PXR Variants and Artemisinin Use in Vietnamese Subjects: Frequency Distribution and Impact on the Interindividual Variability of CYP3A Induction by Artemisinin | Zendy

Rita Piedade | Zendy; Elke Schaeffeler | Zendy; Stefan Winter | Zendy; Sara Asimus | Zendy; Matthias Schwab | Zendy; Michael Ashton | Zendy; Oliver Burk | Zendy; José Pedro Gil | Zendy

Open Access

PXR Variants and Artemisinin Use in Vietnamese Subjects: Frequency Distribution and Impact on the Interindividual Variability of CYP3A Induction by Artemisinin

Author(s) -

Rita Piedade,

Elke Schaeffeler,

Stefan Winter,

Sara Asimus,

Matthias Schwab,

Michael Ashton,

Oliver Burk,

José Pedro Gil

Publication year - 2012

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.06009-11

Subject(s) - pregnane x receptor , artemisinin , genotyping , single nucleotide polymorphism , cyp3a , vietnamese , biology , cyp3a4 , pharmacogenetics , pharmacology , genetics , genotype , cytochrome p450 , endocrinology , in vitro , metabolism , immunology , malaria , plasmodium falciparum , gene , transcription factor , microsome , nuclear receptor , linguistics , philosophy

Artemisinins induce drug metabolism through the activation of the pregnane X receptor (PXR)in vitro . Here, we report the resequencing and genotyping ofPXR variants in 75 Vietnamese individuals previously characterized for CYP3A enzyme activity after artemisinin exposure. We identified a total of 31PXR 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 twoPXR variants, the 8118C→T (Y328Y) and 10719A→G variants.

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