Polycyclic aromatic hydrocarbons stimulate human CYP3A4 promoter activity via PXR.

@article{Luckert2013PolycyclicAH,
  title={Polycyclic aromatic hydrocarbons stimulate human CYP3A4 promoter activity via PXR.},
  author={Claudia Luckert and Anke Ph. D. Ehlers and Thorsten Buhrke and Albrecht Seidel and A. Lampen and Sebastian Hessel},
  journal={Toxicology letters},
  year={2013},
  volume={222 2},
  pages={
          180-8
        }
}
Metabolic activation of polycyclic aromatic hydrocarbons (PAH) is mediated mainly by cytochrome P₄₅₀ monooxygenases (CYP) CYP1A1, 1A2 and 1B1. Several PAH are known to induce these CYP via aryl hydrocarbon receptor (AhR) signaling. Recently, it was shown that the PAH benzo[a]pyrene (BaP) can induce CYP3A4 as well. The induction was suggested to be mediated by the pregnane X receptor (PXR) rather than AhR. Metabolism by CYP3A4 is only known for dihydrodiol metabolites of PAH but not for their… CONTINUE READING
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