Enzymes involved in the bioconversion of ester-based prodrugs

J Pharm Sci. 2006 Jun;95(6):1177-95. doi: 10.1002/jps.20542.


Enzymes are essential for the activation of many prodrugs. In this review, the most important enzymes (e.g., paraoxonase, carboxylesterase, acetylcholinesterase, cholinesterase) involved in the bioconversion of ester-based prodrugs will be discussed in terms of their biology and biochemistry. Most of these enzymes fall into the category of hydrolytic enzymes. However, nonhydrolytic enzymes, including cytochrome P450s, can also catalyze the bioconversion of ester prodrugs and thus will be discussed here. Other factors influencing the ability of these enzymes to catalyze the bioconversion of ester-based prodrugs, particularly species and interindividual differences and stereochemical and structural features of the prodrugs, will be discussed.

Publication types

  • Review

MeSH terms

  • Animals
  • Cytochrome P-450 Enzyme System / genetics
  • Cytochrome P-450 Enzyme System / metabolism
  • Enzyme Activation
  • Enzymes / genetics
  • Enzymes / metabolism*
  • Esterases / genetics
  • Esterases / metabolism
  • Esters
  • Hydrolases / metabolism
  • Prodrugs / chemistry
  • Prodrugs / metabolism*
  • Species Specificity
  • Structure-Activity Relationship


  • Enzymes
  • Esters
  • Prodrugs
  • Cytochrome P-450 Enzyme System
  • Hydrolases
  • Esterases