ArticleFASEB journal : official publication of the Federation of American Societies for Experimental Biology2016
Dissociated sterol-based liver X receptor agonists as therapeutics for chronic inflammatory diseases.
Article in FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 28 citations in OpenAlex.
- Liver X receptor: A potential target for inflammatory bowel disease and colorectal cancer (Review).Molecular medicine reports · 2026Review
- Isolinderalactone regulates macrophage polarization and efferocytosis by activating the LXRα pathway against ulcerative colitis.Chinese medicine · 2025Article
- Targeting ABCG1 and SREBP-2 mediated cholesterol homeostasis ameliorates Zika virus-induced ocular pathology.iScience · 2024Article
- International Union of Basic and Clinical Pharmacology CXIII: Nuclear Receptor Superfamily-Update 2023.Pharmacological reviews · 2023Review
- Neurosteroid Receptor Modulators for Treating Traumatic Brain Injury.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2023Review
- Loss of ERβ in Aging LXRαβ Knockout Mice Leads to Colitis.International journal of molecular sciences · 2023Article
- Progress toward the De Novo Asymmetric Synthesis of Euphanes.Organic letters · 2022Article
- Microglia and Neuroinflammation: Crucial Pathological Mechanisms in Traumatic Brain Injury-Induced Neurodegeneration.Frontiers in aging neuroscience · 2022Review
- The liver X receptor agonist LXR 623 restricts flavivirus replication.Emerging microbes & infections · 2021Article
- Disrupted Lipid Metabolism in Multiple Sclerosis: A Role for Liver X Receptors?Frontiers in endocrinology · 2021Review
- Microglia facilitate repair of demyelinated lesions via post-squalene sterol synthesis.Nature neuroscience · 2021Article
- Epigenetic Regulation of Kupffer Cell Function in Health and Disease.Frontiers in immunology · 2020Review
- Role of Myeloid-Epithelial-Reproductive Tyrosine Kinase and Macrophage Polarization in the Progression of Atherosclerotic Lesions Associated With Nonalcoholic Fatty Liver Disease.Frontiers in pharmacology · 2019Review
- Integrating Thyroid Hormone Signaling in Hypothalamic Control of Metabolism: Crosstalk Between Nuclear Receptors.International journal of molecular sciences · 2018Review
- A critical role for ABC transporters in persistent lung inflammation in the development of emphysema after smoke exposure.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2018Article
- Cell-specific discrimination of desmosterol and desmosterol mimetics confers selective regulation of LXR and SREBP in macrophages.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- Article
- The challenges and promise of targeting the Liver X Receptors for treatment of inflammatory disease.Pharmacology & therapeutics · 2018Review
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 1 country.
Funding
Abstract
Liver X receptor (LXR), a nuclear hormone receptor, is an essential regulator of immune responses. Activation of LXR-mediated transcription by synthetic agonists, such as T0901317 and GW3965, attenuates progression of inflammatory disease in animal models. However, the adverse effects of these conventional LXR agonists in elevating liver lipids have impeded exploitation of this intriguing mechanism for chronic therapy. Here, we explore the ability of a series of sterol-based LXR agonists to alleviate inflammatory conditions in mice without hepatotoxicity. We show that oral treatment with sterol-based LXR agonists in mice significantly reduces dextran sulfate sodium colitis-induced body weight loss, which is accompanied by reduced expression of inflammatory markers in the large intestine. The anti-inflammatory property of these agonists is recapitulated in vitro in mouse lamina propria mononuclear cells, human colonic epithelial cells, and human peripheral blood mononuclear cells. In addition, treatment with LXR agonists dramatically suppresses inflammatory cytokine expression in a model of traumatic brain injury. Importantly, in both disease models, the sterol-based agonists do not affect the liver, and the conventional agonist T0901317 results in significant liver lipid accumulation and injury. Overall, these results provide evidence for the development of sterol-based LXR agonists as novel therapeutics for chronic inflammatory diseases.-Yu, S., Li, S., Henke, A., Muse, E. D., Cheng, B., Welzel, G., Chatterjee, A. K., Wang, D., Roland, J., Glass, C. K., Tremblay, M. Dissociated sterol-based liver X receptor agonists as therapeutics for chronic inflammatory diseases.
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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.