Glutathione conjugates and their synthetic derivatives as inhibitors of glutathione-dependent enzymes involved in cancer and drug resistance

Drug Metab Rev. 2002 Nov;34(4):821-63. doi: 10.1081/dmr-120015695.


Alterations in levels of glutathione (GSH) and glutathione-dependent enzymes have been implicated in cancer and multidrug resistance of tumor cells. The activity of a number of these, the multidrug resistance-associated protein 1, glutathione S-transferase, DNA-dependent protein kinase, glyoxalase I, and gamma-glutamyl transpeptidase, can be inhibited by GSH-conjugates and synthetic analogs thereof. In this review we focus on the function of these enzymes and carriers in cancer and anti-cancer drug resistance, in relation to their inhibition by GSH-conjugate analogs.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Resistance, Neoplasm / physiology*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / metabolism*
  • Enzyme Inhibitors / pharmacology
  • Enzyme Inhibitors / therapeutic use
  • Glutathione / antagonists & inhibitors
  • Glutathione / metabolism*
  • Humans
  • Neoplasms / drug therapy
  • Neoplasms / enzymology*


  • Enzyme Inhibitors
  • Glutathione