Issue 12, 2010

A panel of subunit-selective activity-based proteasome probes

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 β1 and β5 sites of the constitutive proteasome.

Graphical abstract: A panel of subunit-selective activity-based proteasome probes

Supplementary files

Article information

Article type
Paper
Submitted
15 Jan 2010
Accepted
09 Apr 2010
First published
06 May 2010

Org. Biomol. Chem., 2010,8, 2719-2727

A panel of subunit-selective activity-based proteasome probes

M. Verdoes, L. I. Willems, W. A. van der Linden, B. A. Duivenvoorden, G. A. van der Marel, B. I. Florea, A. F. Kisselev and H. S. Overkleeft, Org. Biomol. Chem., 2010, 8, 2719 DOI: 10.1039/C001036G

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