Chemistry in living cells: Detection of active proteasomes by a two-step labeling strategy

Huib Ovaa, Paul F. Van Swieten, Benedikt M. Kessler, Michiel A. Leeuwenburgh, Edda Fiebiger, Adrianus M.C.H. Van den Nieuwendijk, Paul J. Galardy, Gijsbert A. Van der Marel, Hidde L. Ploegh, Herman S. Overkleeft

Research output: Contribution to journalArticle

128 Scopus citations

Abstract

In vivo targeting of the proteasome: Probe 1 is a cell-permeable irreversible inhibitor that alkylates the active-site residues of the proteasome in a Michael fashion. After cell lysis, a biotin moiety is introduced by Staudinger ligation to yield construct 2. This strategy allows activity profiling of the catalytic activities of the proteasome in vivo.

Original languageEnglish (US)
Pages (from-to)3626-3629
Number of pages4
JournalAngewandte Chemie - International Edition
Volume42
Issue number31
DOIs
StatePublished - Aug 11 2003

Keywords

  • Bioorganic chemistry
  • Inhibitors
  • Peptides
  • Proteomics
  • Solid-phase synthesis

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)

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    Ovaa, H., Van Swieten, P. F., Kessler, B. M., Leeuwenburgh, M. A., Fiebiger, E., Van den Nieuwendijk, A. M. C. H., Galardy, P. J., Van der Marel, G. A., Ploegh, H. L., & Overkleeft, H. S. (2003). Chemistry in living cells: Detection of active proteasomes by a two-step labeling strategy. Angewandte Chemie - International Edition, 42(31), 3626-3629. https://doi.org/10.1002/anie.200351314