4.8 Review

Protease-Activated Drug Development

Journal

THERANOSTICS
Volume 2, Issue 2, Pages 156-178

Publisher

IVYSPRING INT PUBL
DOI: 10.7150/thno.4068

Keywords

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

Funding

  1. National Institutes of Biomedical Imaging and Bioengineering (NIBIB), National Institutes of Health (NIH)
  2. NIH [K99/R00]

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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.

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