Results 21 to 30 of about 8,905 (163)
Marine and Semi-Synthetic Hydroxysteroids as New Scaffolds for Pregnane X Receptor Modulation
Marine Drugs, 2014 In recent years many sterols with unusual structures and promising biological profiles have been identified from marine sources. Here we report the isolation of a series of 24-alkylated-hydroxysteroids from the soft coral Sinularia kavarattiensis, acting
Valentina Sepe +12 more
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Pregnane X Receptor (PXR) Polymorphisms and Cancer Treatment
Biomolecules, 2021 Pregnane X Receptor (PXR) belongs to the nuclear receptors’ superfamily and mainly functions as a xenobiotic sensor activated by a variety of ligands. PXR is widely expressed in normal and malignant tissues. Drug metabolizing enzymes and transporters are
Aikaterini Skandalaki +2 more
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Pregnane X Receptor Is a Target of Farnesoid X Receptor [PDF]
Journal of Biological Chemistry, 2006 The pregnane X receptor (PXR) is an essential component of the body's detoxification system. PXR is activated by a broad spectrum of xenobiotics and endobiotics, including bile acids and their precursors. Bile acids in high concentrations are toxic; therefore, their synthesis is tightly regulated by the farnesoid X receptor, and their catabolism ...
Jung D, Mangelsdorf DJ, Meyer UA
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Functional evolution of the pregnane X receptor [PDF]
Expert Opinion on Drug Metabolism & Toxicology, 2006 The pregnane X receptor (PXR; NR1I2) is a nuclear hormone receptor (NR) that transcriptionally regulates genes encoding transporters and drug-metabolising enzymes in the liver and intestine. PXR activation leads to enhanced metabolism and elimination of xenobiotics and endogenous compounds such as hormones and bile salts.
Manisha, Iyer +2 more
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The constitutive androstane receptor and pregnane X receptor in the brain [PDF]
British Journal of Pharmacology, 2020 Since their discovery, the orphan nuclear receptors constitutive androstane receptor (CAR;NR1I3) and pregnane X receptor (PXR;NR1I2) have been regarded as master regulators of drug disposition and detoxification mechanisms. They regulate the metabolism and transport of endogenous mediators and xenobiotics in organs including the liver, intestine and ...
Pablo Torres‐Vergara +5 more
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The pregnane X receptor in tuberculosis therapeutics [PDF]
Expert Opinion on Drug Metabolism & Toxicology, 2015 Among the infectious diseases, tuberculosis (TB) remains the second most common cause of death after HIV. TB treatment requires the combination of multiple drugs including the rifamycin class. However, rifamycins are activators of human pregnane X receptor (PXR), a transcription factor that regulates drug metabolism, drug resistance, energy metabolism ...
Amina I, Shehu +3 more
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Cells, 2021 The pregnane X receptor (PXR, NR1I2) is a nuclear receptor which exerts its regulatory function by heterodimerization with the retinoid-X-receptor α (RXRα, NR2B1) and binding to the promoter and enhancer regions of diverse target genes.
Juan Pablo Rigalli +3 more
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Post-translational modification of pregnane x receptor [PDF]
Pharmacological Research, 2011 Pregnane x receptor (PXR, NR1I2) was originally characterized as a broad spectrum entero-hepatic xenobiotic 'sensor' and master-regulator of drug inducible gene expression. A compelling description of ligand-mediated gene activation has been unveiled in the last decade that firmly establishes this receptor's central role in the metabolism and transport
Staudinger, Jeffrey Leonard +3 more
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Resveratrol as an Inhibitor of Pregnane X Receptor (PXR): Another Lesson in PXR Antagonism
Journal of Pharmacological Sciences, 2014 .: The pregnane X receptor (PXR) plays a central role in the regulation of metabolism. Only few PXR antagonists have been described and the mechanism of PXR inhibition is mostly hypothetical or believed to be allosteric.
Tomas Smutny, Petr Pavek
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PLoS ONE, 2015 Liver grafts donated after cardiac death are increasingly used to expand the donor pool but are prone to ischaemic-type biliary lesions. The anti-inflammatory effects of the activated pregnane X receptor have previously been shown to be beneficial in a ...
Aimen O Amer +10 more
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