AI Article Synopsis
- The proteasome is a crucial enzyme involved in various regulatory processes, and the study introduces a new inhibitor called MV151 that specifically targets it.
- MV151 can be used to visualize proteasome activity in living cells and helps in comparing other proteasome inhibitors.
- This inhibitor shows promise for diverse applications, including studying proteasome functions in cells, profiling activity in clinical settings, and analyzing how different inhibitors affect specific proteasome subunits.
Article Abstract
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 determined by MV151 labeling. Administration of MV151 to mice allowed for in vivo labeling of proteasomes, which correlated with inhibition of proteasomal degradation in the affected tissues. This probe can be used for many applications ranging from clinical profiling of proteasome activity, to biochemical analysis of subunit specificity of inhibitors, and to cell biological analysis of the proteasome function and dynamics in living cells.
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| http://dx.doi.org/10.1016/j.chembiol.2006.09.013 | DOI Listing |
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