ArticleThe EMBO journal2001
X-ray structure of the orphan nuclear receptor RORbeta ligand-binding domain in the active conformation.
Article in The EMBO journal, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 49 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
49 citing papers in PubMed, 121 citations in OpenAlex.
- Discovery of natural RORγt inhibitor using machine learning, virtual screening, and in vivo validation.Journal of advanced research · 2026Article
- A Complex Interplay Between Melatonin and RORβ: RORβ is Unlikely a Putative Receptor for Melatonin as Revealed by Biophysical Assays.Molecular neurobiology · 2025Article
- Review
- InsPection of electron density maps supports wrongly modeled hexakisphosphate (InsP6) bound to African swine fever mRNA-decapping enzyme g5Rp.Journal of virology · 2024Article
- Case Report: A 3' splice site variation inFrontiers in genetics · 2024Article
- International Union of Basic and Clinical Pharmacology CXIII: Nuclear Receptor Superfamily-Update 2023.Pharmacological reviews · 2023Review
- Identification of the Natural Steroid Sapogenin Diosgenin as a Direct Dual-Specific RORα/γ Inverse Agonist.Biomedicines · 2022Article
- Structural overview and perspectives of the nuclear receptors, a major family as the direct targets for small-molecule drugs.Acta biochimica et biophysica Sinica · 2022Article
- Recent advances in modulators of circadian rhythms: an update and perspective.Journal of enzyme inhibition and medicinal chemistry · 2020Review
- A maresin 1/RORα/12-lipoxygenase autoregulatory circuit prevents inflammation and progression of nonalcoholic steatohepatitis.The Journal of clinical investigation · 2019Article
- Ternary crystal structure of human RORγ ligand-binding-domain, an inhibitor and corepressor peptide provides a new insight into corepressor interaction.Scientific reports · 2018Article
- Identification of potent RORβ modulators: Scaffold variation.Bioorganic & medicinal chemistry letters · 2018Article
- Identification of an aminothiazole series of RORβ modulators.Bioorganic & medicinal chemistry letters · 2018Article
- Osteoprotection Through the Deletion of the Transcription Factor Rorβ in Mice.Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research · 2018Article
- Development and Therapeutic Potential of Small-Molecule Modulators of Circadian Systems.Annual review of pharmacology and toxicology · 2018Review
- The obesity-related pathology and Th17 cells.Cellular and molecular life sciences : CMLS · 2017Review
- The Small Molecule Nobiletin Targets the Molecular Oscillator to Enhance Circadian Rhythms and Protect against Metabolic Syndrome.Cell metabolism · 2016Article
- Identification of an allosteric binding site for RORγt inhibition.Nature communications · 2015Article
- Identification of natural RORγ ligands that regulate the development of lymphoid cells.Cell metabolism · 2015Article
- ROR nuclear receptors: structures, related diseases, and drug discovery.Acta pharmacologica Sinica · 2015Review
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The retinoic acid-related orphan receptor beta (RORbeta) exhibits a highly restricted neuronal-specific expression pattern in brain, retina and pineal gland. So far, neither a natural RORbeta target gene nor a functional ligand have been identified, and the physiological role of the receptor is not well understood. We present the crystal structure of the ligand-binding domain (LBD) of RORbeta containing a bound stearate ligand and complexed with a coactivator peptide. In the crystal, the monomeric LBD adopts the canonical agonist-bound form. The fatty acid ligand-coactivator peptide combined action stabilizes the transcriptionally active conformation. The large ligand-binding pocket is strictly hydrophobic on the AF-2 side and more polar on the beta-sheet side where the carboxylate group of the ligand binds. Site-directed mutagenesis experiments validate the significance of the present structure. Homology modeling of the other isotypes will help to design isotype-selective agonists and antagonists that can be used to characterize the physiological functions of RORs. In addition, our crystallization strategy can be extended to other orphan nuclear receptors, providing a powerful tool to delineate their functions.
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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.