ArticleNature communications2020
Structure of the human gonadotropin-releasing hormone receptor GnRH1R reveals an unusual ligand binding mode.
Article in Nature communications, 2020. 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, 52 citations in OpenAlex.
- Article
- Development of a novel NanoBRET high-throughput drug screening assay for human GnRH receptor using sulfo-cyanine 5 fluorophore.Journal of pharmaceutical analysis · 2026Article
- Differential hypothalamic regulation of FSH and LH secretion from the fish pituitary by GnRH and CCK.Reproduction (Cambridge, England) · 2025Article
- Computational modelling reveals novel insights into GnRH receptor activation and binding dynamics.Scientific reports · 2025Article
- Protective Effects ofFood science & nutrition · 2025Article
- Cryo-EM structures of GnRHR: Foundations for next-generation therapeutics.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Identification of Environmental Compounds That May Trigger Early Female Puberty by Activating Human GnRHR and KISS1R.Endocrinology · 2024Article
- Article
- Review
- G Protein-Coupled Receptor-Ligand Pose and Functional Class Prediction.International journal of molecular sciences · 2024Article
- G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery.Signal transduction and targeted therapy · 2024Review
- Glu102Biochemistry · 2024Article
- Peptide-Drug Conjugates: Design, Chemistry, and Drug Delivery System as a Novel Cancer Theranostic.ACS pharmacology & translational science · 2024Review
- Enhancement of Female Rat Fertility via Ethanolic Extract fromMolecules (Basel, Switzerland) · 2024Article
- Computational drug repurposing effort for identifying novel hits for the treatment of diseases such as endometriosis, uterine fibroids, and prostate cancer.Turkish journal of chemistry · 2024Article
- Rational Design, Synthesis and Binding Affinity Studies of Anthraquinone Derivatives Conjugated to Gonadotropin-Releasing Hormone (GnRH) Analogues towards Selective Immunosuppression of Hormone-Dependent Cancer.International journal of molecular sciences · 2023Article
- GNRH family genes contributed to gender-specific disparity of bladder cancer prognosis through exerting opposite regulatory roles between males and females.Journal of cancer research and clinical oncology · 2023Article
- Elagolix Sodium Salt and Its Synthetic Intermediates: A Spectroscopic, Crystallographic, and Conformational Study.Molecules (Basel, Switzerland) · 2023Article
- Improving the Modeling of Extracellular Ligand Binding Pockets in RosettaGPCR for Conformational Selection.International journal of molecular sciences · 2023Article
- Structural basis for recognition of antihistamine drug by human histamine receptor.Nature communications · 2022Article
Corrections and comments
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Authors and funding
12 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Gonadotrophin-releasing hormone (GnRH), also known as luteinizing hormone-releasing hormone, is the main regulator of the reproductive system, acting on gonadotropic cells by binding to the GnRH1 receptor (GnRH1R). The GnRH-GnRH1R system is a promising therapeutic target for maintaining reproductive function; to date, a number of ligands targeting GnRH1R for disease treatment are available on the market. Here, we report the crystal structure of GnRH1R bound to the small-molecule drug elagolix at 2.8 Å resolution. The structure reveals an interesting N-terminus that could co-occupy the enlarged orthosteric binding site together with elagolix. The unusual ligand binding mode was further investigated by structural analyses, functional assays and molecular docking studies. On the other hand, because of the unique characteristic of lacking a cytoplasmic C-terminal helix, GnRH1R exhibits different microswitch structural features from other class A GPCRs. In summary, this study provides insight into the ligand binding mode of GnRH1R and offers an atomic framework for rational drug design.
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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.