High throughput discovery of heteroaromatic-modifying enzymes allows enhancement of novobiocin selectivity.
Patel SM., de la Fuente M., Ke S., Guimarães AMR., Oliyide AO., Ji X., Stapleton P., Osbourn A., Pan Y., Bowles DJ., Davis BG., Schatzlein A., Yang M.
Glycosylated analogues of novobiocin, discovered using a broad library of enzymes, have 100-fold improved activity against breast, brain, pancreatic, lung and ovarian cancers and ablated associated off-target activity leading to an up to 2.7 × 10(4) fold increase in selectivity.