ROR nuclear receptors: Structures, related diseases, and drug discovery
Open accessAbstract
Nuclear receptors (NRs) are ligand-regulated transcription factors that regulate metabolism, development and immunity. The NR superfamily is one of the major classes of drug targets for human diseases. Retinoic acid receptor-related orphan receptor (ROR) α, β and γ belong to the NR superfamily, and these receptors are still considered as 'orphan' receptors because the identification of their endogenous ligands has been controversial. Recent studies have demonstrated that these receptors are regulated by synthetic ligands, thus emerge as important drug targets for the treatment of multiple sclerosis, rheumatoid arthritis, psoriasis, etc. Studying the structural basis and ligand development of RORs will pave the way for a better understanding of the roles of these receptors in human diseases. Here, we review the structural basis, disease relevance, strategies for ligand identification, and current status of development of therapeutic ligands for RORs.
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The ROR family has three tissue-specific isoforms: RORalpha is mainly in liver and brain, RORbeta in retina and brain, and RORgamma in liver and testes.
“Therefore, RORα is mainly found in the liver and the brain, β in the retina and the brain, and γ in the liver and the testes, among other tissues [163].”
From Vitamin A Update: Forms, Sources, Kinetics, Detection, Function, Deficiency, Therapeutic Use and Toxicity (2021) · cites this paper as [163]
The “RORs and ROR-related diseases” section lists every tissue named in the citing sentence and says the three receptors have distinct expression patterns. It describes RORα as widely expressed across eight tissues and RORγ as highly expressed across seven, however, so it does not establish that the two named tissues are the main sites for either receptor. The source also calls α, β, and γ members of the ROR subfamily, not three isoforms. Page numbers were not provided for the passage. (LLM, conf=0.88)
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Jin, L., Lin, S., Rong, H., Zheng, S., Jin, S., Wang, R., & Li, Y. (2011) · Journal of Biological Chemistry · doi:10.1074/jbc.m111.266023 · Cited by 28 · see citing works
Identification of tertiary sulfonamides as RORc inverse agonists
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Flagged first, then by citations
Research works printed but not linked: 1
- Blumberg B, Evans RM. Orphan nuclear receptors -new ligands and new possibilities. Genes Dev 1998; 12: 3149-55.
Cited by
Sorted by citations
Carazo, A., Macáková, K., Matoušová, K., Krčmová, L. K., Protti, M., & Mladěnka, P. (2021) · Nutrients · doi:10.3390/nu13051703 · Cited by 418 · see citing works
Target identification among known drugs by deep learning from heterogeneous networks
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- Authors
- Zhang, Y., Luo, X.-Y., Wu, D.-H., & Xu, Y.
- Affiliations
- Chinese Academy of Sciences (CN)
- Corresponding author
- Xu, Yong
- ORCID
- Venue
- Acta Pharmacologica Sinica
- Published
- 2014-12-15
- Volume
- 36
- Issue
- 1
- Pages
- 71-87
- ISSN
- 0253-9756 (ISSN-L)
- 1671-4083
- 1745-7254
- PMC
- PMC4571318
- OpenAlex
- W1971126801
- Cited by
- 151
- References
- 97
- Citations by year
- 2026: 19 · 2025: 12 · 2024: 13 · 2023: 18 · 2022: 10 · 2021: 15 · 2020: 11 · 2019: 17 · 2018: 12 · 2017: 11 · 2016: 10 · 2015: 3
- FWCI
- 0.99
- Type
- journal article
- Language
- en
- Update notices
- correction (2015-02-03)
- Open access
- bronze
- doi.org
- Locations
- Acta Pharmacologica Sinica (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Natural Science Foundation of China (973 Program, 81373325)
- National Key Research and Development Program of China
- Topics
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Nuclear Receptors and Signaling
- Life Sciences › Immunology and Microbiology › Immunology › Psoriasis: Treatment and Pathogenesis
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Retinoids in leukemia and cellular processes
- Keywords
- RORα, RORβ, RORγ, orphan receptors, synthetic ligands, endogenous ligands, ligand identification, receptor structure, multiple sclerosis, rheumatoid arthritis, psoriasis, drug discovery
- MeSH terms
- Animals, Humans, Ligands, Drug Discovery, Orphan Nuclear Receptors
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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