Ticlopidine as a selective mechanism-based inhibitor of human cytochrome P450 2C19.

@article{HaDuong2001TiclopidineAA,
  title={Ticlopidine as a selective mechanism-based inhibitor of human cytochrome P450 2C19.},
  author={Ng{\^u}yet-Thanh Ha-Duong and Sylvie Dijols and Arthur Macherey and Joyce A. Goldstein and Patrick M Dansette and Daniel Mansuy},
  journal={Biochemistry},
  year={2001},
  volume={40 40},
  pages={
          12112-22
        }
}
Experiments using recombinant yeast-expressed human liver cytochromes P450 confirmed previous literature data indicating that ticlopidine is an inhibitor of CYP 2C19. The present studies demonstrated that ticlopidine is selective for CYP 2C19 within the CYP 2C subfamily. UV-visible studies on the interaction of a series of ticlopidine derivatives with CYP 2C19 showed that ticlopidine binds to the CYP 2C19 active site with a K(s) value of 2.8 +/- 1 microM. Derivatives that do not involve either… CONTINUE READING
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