Inhibition of human thiopurine methyltransferase by furosemide, bendroflumethiazide and trichlormethiazide

@article{Lysaa1996InhibitionOH,
  title={Inhibition of human thiopurine methyltransferase by furosemide, bendroflumethiazide and trichlormethiazide},
  author={Roy Andre Lysaa and Trude Giverhaug and H. Lib{\ae}k Wold and Jarle Aarbakke},
  journal={European Journal of Clinical Pharmacology},
  year={1996},
  volume={49},
  pages={393-396}
}
Results: Incubation in vitro of human recombinant and erythrocyte (RBC) thiopurine methyl transferase (TPMT) with furosemide, bendroflumethiazide and trichlormethiazide demonstrated inhibition of both enzyme preparations, with IC50 values of 170 μM, 360 μM and 1 mM, respectively. Kinetic studies revealed that the inhibition was mixed or non-competitive with regard both to the thiopurine substrate 6-mercaptopurine (6-MP) and the methyl donor S-adenosyl-L-methionine. Conclusion: Since S… CONTINUE READING