) · 2023Article
- Biased signaling due to oligomerization of the G protein-coupled platelet-activating factor receptor.Nature communications · 2022Article
- Class A and C GPCR Dimers in Neurodegenerative Diseases.Current neuropharmacology · 2022Review
- G-protein signaling is required for increasing germline stem cell division frequency in response to mating in Drosophila males.Scientific reports · 2020Article
- Cryo-EM structure of the native rhodopsin dimer in nanodiscs.The Journal of biological chemistry · 2019Article
- Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors.Journal of medicinal chemistry · 2019Article
- Dynamic tuneable G protein-coupled receptor monomer-dimer populations.Nature communications · 2018Article
- Evidence for functional pre-coupled complexes of receptor heteromers and adenylyl cyclase.Nature communications · 2018Article
- Synthesis and Structure-Activity Relationships of Tool Compounds Based on WAY163909, a 5-HTACS chemical neuroscience · 2017Article
- Heterodimers of serotonin receptor subtypes 2 are driven by 5-HTThe Journal of biological chemistry · 2017Article
- Multivalent ligands for the serotonin 5-HTMedChemComm · 2017Article
- Phosphorylation of β-arrestin2 at ThreLife · 2017Article
- The Serotonin Receptor Subtype 5b Specifically Interacts with Serotonin Receptor Subtype 1A.Frontiers in molecular neuroscience · 2017Article
- Homodimerization enhances both sensitivity and dynamic range of the ligand-binding domain of type 1 metabotropic glutamate receptor.FEBS letters · 2016Article
- Native serotonin 5-HT2C receptors are expressed as homodimers on the apical surface of choroid plexus epithelial cells.Molecular pharmacology · 2015Article
- Ghrelin receptor conformational dynamics regulate the transition from a preassembled to an active receptor:Gq complex.Proceedings of the National Academy of Sciences of the United States of America · 2015Article
Corrections and comments
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Authors and funding
11 authors at 5 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The discovery that class C G protein-coupled receptors (GPCRs) function as obligatory dimeric entities has generated major interest in GPCR oligomerization. Oligomerization now appears to be a common feature among all GPCR classes. However, the functional significance of this process remains unclear because, in vitro, some monomeric GPCRs, such as rhodopsin and β(2)-adrenergic receptors, activate G proteins. By using wild type and mutant serotonin type 4 receptors (5-HT(4)Rs) (including a 5-HT(4)-RASSL) expressed in COS-7 cells as models of class A GPCRs, we show that activation of one protomer in a dimer was sufficient to stimulate G proteins. However, coupling efficiency was 2 times higher when both protomers were activated. Expression of combinations of 5-HT(4), in which both protomers were able to bind to agonists but only one could couple to G proteins, suggested that upon agonist occupancy, protomers did not independently couple to G proteins but rather that only one G protein was activated. Coupling of a single heterotrimeric G(s) protein to a receptor dimer was further confirmed in vitro, using the purified recombinant WT RASSL 5-HT(4)R obligatory heterodimer. These results, together with previous findings, demonstrate that, differently from class C GPCR dimers, class A GPCR dimers have pleiotropic activation mechanisms.
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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.