Pregnane X receptor and natural products: beyond drug–drug interactions

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Pregnane X receptor and natural products: beyond drug-drug interactions.

The pregnane X receptor (PXR, NR1I2) is a member of the nuclear receptor superfamily that is activated by a myriad of compounds and natural products in clinical use. Activation of PXR represents the basis for several clinically important drug-drug interactions. Although PXR activation has undesirable effects in patients on combination therapy, it also mediates the hepatoprotective effects exhib...

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Synthetic drugs and natural products as modulators of constitutive androstane receptor (CAR) and pregnane X receptor (PXR).

Constitutive androstane receptor (CAR) and pregnane X receptor (PXR) are members of the nuclear receptor superfamily. These transcription factors are predominantly expressed in the liver, where they are activated by structurally diverse compounds, including many drugs and endogenous substances. CAR and PXR regulate the expression of a broad range of genes, which contribute to transcellular tran...

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Activation of pregnane X receptor inhibits

Received 8 August 2012 Revised 7 November 2012 Accepted 2 December 2012 Published Online First 5 January 2013 ABSTRACT Objective To assess the antifibrotic effects of pregnane X receptors (PXRs) in experimental dermal fibrosis. Methods The antifibrotic effects of PXR activation by 5-pregnen-3β-ol-20-one-16α-carbonitrile (PCN) were studied in the bleomycin model for prevention of dermal fibrosis...

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The human pregnane X receptor: genomic structure and identification and functional characterization of natural allelic variants.

The pregnane X receptor (PXR)/steroid and xenobiotic receptor (SXR) transcriptionally activates cytochrome P4503A4 (CYP3A4) when ligand activated by endobiotics and xenobiotics. We cloned the human PXR gene and analysed the sequence in DNAs of individuals whose CYP3A phenotype was known. The PXR gene spans 35 kb, contains nine exons, and mapped to chromosome 13q11-13. Thirty-eight single nucleo...

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Indolizidines and quinolizidines: natural products and beyond

Alkaloids occur in such astonishing profusion in nature that one tends to forget that they are assembled from a relatively small number of structural motifs. Among the motifs that are most frequently encountered are bicyclic systems containing bridgehead nitrogen, especially 1azabicyclo[4.3.0]nonanes and 1-azabicyclo[4.4.0]decanes or their unsaturated analogues – the indolizidines and quinolizi...

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ژورنال

عنوان ژورنال: Expert Opinion on Drug Metabolism & Toxicology

سال: 2006

ISSN: 1742-5255,1744-7607

DOI: 10.1517/17425255.2.6.847