A panel of subunit-selective activity-based proteasome probes

一组基于亚基选择性活性的蛋白酶体探针

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作者:Martijn Verdoes, Lianne I Willems, Wouter A van der Linden, Boudewijn A Duivenvoorden, Gijsbert A van der Marel, Bogdan I Florea, Alexei F Kisselev, Herman S Overkleeft

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.

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