Chemistry in Living Cells: Detection of Active Proteasomes by a Two??Step Labeling Strategy

…, BM Kessler, MA Leeuwenburgh, E Fiebiger…

Index: Ovaa, Huib; Van Swieten, Paul F.; Kessler, Benedikt M.; Leeuwenburgh, Michiel A.; Fiebiger, Edda; Van den Nieuwendijk, Adrianus M. C. H.; Galardy, Paul J.; Van der Marel, Gijsbert A.; Ploegh, Hidde L.; Overkleeft, Herman S. Angewandte Chemie - International Edition, 2003 , vol. 42, # 31 p. 3626 - 3629

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Citation Number: 162

Abstract

Herein we describe a new functional-proteomics strategy that allows two-step labeling of the catalytically active subunits of the proteasome in living cells. The proteasome is a multi- catalytic proteinase that accounts for the bulk of cytosolic and nuclear proteolysis. We have previously reported the development of a set of extended, peptidebased, irreversible proteasome inhibitors.[6] The most potent of these, AdaAhx3L3VS 1 (Scheme 1), is unique ...