Protease-activated drug development

Ki Young Choi, Magdalena Swierczewska, Seulki Lee, Xiaoyuan Chen

Research output: Contribution to journalReview articlepeer-review

165 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)156-179
Number of pages24
Issue number2
StatePublished - 2012
Externally publishedYes


  • Activatable probe
  • Alzheimer's disease
  • Aspartyl protease
  • Cancer
  • Caspase
  • Cathepsin
  • Kallikrein
  • MMP
  • PSA
  • Protease
  • Serine protease

ASJC Scopus subject areas

  • Medicine (miscellaneous)
  • Pharmacology, Toxicology and Pharmaceutics (miscellaneous)


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