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.
Hudson, S. A., McLean, K. J., Surade, S., Yang, Y-Q., Leys, D., Ciulli, A., Munro, A. W., & Abell, C. (2012). Application of fragment screening and merging to the discovery of inhibitors of the Mycobacterium tuberculosis cytochrome P450 CYP121. Angewandte Chemie International Edition, 51(37), 9311-9316. https://doi.org/10.1002/anie.201202544