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Theranostics. 2012;2(2):156-78. doi: 10.7150/thno.4068. Epub 2012 Feb 8.

Protease-activated drug development.

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1. Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineering (NIBIB), National Institutes of Health (NIH), Bethesda, Maryland, 20892, USA.


In this extensive review, we elucidate the importance of proteases and their role in drug development in various diseases with an emphasis on cancer. First, key proteases are introduced along with their function in disease progression. Next, we link these proteases as targets for the development of prodrugs and provide clinical examples of protease-activatable prodrugs. Finally, we provide significant design considerations needed for the development of the next generation protease-targeted and protease-activatable prodrugs.


Alzheimer's disease; MMP; PSA; Protease; activatable probe; aspartyl protease; cancer; caspase; cathepsin; kallikrein; serine protease

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