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Updated: Jun 22, 2026

Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases
14:57

Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases

Published on: October 10, 2020

Glutathione transferases as targets for cancer therapy

Paolo Ruzza1, Antonio Rosato, Carlo Riccardo Rossi

  • 1Institute of Biomolecular Chemistry of CNR, Padova, Italy. paolo.ruzza@unipd.it

Anti-Cancer Agents in Medicinal Chemistry
|June 23, 2009
PubMed

Insights

Glutathione transferases (GSTs) inactivate anticancer drugs and promote drug resistance. This review covers GST inhibitors and prodrugs, offering insights into targeting these proteins for cancer therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Cytosolic glutathione transferases (GSTs) are involved in detoxifying electrophilic anticancer agents.
  • Some GSTs, particularly GSTP1-1, are implicated in cellular apoptosis modulation and anticancer drug resistance.
  • Tumor overexpression of GSTs necessitates strategies to overcome resistance, such as GST inhibitors and prodrugs.

Purpose of the Study:

  • To review the current structural and pharmacological knowledge of GST-targeting compounds.
  • To explore the dual role of GSTs in anticancer drug inactivation and resistance modulation.
  • To discuss the therapeutic potential of inhibiting GSTs or utilizing GST-activated prodrugs.

Main Methods:

  • Literature review of structural and pharmacological data on GST-targeting compounds.
  • Analysis of the role of GSTs in drug metabolism and resistance mechanisms.
  • Synthesis of information on GST inhibitors and GST-activated prodrugs.

Main Results:

  • GSTs catalyze the inactivation of anticancer drugs through glutathione conjugation.
  • Overexpression of specific GSTs, like GSTP1-1, correlates with resistance to various anticancer agents.
  • GSTs can negatively modulate stress/drug-induced apoptosis via kinase interactions.

Conclusions:

  • GSTs represent a significant challenge in cancer chemotherapy due to their role in drug resistance.
  • Targeting GSTs with specific inhibitors or prodrugs is a promising strategy to enhance anticancer drug efficacy.
  • Further research into the structural and pharmacological properties of GST-targeting compounds is warranted.

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