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

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.

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Bibliographische Detailangaben
Veröffentlicht in:	Chemical communications (Cambridge, England) England), 2011-10, Vol.47 (38), p.10569
Hauptverfasser:	Patel, Sital M, de la Fuente, Maria, Ke, Song, Guimarães, Andreia M R, Oliyide, Adeola O, Ji, Xiaoyun, Stapleton, Paul, Osbourn, Anne, Pan, Yi, Bowles, Dianna J, Davis, Benjamin G, Schatzlein, Andreas, Yang, Min
Format:	Artikel
Sprache:	eng
Schlagworte:	Cell Line, Tumor DNA Topoisomerases, Type II - chemistry DNA Topoisomerases, Type II - metabolism Drug Screening Assays, Antitumor Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - toxicity Enzymes - chemistry Enzymes - metabolism Glycosylation - drug effects HSP90 Heat-Shock Proteins - antagonists & inhibitors HSP90 Heat-Shock Proteins - metabolism Humans Novobiocin - chemical synthesis Novobiocin - chemistry Novobiocin - toxicity
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Beschreibung
Zusammenfassung:	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.
ISSN:	1359-7345 1364-548X
DOI:	10.1039/c1cc13552j