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Keywords:

  • cytochrome P450;
  • drug design;
  • fragment screening;
  • tuberculosis
Thumbnail image of graphical abstract

Pieces of the puzzle: The first fragment-based approach was used to target cytochrome P450 enzymes (CYPs) for drug development (see scheme). The experiments provide new insights into the binding site of the essential Mycobacterium tuberculosis CYP121 enzyme, and resulted in a promising novel lead compound based on fragment merging.