Issue 8, 2010
From the journal:

Organic & Biomolecular Chemistry

Proteasome selectivity towards Michael acceptor containing oligopeptide-based inhibitors†‡

Wouter A. van der Linden,a   Paul P. Geurink,a   Chris Oskam,a   Gijsbert A. van der Marel,a   Bogdan I. Floreaa  and  Herman S. Overkleeft*a  

* Corresponding authors

a Leiden Institute of Chemistry and Netherlands Proteomics Centre, P.O. Box 9502, Leiden, The Netherlands
E-mail: h.s.overkleeft@chem.leidenuniv.nl
Fax: +31-71-5274307
Tel: +31-71-5274342

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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Article information

DOI
https://doi.org/10.1039/B924134E
Article type
Paper
Submitted
18 Nov 2009
Accepted
08 Feb 2010
First published
25 Feb 2010

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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