High throughput discovery of heteroaromatic-modifying enzymes allows enhancement of novobiocin selectivity.

Patel, S.M., Fuente, M.de la, Ke, S., Guimarães, A.M.R., Oliyide, A.O., Ji, X., Stapleton, P.D., Osbourn, A., Pan, Y., Bowles, D.J., Davis, B.G., Schatzlein, A.G. and Yang, M. (2011) High throughput discovery of heteroaromatic-modifying enzymes allows enhancement of novobiocin selectivity. Chemical Communications, 47 (38). pp. 10569-10571. 10.1039/C1CC13552J .

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DOI: 10.1039/C1CC13552J

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 × 10(4) fold increase in selectivity.

Item Type:Article
Departments, units and centres:Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry
ID Code:2318
Journal or Publication Title:Chemical Communications
Deposited By:Library Staff
Deposited On:13 Oct 2011 11:25
Last Modified:13 Oct 2011 11:55

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