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The pregnane X receptor: from bench to bedside [PDF]
The pregnane X receptor (PXR; NR1I2), a member of the nuclear receptor superfamily, regulates the expression of metabolic enzymes and transporters involved in the response of mammals to their chemical environment.To summarize the functions and clinical implications of PXR.In the current review, the clinical implications of PXR are discussed, and the ...
Jeffrey R Idle, Frank J Gonzalez
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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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Transcriptional Regulation of the Human Pregnane-X Receptor
Drug Metabolism Reviews, 2006This review addresses the general structure and function of nuclear receptors and places specific emphasis on their role in xenosensing, resulting in the activation of a battery of genes mediating drug metabolism, conjugation, and transport. The pregnane-X receptor is a nuclear receptor that functions to control a battery of genes predominantly ...
Gibson, GG +4 more
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Pregnane X receptor and drug-induced liver injury [PDF]
The liver plays a central role in transforming and clearing foreign substances. The continuous exposure of the liver to xenobiotics sometimes leads to impaired liver function, referred to as drug-induced liver injury (DILI). The pregnane X receptor (PXR) tightly regulates the expression of genes in the hepatic drug-clearance system and its undesired ...
Sérgio C Chai, Taosheng Chen
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Pregnane X Receptor‐Mediated Transcription
2005The pregnane X receptor (PXR, receptor NR1I2) is a ligand-activated transcription factor that is activated by structurally diverse endogenous steroids and foreign chemicals and serves as an important steroid and xenobiotic sensor. This member of the nuclear receptor superfamily is highly expressed in liver and in the gastrointestinal tract, where it ...
Thomas K H, Chang, David J, Waxman
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Dietary phytochemicals as modulators of human pregnane X receptor
Critical Reviews in Food Science and Nutrition, 2021As a promiscuous xenobiotic sensor, pregnane X receptor (PXR) plays a crucial role in drug metabolism. Since dietary phytochemicals exhibit the potential to modulate human PXR, this review aims to summarize the plant-derived PXR modulators, including agonists, partial agonists, and antagonists.
Jie, Zhang +4 more
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A Pharmacophore for Human Pregnane X Receptor Ligands
Drug Metabolism and Disposition, 2002The pregnane X receptor (PXR) is involved in transcriptional regulation of multiple cytochromes P450 and multidrug resistance-associated protein (MDR1), which encodes for the drug transporter P-glycoprotein. Crystal structure analyses suggest that the ligand binding domain is highly hydrophobic and flexible, allowing molecules of differing sizes to ...
Sean, Ekins, Jon A, Erickson
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Functions of pregnane X receptor in self-detoxification
Amino Acids, 2017Pregnane X receptor (PXR, NR1I2), a member of the nuclear receptor superfamily, is a crucial regulator of nutrient metabolism and metabolic detoxification such as metabolic syndrome, xenobiotic metabolism, inflammatory responses, glucose, cholesterol and lipid metabolism, and endocrine homeostasis.
Liuqin, He +8 more
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Rabbit Pregnane X Receptor Is Activated by Rifampicin
Drug Metabolism and Disposition, 2000Reverse transcriptase-polymerase chain reaction was used to amplify a partial cDNA from rabbit lung mRNA that shared 77% protein sequence identity with the mouse pregnane X receptor (PXR). Rapid amplification of cDNA ends from a rabbit kidney lambdaZAP expression library resulted in the isolation of overlapping cDNAs spanning the complete coding ...
U, Savas +3 more
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[Advances on pregnane X receptor].
Sheng li ke xue jin zhan [Progress in physiology], 2012Pregnane X receptor (PXR), termed with its cognate ligand, is a member of the nuclear receptor superfamily. PXR is expressed mainly in liver, intestine, stomach and kidney, and plays a central role in protecting tissues from potentially toxic exogenous and endogenous compounds.
Jian-ming, Zhou +2 more
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