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.
This journal is © The Royal Society of Chemistry 2011
MeSH terms
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Cell Line, Tumor
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DNA Topoisomerases, Type II / chemistry
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DNA Topoisomerases, Type II / metabolism
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Drug Screening Assays, Antitumor
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / toxicity
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Enzymes / chemistry*
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Enzymes / metabolism
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Glycosylation / drug effects
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HSP90 Heat-Shock Proteins / antagonists & inhibitors
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HSP90 Heat-Shock Proteins / metabolism
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Humans
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Novobiocin / chemical synthesis
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Novobiocin / chemistry*
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Novobiocin / toxicity
Substances
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Enzyme Inhibitors
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Enzymes
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HSP90 Heat-Shock Proteins
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Novobiocin
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DNA Topoisomerases, Type II