A fluorescent broad-spectrum proteasome inhibitor for labeling proteasomes in vitro and in vivo.

  title={A fluorescent broad-spectrum proteasome inhibitor for labeling proteasomes in vitro and in vivo.},
  author={Martijn Verdoes and Bogdan I Florea and Victoria Men{\'e}ndez-Benito and Christa J. Maynard and Martin D Witte and Wouter A. van der Linden and Adrianus M. C. H. van den Nieuwendijk and Tanja N Hofmann and Celia R Berkers and Fijs W. B. van Leeuwen and Tom A.M. Groothuis and Michiel A. Leeuwenburgh and Huib Ovaa and Jacques Neefjes and Dmitri V. Filippov and Gijs A. van Der Marel and Nico P Dantuma and Herman S Overkleeft},
  journal={Chemistry & biology},
  volume={13 11},
The proteasome is an essential evolutionary conserved protease involved in many regulatory systems. Here, we describe the synthesis and characterization of the activity-based, fluorescent, and cell-permeable inhibitor Bodipy TMR-Ahx(3)L(3)VS (MV151), which specifically targets all active subunits of the proteasome and immunoproteasome in living cells, allowing for rapid and sensitive in-gel detection. The inhibition profile of a panel of commonly used proteasome inhibitors could be readily… CONTINUE READING
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