Pregnane X receptor (PXR) is a ligand-activated nuclear receptor that transcriptionally upregulates drug-metabolizing enzymes [e.g., cytochrome P450 3A4 (CYP3A4)] and transporters.
Rebecca R. Florke Gee +6 more
doaj +1 more source
A novel panel of mouse models to evaluate the role of human pregnane X receptor and constitutive androstane receptor in drug response [PDF]
The pregnane X receptor (PXR) and the constitutive androstane receptor (CAR) are closely related orphan nuclear hormone receptors that play a critical role as xenobiotic sensors in mammals.
Zevnik, Branko +13 more
core +1 more source
Resveratrol Suppresses the Inducible Expression of CYP3A4 Through the Pregnane X Receptor
.: The pregnane X receptor (PXR, NR1I2), a member of the nuclear receptor superfamily, is activated by a number of clinically prescribed drugs and herbal extracts.
Rongrong Deng +10 more
doaj +1 more source
Pregnane X receptor (PXR) is a key nuclear receptor that mediates drug metabolism and stimulates hepatocyte proliferation. However, the lack of PXR expression in human pluripotent stem cell-derived hepatocytes limits their application for drug screening ...
Hyemin Kim +5 more
doaj +1 more source
The evolution of drug-activated nuclear receptors: one ancestral gene diverged into two xenosensor genes in mammals [PDF]
BACKGROUND: Drugs and other xenobiotics alter gene expression of cytochromes P450 (CYP) by activating the pregnane X receptor (PXR) and constitutive androstane receptor (CAR) in mammals.
Urs A Meyer +26 more
core +1 more source
Regulation of xenobiotic and bile acid metabolism by the nuclear pregnane X receptor
The nuclear pregnane X receptor (PXR; NR1I2) is an integral component of the body's defense mechanism against chemical insult (chemoprotection). PXR is activated by a diverse array of lipophilic chemicals, including xenobiotics and endogenous substances,
Steven A. Kliewer, Timothy M. Willson
doaj +1 more source
Activation of Human Stearoyl-Coenzyme A Desaturase 1 Contributes to the Lipogenic Effect of PXR in HepG2 Cells [PDF]
The pregnane X receptor (PXR) was previously known as a xenobiotic receptor. Several recent studies suggested that PXR also played an important role in lipid homeostasis but the underlying mechanism remains to be clearly defined.
Wei, Yijuan +23 more
core +1 more source
The pregnane X receptor (PXR) regulates expression of proteins responsible for all three phases required for the detoxification mechanism, which include CYP450 enzymes, phase II enzymes, and multidrug efflux pumps.
Robert W. Marquis (440601) +11 more
core +1 more source
Mechanistic studies of the phenobarbital-type induction of cytochromes P450 : role of AMP-activated protein kinase [PDF]
Inside the liver cells there are sophisticated mechanisms that have evolved over millions of years to metabolize toxic substances, many of which are fat-soluble compounds making them difficult for the body to excrete.
Blättler, Sharon
core +1 more source
Regulation of hepatic heme synthesis by drugs, bile acids and nutrition : a transcriptional network regulating [delta]-aminolevulinic acid synthase 1 (ALAS1) [PDF]
ALAS1 is the rate limiting enzyme of heme synthesis. It is highly inducible in liver in cases of increased heme demand, such as drug metabolism or in inducible hepatic porphyrias.
Peyer, Anne-Kathrin
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