Activity-Based Proteasome Profiling in Medicinal Chemistry and Chemical Biology

Gerjan De Bruin*, Nan Li, Guillem Paniagua, Lianne Willems, Bo Tao Xin, Martijn Verdoes, Paul P. Geurink, Wouter Van Der Linden, Mario van der Stelt, Gijs Van Der Marel, Herman S. Overkleeft, Bogdan I. Florea

*Corresponding author for this work

Research output: Chapter in Book/Report/Conference proceedingChapter


Activity-based protein profiling (ABPP) is a powerful technique to identify enzymatic activities and to study their functioning - and the effect of inhibitors on this - in vitro, in situ, and in vivo. In this chapter some case studies on activity-based profiling of mammalian proteasomes are discussed. Both direct and two-step bioorthogonal ABPP strategies and their merits are discussed, and the value of ABPP in the establishment of previously uncharted enzymatic activities and the direct visualization of inhibitor specificity are presented. Proteasomes are essential factors in the detection and eradication of virally infected cells. Besides their fundamental interest, proteasomes are relevant therapeutic targets. Proteasomes are useful targets in the development of chemical biology research strategies, and in return chemical biology approaches help in establishing proteasome activities in health and disease and in determining their relevance as drug targets.

Original languageEnglish
Title of host publicationConcepts and Case Studies in Chemical Biology
Number of pages14
ISBN (Electronic)9783527687503
ISBN (Print)9783527336111
Publication statusPublished - 6 Oct 2014


  • Activity-based proteasome profiling (ABPP)
  • Chemical biology
  • Medicinal chemistry

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