The aldo-keto reductase superfamily and its role in drug metabolism and detoxification

Drug Metab Rev. 2008;40(4):553-624. doi: 10.1080/03602530802431439.


The aldo-keto reductase (AKR) superfamily comprises enzymes that catalyze redox transformations involved in biosynthesis, intermediary metabolism, and detoxification. Substrates of AKRs include glucose, steroids, glycosylation end-products, lipid peroxidation products, and environmental pollutants. These proteins adopt a (beta/alpha)(8) barrel structural motif interrupted by a number of extraneous loops and helixes that vary between proteins and bring structural identity to individual families. The human AKR family differs from the rodent families. Due to their broad substrate specificity, AKRs play an important role in the phase II detoxification of a large number of pharmaceuticals, drugs, and xenobiotics.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Alcohol Oxidoreductases / chemistry*
  • Alcohol Oxidoreductases / genetics
  • Alcohol Oxidoreductases / physiology*
  • Aldehyde Reductase
  • Aldo-Keto Reductases
  • Animals
  • Humans
  • Inactivation, Metabolic / genetics
  • Inactivation, Metabolic / physiology
  • Pharmaceutical Preparations / chemistry*
  • Pharmaceutical Preparations / metabolism*
  • Protein Structure, Secondary / drug effects
  • Protein Structure, Secondary / genetics
  • Protein Structure, Secondary / physiology


  • Pharmaceutical Preparations
  • Alcohol Oxidoreductases
  • Aldo-Keto Reductases
  • Aldehyde Reductase