Abstract
Mammals express seven different catalytically active proteasome subunits. In order to determine the roles of the different proteolytically active subunits in antigen presentation and other cellular processes, highly specific inhibitors and activity-based probes that selectively target specific active sites are needed. In this work we present the development of fluorescent activity-based probes that selectively target the beta1 and beta5 sites of the constitutive proteasome.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Binding Sites
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Cells, Cultured
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Enzyme Inhibitors / chemistry
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Fluorescent Dyes / chemistry*
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Humans
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Models, Molecular
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Proteasome Endopeptidase Complex / chemistry
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Proteasome Endopeptidase Complex / metabolism*
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Proteasome Inhibitors
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Protein Subunits / antagonists & inhibitors
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Protein Subunits / chemistry*
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Protein Subunits / metabolism
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Substrate Specificity
Substances
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Enzyme Inhibitors
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Fluorescent Dyes
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Proteasome Inhibitors
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Protein Subunits
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Proteasome Endopeptidase Complex