Enzymes and Targeted Activation of Prodrugs

Yanhui Yang, Yu Chen, Herve Aloysius, Daigo Inoyama, Longqin Hu

Research output: Chapter in Book/Report/Conference proceedingChapter


Currently, 5-7% of the drugs approved worldwide can be classified as prodrugs, and approximately 15% of all new drugs approved each year were prodrugs. Activation of prodrugs can involve many endogenous enzymes including CYP450, DT-diaphorase, tyrosinase, CE, and P-glucuronidase. Exogenous enzymes can also be used to activate prodrugs as in antibody-directed enzyme prodrug therapy (ADEPT), gene-directed enzyme prodrug therapy (GDEPT), virus-directed enzyme prodrug therapy (VDEPT), and polymer-directed enzyme prodrug therapy (PDEPT). This chapter provides an overview of the enzymes used in prodrug activation with emphasis to their structure, distribution, and mechanism of activation for typical prodrugs. There are a wide variety of enzymes (primarily from bacterial sources), such as carboxypeptidase G2 (CPG2), ß-glucuronidase, and nitroreductase (NTR), that have been used in ADEPT, GDEPT, and VDEPT approaches.

Original languageEnglish (US)
Title of host publicationEnzyme Technologies
Subtitle of host publicationPluripotent Players in Discovering Therapeutic Agent
Number of pages73
ISBN (Electronic)9781118739907
ISBN (Print)9780470286265
StatePublished - Dec 9 2013

All Science Journal Classification (ASJC) codes

  • Biochemistry, Genetics and Molecular Biology(all)


  • Antibody-directed enzyme prodrug therapy (ADEPT)
  • Endogenous enzymes
  • Enzymes
  • Gene-directed enzyme prodrug therapy (GDEPT)
  • Nonendogenous enzymes
  • Prodrugs


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