Comparison of two immortalized human cell lines to study nuclear receptor-mediated CYP3A4 induction.

@article{Harmsen2008ComparisonOT,
  title={Comparison of two immortalized human cell lines to study nuclear receptor-mediated CYP3A4 induction.},
  author={Stefan Harmsen and Andries S Koster and Jos H. Beijnen and Jan H. M. Schellens and Irma Meijerman},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2008},
  volume={36 6},
  pages={1166-71}
}
Since CYP3A4 is responsible for the biotransformation of over 50% of all clinically used drugs, induction results in an increased clearance of many concomitantly administered drugs, thereby decreasing treatment efficacy or, in the case of prodrugs, lead to severe intoxications. CYP3A4 induction is regulated by the pregnane X receptor, constitutive androstane receptor, and vitamin D receptor. Since these nuclear receptors show large interspecies differences, accurate prediction of nuclear… CONTINUE READING

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