Rat cytochrome p450 1A and 3A enzymes involved in bioactivation of tegafur to 5-fluorouracil and autoinduced by tegafur in liver microsomes.

@article{Yamazaki2001RatCP,
  title={Rat cytochrome p450 1A and 3A enzymes involved in bioactivation of tegafur to 5-fluorouracil and autoinduced by tegafur in liver microsomes.},
  author={Hiroshi Yamazaki and Tomoko Komatsu and Kei Takemoto and Noriaki Shimada and Miki Nakajima and Tsuyoshi Yokoi},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2001},
  volume={29 6},
  pages={794-7}
}
Tegafur, an anticancer prodrug, is reported to be bioactivated to 5-fluorouracil (5-FU) by cytochrome P450 (P450) enzymes. Liver microsomal P450 enzymes involved in the biotransformation of tegafur into 5-FU in rats and the effect of tegafur in vivo on P450 levels in rats were investigated. Of 12 cDNA-expressed rat P450 enzymes tested, CYP1A2, CYP3A1, and CYP2C11 had high 5-FU formation rates from 100 microM and 1.0 mM tegafur concentrations. The contributions of CYP1A, CYP2C, and CYP3A enzymes… CONTINUE READING

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