Aldehyde Dehydrogenase Inhibitors for Cancer Therapeutics

Trends Pharmacol Sci. 2019 Oct;40(10):774-789. doi: 10.1016/ Epub 2019 Sep 9.


Aldehyde dehydrogenases (ALDHs) are highly expressed in the chemotherapy- and radiotherapy-resistant cell subpopulations of many different cancer types. Accordingly, the development of ALDH inhibitors may be the most direct approach to target these cell populations. However, inhibiting multiple ALDH family members can be toxic and isoform-specific inhibition is often ineffective. This review discusses the role of ALDH in cancer and therapy resistance, and then overviews the various available ALDH inhibitors with a focus on the clinical potential and limitations of these agents as cancer therapeutics. Finally, challenges and future research directions to effectively target ALDH in the management of cancer therapy resistance are discussed.

Keywords: aldehyde dehydrogenase; cancer pharmacology; cancer resistance; cancer stem cells; cancer therapy; targeted inhibitors.

Publication types

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

MeSH terms

  • Aldehyde Dehydrogenase / antagonists & inhibitors*
  • Aldehyde Dehydrogenase / metabolism
  • Animals
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / therapeutic use
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology*


  • Enzyme Inhibitors
  • Aldehyde Dehydrogenase