In vitro studies on the metabolic activation of the furanopyridine L-754,394, a highly potent and selective mechanism-based inhibitor of cytochrome P450 3A4.

@article{SahaliSahly1996InVS,
  title={In vitro studies on the metabolic activation of the furanopyridine L-754,394, a highly potent and selective mechanism-based inhibitor of cytochrome P450 3A4.},
  author={Y Sahali-Sahly and Suresh K. Balani and Jiunn Huei Lin and Thomas A Baillie},
  journal={Chemical research in toxicology},
  year={1996},
  volume={9 6},
  pages={1007-12}
}
L-754,394, a furanopyridine derivative, is an experimental anti-HIV agent which has been shown to be an unusually potent and selective inhibitor of cytochrome P450 3A enzymes in a number of mammalian species. In the present studies, L-754,394 was demonstrated to undergo NADPH-dependent metabolic activation in hepatic microsomal preparations from rats, dogs, rhesus monkeys, and humans to electrophilic intermediates which became bound covalently to cellular proteins. The extent of binding was… CONTINUE READING