Results 211 to 220 of about 18,065 (250)
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Pregnane X Receptor‐Mediated Transcription

2005
The 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
openaire   +2 more sources

Diethylstilbestrol-scaffold-based pregnane X receptor modulators

European Journal of Medicinal Chemistry, 2015
Due 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
openaire   +3 more sources

Pregnane X Receptor Agonists Impair Postprandial Glucose Tolerance

Clinical Pharmacology & Therapeutics, 2013
We conducted a randomized, open, placebo-controlled crossover trial to investigate the effects of the pregnane X receptor (PXR) agonist rifampin on an oral glucose tolerance test (OGTT) in 12 healthy volunteers. The subjects were administered 600 mg rifampin or placebo once daily for 7 days, and OGTT was performed on the eighth day.
Hukkanen Janne   +5 more
openaire   +2 more sources

Transcriptional Regulation of the Human Pregnane-X Receptor

Drug Metabolism Reviews, 2006
This 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
openaire   +3 more sources

Functions of pregnane X receptor in self-detoxification

Amino Acids, 2017
Pregnane 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
openaire   +2 more sources

Pregnane X Receptor: Promiscuous regulator of detoxification pathways

The International Journal of Biochemistry & Cell Biology, 2007
The 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
openaire   +2 more sources

[Advances on pregnane X receptor].

Sheng li ke xue jin zhan [Progress in physiology], 2012
Pregnane 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.
Dan, Pu, You-Fei, Guan
openaire   +3 more sources

A Pharmacophore for Human Pregnane X Receptor Ligands

Drug Metabolism and Disposition, 2002
The 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
openaire   +2 more sources

Epigenetic regulation of pregnane X receptor activity

Drug Metabolism Reviews, 2013
Pregnane 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 ...
openaire   +2 more sources

Rabbit Pregnane X Receptor Is Activated by Rifampicin

Drug Metabolism and Disposition, 2000
Reverse 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
openaire   +2 more sources

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