The differences in drug disposition gene induction by rifampicin and rifabutin are unlikely due to different effects on important pregnane X receptor (NR1I2) splice variants. [PDF]
Naunyn Schmiedebergs Arch PharmacolNilles J +7 more
europepmc +1 more source
Ostéomalacie consécutive à la prise prolongée de médicaments : Sur la piste de PXR, un récepteur impliqué dans la détoxication [PDF]
, 2005 Pascussi, Jean-Marc +1 more
core
Cocaine regulates antiretroviral therapy CNS access through pregnane-x receptor-mediated drug transporter and metabolizing enzyme modulation at the blood brain barrier. [PDF]
Fluids Barriers CNSColón Ortiz R +9 more
europepmc +1 more source
Pregnane X receptor: a double-edged sword.
Chinese medical journal, 2009 Dao-kui, Fang, Jian-qing, Zhang
openaire +1 more source
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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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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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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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Pregnane X Receptor Agonists Impair Postprandial Glucose Tolerance
Clinical Pharmacology & Therapeutics, 2013We 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
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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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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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