Ketoconazole-induced conformational changes in the active site of cytochrome P450eryF.

  title={Ketoconazole-induced conformational changes in the active site of cytochrome P450eryF.},
  author={Jill R. Cupp-Vickery and Carlos Garc{\'i}a and Andrew Hofacre and Kathleen Mcgee-Estrada},
  journal={Journal of molecular biology},
  volume={311 1},
The azole-based P450 inhibitor ketoconazole is used to treat fungal infections and functions by blocking ergosterol biosynthesis in yeast. Ketoconazole binds to mammalian P450 enzymes and this can result in drug-drug interactions and lead to liver damage. To identify protein-drug interactions that contribute to binding specificity and affinity, we determined the crystal structure of ketoconazole complexed with P450eryF. In the P450eryF/ketoconazole structure, the azole moiety and nearby rings… CONTINUE READING


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