Polymorphic variants (CYP2C9*3 and CYP2C9*5) and the F114L active site mutation of CYP2C9: effect on atypical kinetic metabolism profiles.

@article{Tracy2002PolymorphicV,
  title={Polymorphic variants (CYP2C9*3 and CYP2C9*5) and the F114L active site mutation of CYP2C9: effect on atypical kinetic metabolism profiles.},
  author={Timothy S. Tracy and James Matthew Hutzler and Robert L Haining and Allan E Rettie and Matthew A. Hummel and Leslie J. Dickmann},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2002},
  volume={30 4},
  pages={385-90}
}
CYP2C9 wild-type protein has been shown to exhibit atypical kinetic profiles of metabolism that may affect in vitro-in vivo predictions made during the drug development process. Previous work suggests a substrate-dependent effect of polymorphic variants of CYP2C9 on the rate of metabolism; however, it is hypothesized that these active site amino acid changes will affect the kinetic profile of a drug's metabolism as well. To this end, the kinetic profiles of three model CYP2C9 substrates… CONTINUE READING

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