ArticleThe Journal of biological chemistry2013
Heterodimerization with Its splice variant blocks the ghrelin receptor 1a in a non-signaling conformation: a study with a purified heterodimer assembled into lipid discs.
Article in The Journal of biological chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 53 citations in OpenAlex.
- Midbrain ghrelin receptor signalling regulates binge drinking in a sex specific manner.Nature communications · 2025Article
- Role and molecular mechanism of ghrelin in degenerative musculoskeletal disorders.Journal of cellular and molecular medicine · 2023Review
- Ghrelin receptor signaling in health and disease: a biased view.Trends in endocrinology and metabolism: TEM · 2023Review
- Toward a consensus nomenclature for ghrelin, its non-acylated form, liver expressed antimicrobial peptide 2 and growth hormone secretagogue receptor.Journal of neuroendocrinology · 2023Review
- Discovery of a functionally selective ghrelin receptor (GHSRProceedings of the National Academy of Sciences of the United States of America · 2022Article
- G protein-coupled receptor-effector macromolecular membrane assemblies (GEMMAs).Pharmacology & therapeutics · 2022Review
- Complexes of Ghrelin GHS-R1a, GHS-R1b, and Dopamine DThe Journal of neuroscience : the official journal of the Society for Neuroscience · 2022Article
- Differential Influence ofPharmaceuticals (Basel, Switzerland) · 2021Article
- The emerging role of heterodimerisation and interacting proteins in ghrelin receptor function.The Journal of endocrinology · 2021Review
- Ghrelin octanoylation by ghrelinOpen biology · 2021Review
- Cocaine Blocks Effects of Hunger Hormone, Ghrelin, Via Interaction with Neuronal Sigma-1 Receptors.Molecular neurobiology · 2019Article
- Clarifying the Ghrelin System's Ability to Regulate Feeding Behaviours Despite Enigmatic Spatial Separation of the GHSR and Its Endogenous Ligand.International journal of molecular sciences · 2017Review
- Hormones and Neuropeptide Receptor Heteromers in the Ventral Tegmental Area. Targets for the Treatment of Loss of Control of Food Intake and Substance Use Disorders.Current treatment options in psychiatry · 2017Review
- Novel nuclear hENT2 isoforms regulate cell cycle progression via controlling nucleoside transport and nuclear reservoir.Cellular and molecular life sciences : CMLS · 2016Article
- A Significant Role of the Truncated Ghrelin Receptor GHS-R1b in Ghrelin-induced Signaling in Neurons.The Journal of biological chemistry · 2016Article
- Article
- 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
- Article
- Amphipols in G protein-coupled receptor pharmacology: what are they good for?The Journal of membrane biology · 2014Review
- Ghrelin: ghrelin as a regulatory Peptide in growth hormone secretion.Journal of clinical and diagnostic research : JCDR · 2014Review
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Heterodimerization of G protein-coupled receptors has an impact on their signaling properties, but the molecular mechanisms underlying heteromer-directed selectivity remain elusive. Using purified monomers and dimers reconstituted into lipid discs, we explored how dimerization impacts the functional and structural behavior of the ghrelin receptor. In particular, we investigated how a naturally occurring truncated splice variant of the ghrelin receptor exerts a dominant negative effect on ghrelin signaling upon dimerization with the full-length receptor. We provide direct evidence that this dominant negative effect is due to the ability of the non-signaling truncated receptor to restrict the conformational landscape of the full-length protein. Indeed, associating both proteins within the same disc blocks all agonist- and signaling protein-induced changes in ghrelin receptor conformation, thus preventing it from activating its cognate G protein and triggering arrestin 2 recruitment. This is an unambiguous demonstration that allosteric conformational events within dimeric assemblies can be directly responsible for modulation of signaling mediated by G protein-coupled receptors.
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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.