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Issue 8, 2010
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Proteasome selectivity towards Michael acceptor containing oligopeptide-based inhibitors

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Abstract

The synthesis and biological evaluation of ten Michael acceptors containing potential proteasome inhibitors are described. Cellular targets of azide containing inhibitors Ib and VIIIb 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-MS2 identification. This strategy appears to be an attractive alternative to gel-based competition assays.

Graphical abstract: Proteasome selectivity towards Michael acceptor containing oligopeptide-based inhibitors

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Publication details

The article was received on 18 Nov 2009, accepted on 08 Feb 2010 and first published on 25 Feb 2010


Article type: Paper
DOI: 10.1039/B924134E
Citation: Org. Biomol. Chem., 2010,8, 1885-1893

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    Proteasome selectivity towards Michael acceptor containing oligopeptide-based inhibitors

    W. A. van der Linden, P. P. Geurink, C. Oskam, G. A. van der Marel, B. I. Florea and H. S. Overkleeft, Org. Biomol. Chem., 2010, 8, 1885
    DOI: 10.1039/B924134E

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