ArticleNature communications2023
An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism.
Article in Nature communications, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 32 citations in OpenAlex.
- Ethanolamine plasmalogens increase luteinising hormone pulsatility and are associated with GPR61 expression in bovine gonadotrophin-releasing hormone neurons.Journal of neuroendocrinology · 2026Article
- Protein Engineering-Enabled Cryo-EM Investigation of Small GTPases.Journal of molecular biology · 2026Article
- A Sulfonamide Intermediate Elicits Therapeutic Effect Against Sepsis by Enhancing Neutrophil Maturation.Journal of cellular and molecular medicine · 2026Article
- Article
- Twist-encoded magnetic plasmon interferometry for label-free, orientation-resolved single-molecule imaging.Science advances · 2026Article
- International Union of Basic and Clinical Pharmacology. CXXII. Applying an objective evaluation to the status of class A orphan G protein-coupled receptors.Pharmacological reviews · 2026Review
- Structure of the melatonin-related orphan receptor, GPR50.Molecules and cells · 2026Article
- Intracellular and dual-site inhibition of a bitter taste GPCR.Cellular and molecular life sciences : CMLS · 2026Article
- Constitutive activity among orphan G protein-coupled receptors: Molecular mechanisms and pharmacological perspectives.Molecular pharmacology · 2026Review
- Designing Rigid Protein Fiducials to Visualize GPCR Conformational States.bioRxiv : the preprint server for biology · 2026Article
- Structural insights into nonpeptide antagonist inhibition of somatostatin receptor subtype 5.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Structural insights into selective and dual antagonism of EP2 and EP4 prostaglandin receptors.The EMBO journal · 2025Article
- Article
- Constitutively active orphan G protein-coupled receptors through the lenses of cryo-electron microscopy.The Journal of biological chemistry · 2025Review
- Effects of chemosynthetic choline plasmalogens on gonadotropin secretion from bovine gonadotrophs.The Journal of reproduction and development · 2025Article
- Identification and molecular characterization of missense mutations in orphan G protein-coupled receptor GPR61 occurring in severe obesity.Molecular pharmacology · 2025Article
- An integrative approach prioritizes the orphan GPR61 genomic region in tissue-specific regulation of chronotype.Sleep advances : a journal of the Sleep Research Society · 2025Article
- A fiducial-assisted strategy compatible with resolving small MFS transporter structures in multiple conformations using cryo-EM.Nature communications · 2025Article
- A bitter anti-inflammatory drug binds at two distinct sites of a human bitter taste GPCR.Nature communications · 2024Article
- Structural perspectives on chemokine receptors.Biochemical Society transactions · 2024Review
Corrections and comments
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Authors and funding
23 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
GPR61 is an orphan GPCR related to biogenic amine receptors. Its association with phenotypes relating to appetite makes it of interest as a druggable target to treat disorders of metabolism and body weight, such as obesity and cachexia. To date, the lack of structural information or a known biological ligand or tool compound has hindered comprehensive efforts to study GPR61 structure and function. Here, we report a structural characterization of GPR61, in both its active-like complex with heterotrimeric G protein and in its inactive state. Moreover, we report the discovery of a potent and selective small-molecule inverse agonist against GPR61 and structural elucidation of its allosteric binding site and mode of action. These findings offer mechanistic insights into an orphan GPCR while providing both a structural framework and tool compound to support further studies of GPR61 function and modulation.
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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.