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Liver X receptor biology and pharmacology: new pathways, challenges and opportunities
Abstract
Nuclear receptors (NRs) are master regulators of transcriptional programs that integrate the homeostatic control of almost all biological processes. Their direct mode of ligand regulation and genome interaction is at the core of modern pharmacology. The two liver X receptors LXRα and LXRβ are among the emerging newer drug targets within the NR family. LXRs are best known as nuclear oxysterol receptors and physiological regulators of lipid and cholesterol metabolism that also act in an anti-inflammatory way. Because LXRs control diverse pathways in development, reproduction, metabolism, immunity and inflammation, they have potential as therapeutic targets for diseases as diverse as lipid disorders, atherosclerosis, chronic inflammation, autoimmunity, cancer and neurodegenerative diseases. Recent insights into LXR signaling suggest future targeting strategies aiming at increasing LXR subtype and pathway selectivity. This review discusses the current status of our understanding of LXR biology and pharmacology, with an emphasis on the molecular aspects of LXR signaling that constitute the potential of LXRs as drug targets.
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Activation of LXR by oxysterols positively regulates LXR target genes and inhibits SREBP processing.
“Activation of LXR by oxysterols positively regulates LXR target genes and inhibits SREBP processing.”
From A novel posttranscriptional mechanism for dietary cholesterol-mediated suppression of liver LDL receptor expression (2014) · cites this paper as [34]
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Woo, J. H., Lee, J. H., Kim, H., Park, S. J., Joe, E.-H., & Jou, I. (2015) · Experimental Neurobiology · doi:10.5607/en.2015.24.2.95 · Cited by 44
Singh, A. B., Kan, C. F. K., Shende, V., Dong, B., & Liu, J. (2014) · Journal of Lipid Research · doi:10.1194/jlr.m049429 · Cited by 35
Metadata
- Authors
- Jakobsson, T., Treuter, E., Gustafsson, J.-Å., & Steffensen, K. R.
- Venue
- Trends in Pharmacological Sciences
- Publisher
- Elsevier BV
- Published
- 2012-07
- Volume
- 33
- Issue
- 7
- Pages
- 394-404
- ISSN
- 0165-6147
- Cited by
- 302
- References
- 7
- Language
- en
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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