Abstract
Artemisinins induce drug metabolism through the activation of the pregnane X receptor (PXR) in vitro. Here, we report the resequencing and genotyping of PXR variants in 75 Vietnamese individuals previously characterized for CYP3A enzyme activity after artemisinin exposure. We identified a total of 31 PXR variants, including 5 novel single nucleotide polymorphisms (SNPs), and we identified significantly different allele frequencies relative to other ethnic groups. A trend of significance was observed between the level of CYP3A4 induction by artemisinin and two PXR variants, the 8118C→T (Y328Y) and 10719A→G variants.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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3' Untranslated Regions / genetics
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Alleles
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Antimalarials / pharmacology*
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Artemisinins / pharmacology*
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Cytochrome P-450 CYP3A / biosynthesis*
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Cytochrome P-450 CYP3A / genetics
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DNA Primers
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Enzyme Induction / drug effects
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Gene Frequency
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Genetic Variation
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Humans
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Pharmaceutical Preparations / metabolism
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Polymorphism, Single Nucleotide
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Pregnane X Receptor
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Receptors, Steroid / drug effects
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Receptors, Steroid / genetics*
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Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
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Vietnam / epidemiology
Substances
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3' Untranslated Regions
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Antimalarials
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Artemisinins
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DNA Primers
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Pharmaceutical Preparations
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Pregnane X Receptor
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Receptors, Steroid
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artemisinin
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Cytochrome P-450 CYP3A