Results 271 to 280 of about 235,181 (316)
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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.
Kang Yao +10 more
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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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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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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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ROLE OF THE NUCLEAR RECEPTOR PREGNANE X RECEPTOR IN ACETAMINOPHEN HEPATOTOXICITY
Drug Metabolism and Disposition, 2005The pregnane X receptor (PXR) is a transcriptional regulator of xenobiotic metabolizing enzymes, including cytochrome P450 3A (CYP3A), and transporters. Pretreatment of mice and rats with inducers of CYP3A increases acetaminophen (APAP) hepatotoxicity. In untreated mice, the amount of hepatic CYP3A11 mRNA is 4-fold greater in PXR(-/-) mice compared to ...
Sheryl G. Wood +19 more
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Pregnane X Receptor: Promiscuous regulator of detoxification pathways
The International Journal of Biochemistry & Cell Biology, 2007The Pregnane X Receptor (PXR) is pivotal for the body's response to toxic xenobiotics and endogenous metabolites. By acting as a ligand-activated transcription factor, PXR regulates all stages of xenobiotic metabolism and transport and is responsible for important inductive drug interactions.
Marko Matic +5 more
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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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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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Pregnane X receptor (PXR) – a contributor to the diabetes epidemic?
dmdi, 2013Abstract Pregnane X receptor (PXR), a ligand-activated nuclear receptor, was originally identified as a regulator of drug and bile acid metabolism. Studies in experimental animals and humans within the last decade have revealed PXR as a regulator of energy metabolism repressing gluconeogenesis and hepatic lipid oxidation. The most recent
Jukka Hakkola +2 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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