High throughput discovery of heteroaromatic-modifying enzymes allows enhancement of novobiocin selectivity
Literature Information
Sital M. Patel, Maria de la Fuente, Song Ke, Andreia M. R. Guimarães, Adeola O. Oliyide, Xiaoyun Ji, Paul Stapleton, Anne Osbourn, Yi Pan, Dianna J. Bowles, Benjamin G. Davis, Andreas Schatzlein, Min Yang
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 × 104 fold increase in selectivity.
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