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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 beta1 and beta5 sites of the constitutive proteasome.

SUBMITTER: Verdoes M

PROVIDER: S-EPMC3042124 | biostudies-literature | 2010 Jun

REPOSITORIES: biostudies-literature

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A panel of subunit-selective activity-based proteasome probes.

Verdoes Martijn M Willems Lianne I LI van der Linden Wouter A WA Duivenvoorden Boudewijn A BA van der Marel Gijsbert A GA Florea Bogdan I BI Kisselev Alexei F AF Overkleeft Herman S HS

Organic & biomolecular chemistry 20100506 12

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. ...[more]

PMID: 20449511

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