A panel of subunit-selective activity-based proteasome probes

作者:Verdoes Martijn; Willems Lianne I; van der Linden Wouter A; Duivenvoorden Boudewijn A; van der Marel Gij**ert A; Florea Bogdan I; Kisselev Alexei F*; Overkleeft Herman S
来源:Organic and Biomolecular Chemistry, 2010, 8(12): 2719-2727.
DOI:10.1039/c001036g

摘要

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 beta 1 and beta 5 sites of the constitutive proteasome.

  • 出版日期2010-6-21