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Pregnane X receptor (PXR): PXR turns on sulfation in phase 2 detoxification, regulating the processing of xenobiotic and endogenous compounds.
Improvement of pruritus and shortening of symptomatic phase has been described in BRIC patients treated with the antibiotic rifampicin, a potent human activator of PXR [76, 77].
Chen et al., "Fluoxetine reduces CES1, CES2, and CYP3A4 expression through decreasing PXR and increasing DEC1 in HepG2 cells," Xenobiotica, vol.
Jones et al., "The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity," Proceedings of the National Academy of Sciences of the United States of America, vol.
Pascussi, "Xenoreceptors CAR and PXR activation and consequences on lipid metabolism, glucose homeostasis, and inflammatory response," Molecular Pharmaceutics, vol.
For ease of interpretation, the data on the 37 in vitro assay endpoints were sub-divided into six groups by the molecular targets as follows: estrogen receptor, PPAR, PXR, aromatase, enzyme, and other (see Tab.
Cyp3a expression has been shown to be regulated by nuclear receptors, including PXR and CAR,,, where with a decrease in nuclear translocation of these receptors, the expression of Cyp3a also declined.
Nuclear receptors CAR and PXR in the regulation of hepatic metabolism.
LS174T cells provide a suitable in-vitro model to test for the effect of Pregnane X receptor (PXR), which mediates the induction of intestinal P-glycoprotein using rifampicin (10).
Treatment of 12-week-old asymptomatic hAPP mice for 7 days with pregnenolone16a-carbonitrile to activate the nuclear receptor pregnane X receptor (PXR) restored ABCB1 expression and transport activity in the brain capillaries and significantly reduced the brain A[beta] levels compared with untreated control mice .
Imai et al., "Mode of action of ethyl tertiary-butyl ether hepatotumorigenicity in the rat: Evidence for a role of oxidative stress via activation of CAR, PXR and PPAR signaling pathways," Toxicology and Applied Pharmacology, vol.
E- and Z guggulsterones of guggul gum are responsible for the hypolipidaemic activity and they act as the FXR antagonist a nuclear hormone receptor, a bile acid receptor (BAR) antagonist a member of the intracellular receptor superfamily and also inhibit human gene cholesterol 7-alpha-hydroxylase (CYP7A1) gene via activation of pregnane X receptor (PXR).
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