Abstract
Using click chemistry to enable both structural diversity and proteome profiling within a natural product derived library, two out of nineteen lipstatin analogues showed similar activity to Orlistat against fatty acid synthase (FAS), but with an improved ability to induce tumour cell death.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Click Chemistry
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Fatty Acid Synthases / antagonists & inhibitors*
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Fatty Acid Synthases / metabolism
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Humans
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Lactones / chemical synthesis
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Lactones / chemistry*
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Lactones / pharmacology
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Orlistat
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Proteome / chemistry*
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Proteome / metabolism
Substances
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Antineoplastic Agents
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Lactones
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Proteome
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Orlistat
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lipstatin
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Fatty Acid Synthases