Effect of ketoconazole on cholesterol synthesis and on HMG-CoA reductase and LDL-receptor activities in Hep G2 cells.

@article{Kempen1987EffectOK,
  title={Effect of ketoconazole on cholesterol synthesis and on HMG-CoA reductase and LDL-receptor activities in Hep G2 cells.},
  author={Herman J Kempen and K van Son and Louis H. Cohen and Marieke Griffioen and Hans Verboom and Louis M. Havekes},
  journal={Biochemical pharmacology},
  year={1987},
  volume={36 8},
  pages={
          1245-9
        }
}
Ketoconazole, an imidazole derivative, is a member of a class of metabolic inhibitors acting specifically at cytochrome-P450 mediated reactions. We studied the effects of this compound on cholesterol synthesis, and on HMG-CoA reductase and LDL receptor activities, in cultures of human hepatoma cell line Hep G2. Ketoconazole, added in concentrations of 2-100 microM, inhibited cholesterol synthesis, and caused accumulation of lanosterol and dihydrolanosterol. Total mass formation of sterols was… 
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