Carbonic anhydrases: novel therapeutic applications for inhibitors and activators

Nat Rev Drug Discov. 2008 Feb;7(2):168-81. doi: 10.1038/nrd2467.


Carbonic anhydrases (CAs), a group of ubiquitously expressed metalloenzymes, are involved in numerous physiological and pathological processes, including gluconeogenesis, lipogenesis, ureagenesis, tumorigenicity and the growth and virulence of various pathogens. In addition to the established role of CA inhibitors (CAIs) as diuretics and antiglaucoma drugs, it has recently emerged that CAIs could have potential as novel anti-obesity, anticancer and anti-infective drugs. Furthermore, recent studies suggest that CA activation may provide a novel therapy for Alzheimer's disease. This article discusses the biological rationale for the novel uses of inhibitors or activators of CA activity in multiple diseases, and highlights progress in the development of specific modulators of the relevant CA isoforms, some of which are now being evaluated in clinical trials.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Carbonic Anhydrase Inhibitors / pharmacology
  • Carbonic Anhydrase Inhibitors / therapeutic use*
  • Carbonic Anhydrases / chemistry
  • Carbonic Anhydrases / metabolism*
  • Drug Design
  • Humans
  • Isoenzymes
  • Models, Molecular
  • Molecular Structure
  • Structure-Activity Relationship


  • Carbonic Anhydrase Inhibitors
  • Isoenzymes
  • Carbonic Anhydrases