The development of a cocktail CYP2B6, CYP2C8, and CYP3A5 inhibition assay and a preliminary assessment of utility in a drug discovery setting.

@article{ODonnell2007TheDO,
  title={The development of a cocktail CYP2B6, CYP2C8, and CYP3A5 inhibition assay and a preliminary assessment of utility in a drug discovery setting.},
  author={Charles J L O'Donnell and Kenneth H Grime and Paul Courtney and Dean Slee and Rob Riley},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2007},
  volume={35 3},
  pages={381-5}
}
Tools for studying the roles of CYP2B6, CYP2C8, and CYP3A5 in drug metabolism have recently become available. The level of interest in these enzymes has been elevated because investigations have revealed substrate promiscuity and/or polymorphic expression. In this study, we aimed to develop a single cocktail inhibition assay for the three enzymes and assess its utility in drug discovery. Bupropion hydroxylation, amodiaquine N-deethylation, and midazolam 1'-hydroxylation were chosen as probe… CONTINUE READING

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