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Liver X receptors and liver physiology
Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease, 2021The liver x receptors LXRα (NR1H3) and LXRβ (NR1H2) are members of the nuclear hormone receptor superfamily of ligand dependent transcription factors that regulate transcription in response to the direct binding of cholesterol derivatives. Studies using genetic knockouts and synthetic ligands have defined the LXRs as important modulators of lipid ...
Lillian, Russo-Savage, Ira G, Schulman
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Pregnane X Receptor Activation in Liver Perfusion
Transplantation Proceedings, 2022Liver normothermic machine perfusion (NMP) is being adopted as a method of optimizing livers before transplantation. However, there is further potential to use the NMP model as a platform for drug delivery. Pregnane X receptor (PXR) activation upregulates CYP3A expression and has been shown to be protective against ischemia-reperfusion in rodents.
Samuel Moulding +6 more
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Action mechanisms of Liver X Receptors
Biochemical and Biophysical Research Communications, 2014The two Liver X Receptors, LXRα and LXRβ, are nuclear receptors belonging to the superfamily of ligand-activated transcription factors. They share more than 78% homology in amino acid sequence, a common profile of oxysterol ligands and the same heterodimerization partner, Retinoid X Receptor. LXRs play crucial roles in several metabolic pathways: lipid
Chiara, Gabbi +2 more
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Targeting liver X receptors in inflammation
Expert Opinion on Therapeutic Targets, 2013The two oxysterol receptors, 'liver X receptors (LXRs)' LXRα and LXRβ, are amongst the emerging newer drug targets within the nuclear receptor family and targeting LXRs represents novel strategies needed for prevention and treatment of diseases where current therapeutics is inadequate.This review discusses the current understanding of LXR biology with ...
Knut R, Steffensen +2 more
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Liver X Receptors, Atherosclerosis and Inflammation
Current Atherosclerosis Reports, 2012Liver X receptors (LXRs) belong to the nuclear receptor superfamily of ligand-dependent transcription factors. LXRs are activated by oxysterols, metabolites of cholesterol, and therefore act as intracellular sensors of this lipid. There are two LXR genes (α and β) that display distinct tissue/cell expression profiles.
Daryn R, Michael +3 more
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A structural perspective of liver X receptors
2023Liver X receptors α and β are members of the nuclear receptor family, which comprise a flexible N-terminal domain, a DNA binding domain, a hinge linker, and a ligand binding domain. Liver X receptors are important regulators of cholesterol and lipid homeostasis by controlling the transcription of numerous genes.
Jan-Åke, Gustafsson +3 more
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Liver X Receptor and Farnesoid X Receptor as Therapeutic Targets
The American Journal of Cardiology, 2007Despite the success of existing therapies, new therapies targeted toward dyslipidemia are still needed. Liver X receptor (LXR) and farnesoid X receptor (FXR) represent 2 very different attractive targets for new therapeutic development. LXR is a nuclear receptor that primarily acts to rid cells and the body of excess cholesterol. LXR agonists have been
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Targeting liver X receptors in cancer therapeutics
Nature Reviews Cancer, 2015Members of the nuclear receptor superfamily of ligand-dependent transcription factors carry out vital cellular functions and are highly druggable therapeutic targets. Liver X receptors (LXRs) are nuclear receptor family members that function in cholesterol transport, glucose metabolism and the modulation of inflammatory responses.
Chin-Yo, Lin, Jan-Åke, Gustafsson
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The Liver X Receptor and Atherosclerosis
New England Journal of Medicine, 2007Atherosclerosis can be prevented in mice by treating them with a ligand of the liver X receptor β, a protein expressed by macrophages.
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Liver X receptor: from metabolism to cancer
Biochemical Journal, 2014Cholesterol plays an indispensable role in regulating the properties of cell membranes in mammalian cells. Accumulation of cholesterol and its intermediates, such as oxysterols, lead to activation of the nuclear receptors LXRs (liver X receptors).
Nicolas, Venteclef, Pascal, Ferré
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