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Glutathione Transferases: Potential Targets to Overcome Chemoresistance in Solid Tumors

Marija Pljesa-Ercegovac1,2, Ana Savic-Radojevic3,4, Marija Matic5,6

  • 1Institute of Medical and Clinical Biochemistry, Faculty of Medicine, University of Belgrade, 11 000 Belgrade, Serbia. m.pljesa.ercegovac@gmail.com.

International Journal of Molecular Sciences
|November 30, 2018
PubMed

Insights

Glutathione transferases (GSTs) are key in cancer chemoresistance. Targeting these enzymes with specific inhibitors or pro-drugs offers a promising strategy for novel cancer therapies.

Area of Science:

  • Biochemistry
  • Oncology
  • Pharmacology

Background:

  • Multifunctional enzymes glutathione transferases (GSTs) play a critical role in the development of chemoresistance in cancer.
  • Their polymorphic nature and substrate promiscuity enable detoxification of chemotherapeutics and regulation of cell signaling pathways involved in proliferation and apoptosis.
  • Distinct GST expression profiles across cancer types offer opportunities for targeted therapeutic strategies.

Purpose of the Study:

  • To explore the potential of glutathione transferases (GSTs) as therapeutic targets in cancer treatment.
  • To review the application of GST isoenzyme-specific inhibitors and pro-drugs for selective cancer therapy.
  • To discuss the development of novel GST-targeted drugs for overcoming chemoresistance.

Main Methods:

  • Review of existing literature on glutathione transferases (GSTs) in cancer chemoresistance.
  • Analysis of current clinical trials involving GST inhibitors.
  • Examination of strategies for GST-targeted pro-drug bio-activation and development.

Main Results:

  • Certain GST inhibitors are currently undergoing clinical trials.
  • GST isoenzymes can be utilized for targeted bio-activation of specific pro-drugs, enhancing accumulation in cancer cells.
  • Development of GST pro-drugs, derived from conventional anti-cancer agents, is a novel approach for solid tumor treatment.

Conclusions:

  • Glutathione transferases (GSTs) represent a promising target for novel cancer therapies due to their role in chemoresistance.
  • Targeted inhibition or bio-activation strategies exploiting GST isoenzyme specificity can enhance therapeutic efficacy and reduce side effects.
  • Future drug design should focus on selectively targeting GST-overexpressing cancers to combat chemoresistance and minimize off-target toxicity.
Keywords:
chemoresistanceglutathione transferasesinhibitorspro-drugsprotein-protein interaction

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