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Updated: Jun 12, 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 and development of new principles to overcome drug resistance

Andrea Sau1, Francesca Pellizzari Tregno, Francesco Valentino

  • 1Department of Chemical Sciences and Technologies, University of "Tor Vergata", Rome, Italy.

Archives of Biochemistry and Biophysics
|May 25, 2010
PubMed

Insights

Multidrug resistance in cancer involves drug efflux pumps and glutathione S-transferases (GSTs). Targeting GSTs with inhibitors or pro-drugs offers strategies to enhance anticancer drug efficacy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Chemoresistance, a complex trait in cancer, is often associated with the coordinated upregulation of efflux transporters and phase II conjugating enzymes in tumor cells, leading to the multidrug resistance (MDR) phenotype.
  • Overexpression of glutathione S-transferases (GSTs) and efflux pumps in tumors can significantly diminish the therapeutic effectiveness of various anticancer drugs.
  • Emerging evidence highlights the role of GSTs beyond detoxification, implicating them in the regulation of apoptosis via inhibition of the JNK signaling pathway.

Purpose of the Study:

  • To provide a comprehensive overview of strategies aimed at overcoming chemoresistance.
  • To focus on the role of glutathione S-transferases (GSTs) in the development of multidrug resistance.
  • To review current research on GST inhibitors and GST-activated prodrugs as potential anticancer agents.

Main Methods:

  • Literature review of studies investigating chemoresistance mechanisms.
  • Analysis of the role of efflux transporter proteins and phase II conjugating enzymes, particularly GSTs.
  • Examination of research on GST inhibitors and GST-activated prodrugs.

Main Results:

  • Coordinated expression of efflux transporters and GSTs is linked to the multidrug resistance phenotype.
  • GSTs are implicated in the inhibition of the JNK signaling pathway, influencing apoptosis.
  • GST inhibitors and GST-activated prodrugs are being explored as therapeutic approaches.

Conclusions:

  • The glutathione S-transferase (GST) superfamily represents a promising target for developing novel anticancer therapies.
  • Modulating GST activity through inhibitors or prodrugs may offer a viable strategy to circumvent drug resistance.
  • Further pharmaceutical research into GST-targeted agents is warranted to improve the efficacy of cancer treatment.

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