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Chem Commun (Camb). 2011 Oct 14;47(38):10569-71. doi: 10.1039/c1cc13552j. Epub 2011 Aug 24.

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

Author information

1
Department of Pharmaceutical & Biological Chemistry, The School of Pharmacy, University of London, 29/39 Brunswick Square, London, WC1N 1AX, UK.

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.

PMID:
21863200
DOI:
10.1039/c1cc13552j
[Indexed for MEDLINE]

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