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Issue 38, 2011
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High throughput discovery of heteroaromatic-modifying enzymes allows enhancement of novobiocin selectivity

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Abstract

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.

Graphical abstract: High throughput discovery of heteroaromatic-modifying enzymes allows enhancement of novobiocin selectivity

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Publication details

The article was received on 15 Jun 2011, accepted on 29 Jul 2011 and first published on 24 Aug 2011


Article type: Communication
DOI: 10.1039/C1CC13552J
Citation: Chem. Commun., 2011,47, 10569-10571
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    High throughput discovery of heteroaromatic-modifying enzymes allows enhancement of novobiocin selectivity

    S. M. Patel, M. D. L. Fuente, S. Ke, A. M. R. Guimarães, A. O. Oliyide, X. Ji, P. Stapleton, A. Osbourn, Y. Pan, D. J. Bowles, B. G. Davis, A. Schatzlein and M. Yang, Chem. Commun., 2011, 47, 10569
    DOI: 10.1039/C1CC13552J

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