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Pregnane X Receptor as the “Sensor and Effector” in Regulating Epigenome
Journal of Cellular Physiology, 2014The pregnane X receptor (PXR, NR1I2) is a ligand‐activated nuclear receptor which plays an essential role in organism's metabolic detoxification system by sensing the presence of xenobiotics and triggering detoxification responses. In addition to its role in xenobiotic metabolism, PXR has pleiotropic functions in regulating immune/inflammatory ...
Xi, Ma, Jingshu, Chen, Yanan, Tian
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Epigenetic regulation of pregnane X receptor activity
Drug Metabolism Reviews, 2013Pregnane X receptor (PXR, NR1I2) is a ligand-dependent nuclear receptor (NR) that functions as a xenobiotic sensor and effector in coordinately regulating expression of genes of the xenobiotic detoxification network. PXR exerts its transcriptional regulatory functions by dimerization with retinoic X receptor RXR, and PXR-RXR complex binds to specific ...
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Diethylstilbestrol-scaffold-based pregnane X receptor modulators
European Journal of Medicinal Chemistry, 2015Due to its function as a regulator of drug-metabolizing enzymes and transporters, pregnane X receptor (PXR) represents an important factor involved in drug metabolism. In this work, we describe the discovery of diethylstilbestrol-based PXR modulators, which were designed from marine sulfated steroids with PXR agonistic activity, solomonsterols A and B,
Hodnik, Ž +6 more
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INDUCTION OF ABCC3 (MRP3) BY PREGNANE X RECEPTOR ACTIVATORS
Drug Metabolism and Disposition, 2003The pregnane X receptor (PXR) mediates the induction of various genes by xenobiotics, including several ATP-binding cassette transporters. PXR is also activated by bile acids likely to prevent their accumulation to toxic levels; however, the role of PXR in the regulation of MRP3, an important bile acid efflux transporter, has not been elucidated.
Shirley, Teng +2 more
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Ligand- and Structure-Based Pregnane X Receptor Models
2012The human pregnane X receptor (PXR) is a ligand dependent transcription factor that can be activated by structurally diverse agonists including steroid hormones, bile acids, herbal drugs, and prescription medications. PXR regulates the transcription of several genes involved in xenobiotic detoxification and apoptosis.
Sandhya, Kortagere +2 more
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Dietary phytochemicals as modulators of human pregnane X receptor
Critical Reviews in Food Science and Nutrition, 2023, Rajamanikkam Kamaraj, Petr Pavek
exaly
Pregnane-X receptor/constitutive androsterone receptor
Toxicology Letters, 2008Patrick Balaguer +5 more
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