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

doi:10.1002/9783527687503.ch12

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

Chemistry

Research output: Chapter in Book/Report/Conference proceeding › Chapter

Abstract

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 language	English
Title of host publication	Concepts and Case Studies in Chemical Biology
Publisher	Wiley-Blackwell
Pages	177-190
Number of pages	14
ISBN (Electronic)	9783527687503
ISBN (Print)	9783527336111
DOIs	https://doi.org/10.1002/9783527687503.ch12
Publication status	Published - 6 Oct 2014

Keywords

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

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10.1002/9783527687503.ch12

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De Bruin, G., Li, N., Paniagua, G., Willems, L., Xin, B. T., Verdoes, M., Geurink, P. P., Van Der Linden, W., van der Stelt, M., Van Der Marel, G., Overkleeft, H. S., & Florea, B. I. (2014). Activity-Based Proteasome Profiling in Medicinal Chemistry and Chemical Biology. In Concepts and Case Studies in Chemical Biology (pp. 177-190). Wiley-Blackwell. https://doi.org/10.1002/9783527687503.ch12

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abstract = "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.",

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

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doi = "10.1002/9783527687503.ch12",

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De Bruin, G, Li, N, Paniagua, G, Willems, L, Xin, BT, Verdoes, M, Geurink, PP, Van Der Linden, W, van der Stelt, M, Van Der Marel, G, Overkleeft, HS & Florea, BI 2014, Activity-Based Proteasome Profiling in Medicinal Chemistry and Chemical Biology. in Concepts and Case Studies in Chemical Biology. Wiley-Blackwell, pp. 177-190. https://doi.org/10.1002/9783527687503.ch12

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AU - Li, Nan

AU - Paniagua, Guillem

AU - Willems, Lianne

AU - Xin, Bo Tao

AU - Verdoes, Martijn

AU - Geurink, Paul P.

AU - Van Der Linden, Wouter

AU - van der Stelt, Mario

AU - Van Der Marel, Gijs

AU - Overkleeft, Herman S.

AU - Florea, Bogdan I.

PY - 2014/10/6

Y1 - 2014/10/6

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AB - 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.

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BT - Concepts and Case Studies in Chemical Biology

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ER -

Activity-Based Proteasome Profiling in Medicinal Chemistry and Chemical Biology

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Keywords

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