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J Med Chem. 2013 Mar 28;56(6):2165-77. doi: 10.1021/jm301420b. Epub 2013 Mar 1.

Exploring a new frontier in cancer treatment: targeting the ubiquitin and ubiquitin-like activating enzymes.

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  • 1Department of Chemical and Physical Sciences, University of Toronto Mississauga , 3359 Mississauga Road North, Mississauga, Ontario L5L 1C6, Canada.


The labeling of proteins with small ubiquitin (Ub) and ubiquitin-like (Ubl) modifiers regulates a plethora of activities within the cell, such as protein recycling, cell cycle modifications, and protein translocation. These processes are often overactive in diseased cells, leading to unregulated cell growth and disease progression. Therefore, in systems where Ub/Ubl protein labeling is dysregulated, the development of drugs to selectively and potently disrupt Ub/Ubl protein labeling offers a targeted molecular approach for sensitizing these diseased cells. This Perspective outlines the progress that has been made in the context of inhibitor development for targeting Ub/Ubl pathways.

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