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Updated: Nov 6, 2025

Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases
Published on: October 10, 2020
Glutathione S-Transferases in Cancer
Rahul Raj Singh1, Katie M Reindl1
1Department of Biological Sciences, North Dakota State University, Fargo, ND 58108, USA.
Abstract:
In humans, the glutathione S-transferases (GST) protein family is composed of seven members that present remarkable structural similarity and some degree of overlapping functionalities. GST proteins are crucial antioxidant enzymes that regulate stress-induced signaling pathways. Interestingly, overactive GST proteins are a frequent feature of many human cancers. Recent evidence has revealed that the biology of most GST proteins is complex and multifaceted and that these proteins actively participate in tumorigenic processes such as cell survival, cell proliferation, and drug resistance. Structural and pharmacological studies have identified various GST inhibitors, and these molecules have progressed to clinical trials for the treatment of cancer and other diseases. In this review, we discuss recent findings in GST protein biology and their roles in cancer development, their contribution in chemoresistance, and the development of GST inhibitors for cancer treatment.
Insights
Glutathione S-transferases (GST) are key antioxidant enzymes implicated in cancer development and drug resistance. This review explores GSTs
Area of Science:
- Biochemistry and Molecular Biology
- Oncology
- Pharmacology
Background:
- Glutathione S-transferases (GSTs) are a family of crucial antioxidant enzymes in humans.
- These enzymes regulate stress-induced signaling pathways and are often overactive in cancers.
- GSTs play complex roles in tumorigenesis, including promoting cell survival, proliferation, and drug resistance.
Purpose of the Study:
- To review recent findings on GST protein biology in cancer.
- To discuss the role of GSTs in cancer development and chemoresistance.
- To highlight the development of GST inhibitors for cancer therapy.
Main Methods:
- Literature review of recent studies on GSTs in cancer.
- Analysis of structural and pharmacological data for GST inhibitors.
- Synthesis of information on GSTs' roles in tumorigenesis and drug resistance.
Main Results:
- GST proteins are actively involved in key tumorigenic processes.
- Overactive GSTs are frequently observed in various human cancers.
- Numerous GST inhibitors have been identified and advanced to clinical trials.
Conclusions:
- GSTs are multifaceted proteins with significant roles in cancer progression.
- Targeting GSTs with inhibitors presents a promising therapeutic strategy for cancer treatment.
- Further research into GST biology and inhibitor development is warranted.
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