Gene-selective modulation by a synthetic oxysterol ligand of the liver X receptor Published, JLR Papers in Press, August 1, 2004. DOI 10.1194/jlr.M400257-JLR200

@article{Quinet2004GeneselectiveMB,
  title={Gene-selective modulation by a synthetic oxysterol ligand of the liver X receptor Published, JLR Papers in Press, August 1, 2004. DOI 10.1194/jlr.M400257-JLR200},
  author={E. Quinet and D. Savio and Anita R Halpern and L. Chen and C. Miller and P. Nambi},
  journal={Journal of Lipid Research},
  year={2004},
  volume={45},
  pages={1929 - 1942}
}
Liver X receptors (LXRs) play key roles in the regulation of cholesterol homeostasis by limiting cholesterol accumulation in macrophages within arterial wall lesion sites by a mechanism that includes the upregulation of ATP binding cassette transporters. These atheroprotective properties distinguish LXRs as potential targets for pharmaceutical intervention in cardiovascular disease. Their associated activity for promoting lipogenesis and triglyceride accretion through the activation of sterol… Expand
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The liver X receptors (LXRs), members of the nuclear receptor superfamily, play an important role in controlling lipid homeostasis by activating several genes involved in reverse cholesterol transport and deletion and mutational studies indicate it plays a critical role in LXR-mediated induction. Expand
Synthetic LXR ligand inhibits the development of atherosclerosis in mice
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It is demonstrated here that the nonsteroidal LXR agonist GW3965 has potent antiatherogenic activity in two different murine models, providing direct evidence for an atheroprotective effect of LXRs agonists and support their further evaluation as potential modulators of human cardiovascular disease. Expand
Regulation of mouse sterol regulatory element-binding protein-1c gene (SREBP-1c) by oxysterol receptors, LXRα and LXRβ
TLDR
A novel LXR target is described, the sterol regulatory element-binding protein-1c gene (SREBP-1C), which encodes a membrane-bound transcription factor of the basic helix-loop-helix-leucine zipper family and reveals a unique regulatory interplay between cholesterol and fatty acid metabolism. Expand
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It is reported that natural and synthetic LXR ligands induce the expression of the LXRα gene in primary human macrophages and differentiated THP-1 macrophage and that this response is likely to amplify the effects of oxysterols on reverse cholesterol transport. Expand
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TLDR
It is demonstrated that in addition to tandem SREBP sites, the FASpromoter contains a high affinity binding site for the LXR/RXR heterodimer that is conserved in diverse animal species including birds, rodents, and humans. Expand
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TLDR
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TLDR
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TLDR
Endogenous ABC1 gene expression in RAW cells and apolipoprotein A-I mediated cholesterol efflux were also upregulated by both receptor ligands, raising the possibility that ligands that activate the LXR-RXR heterodimer may be useful for the therapeutic modulation of the ABC1 pathway. Expand
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TLDR
Elimination of LXR activity in bone marrow-derived cells mimics many aspects of Tangier disease, a human high density lipoprotein deficiency, including aberrant regulation of cholesterol transporter expression, lipid accumulation in macrophages, splenomegaly, and increased atherosclerosis. Expand
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TLDR
The addition of ABCG5 and ABCG8 to the growing list of LXR target genes further supports the notion that LXRs serve as sterol sensors to coordinately regulate sterol catabolism, storage, efflux, and elimination. Expand
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