Multisite kinetic models for CYP3A4: simultaneous activation and inhibition of diazepam and testosterone metabolism.

@article{Kenworthy2001MultisiteKM,
  title={Multisite kinetic models for CYP3A4: simultaneous activation and inhibition of diazepam and testosterone metabolism.},
  author={Kathryn E. Kenworthy and Stephen E. Clarke and J Andrews and J. Brian Houston},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2001},
  volume={29 12},
  pages={1644-51}
}
Some substrates of cytochrome P450 (CYP) 3A4, the most abundant CYP in the human liver responsible for the metabolism of many structurally diverse therapeutic agents, do not obey classical Michaelis-Menten kinetics and demonstrate homotropic and/or heterotropic cooperativity. The unusual kinetics and differential effects observed between substrates of this enzyme confound the prediction of drug clearance and drug-drug interactions from in vitro data. We have investigated the hypothesis that… CONTINUE READING
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