4.6 Article

A panel of subunit-selective activity-based proteasome probes

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 8, Issue 12, Pages 2719-2727

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c001036g

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Funding

  1. Netherlands Organization for Scientific Research (NWO)
  2. Netherlands Genomics Centre Initiative (NGI)
  3. NCI [RO1CA124634]

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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.

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