Abstract
The synthesis and biological evaluation of ten Michael acceptors containing potential proteasome inhibitors are described. Cellular targets of azide containing inhibitors and were assessed in HEK293T and RAW264.7 cells by a two step labeling strategy, followed by biotin-pulldown, affinity purification, on-bead tryptic digestion and LC-MS(2) identification. This strategy appears to be an attractive alternative to gel-based competition assays.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Cell Line
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology*
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Humans
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Oligopeptides / chemical synthesis
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Oligopeptides / chemistry*
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Oligopeptides / pharmacology*
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Proteasome Endopeptidase Complex / metabolism*
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Proteasome Inhibitors*
Substances
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Enzyme Inhibitors
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Oligopeptides
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Proteasome Inhibitors
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Proteasome Endopeptidase Complex