Evaluation of fluorescence- and mass spectrometry-based CYP inhibition assays for use in drug discovery.

@article{Bell2008EvaluationOF,
  title={Evaluation of fluorescence- and mass spectrometry-based CYP inhibition assays for use in drug discovery.},
  author={Leslie C Bell and Shari Bickford and Phong H. Nguyen and Jianling Wang and Timothy He and Bailin Zhang and Yannick Friche and Alfred G. Zimmerlin and Laszlo Urban and Dejan Bojanic},
  journal={Journal of biomolecular screening},
  year={2008},
  volume={13 5},
  pages={343-53}
}
The potential for metabolism-related drug-drug interactions by new chemical entities is assessed by monitoring the impact of these compounds on cytochrome P450 (CYP) activity using well-characterized CYP substrates. The conventional gold standard approach for in vitro evaluation of CYP inhibitory potential uses pooled human liver microsomes (HLM) in conjunction with prototypical drug substrates, often quantified by LC-MS/MS. However, fluorescent CYP inhibition assays, which use recombinantly… CONTINUE READING