The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.

@article{Lehmann1998TheHO,
  title={The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.},
  author={J{\"u}rgen M. Lehmann and D. D. Mckee and Mike A Watson and Timothy M. Willson and J T Moore and Steven A. Kliewer},
  journal={The Journal of clinical investigation},
  year={1998},
  volume={102 5},
  pages={
          1016-23
        }
}
The cytochrome P-450 monooxygenase 3A4 (CYP3A4) is responsible for the oxidative metabolism of a wide variety of xenobiotics including an estimated 60% of all clinically used drugs. Although expression of the CYP3A4 gene is known to be induced in response to a variety of compounds, the mechanism underlying this induction, which represents a basis for drug interactions in patients, has remained unclear. We report the identification of a human (h) orphan nuclear receptor, termed the pregnane X… Expand
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  • Biology, Medicine
  • Acta biochimica Polonica
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TLDR
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TLDR
PXR activation measurements using an in vitro reporter gene approach appears to provide a rapid and relatively inexpensive means for predicting whether compounds will induce CYP3A levels in vivo. Expand
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