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Updated: Dec 12, 2025
Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases
Published on: October 10, 2020
Development of Telintra as an Inhibitor of Glutathione S-Transferase P
Jie Zhang1, Zhi-Wei Ye1, Yvonne Janssen-Heininger2
1Department of Cell and Molecular Pharmacology and Experimental Therapeutics, Medical University of South Carolina, Charleston, SC, USA.
Abstract:
Glutathione S-transferase P (GSTP) is a component of a complex series of pathways that provide cellular redox homeostasis. It is an abundant protein in certain tumors and is over-expressed in cancer drug resistance. It has diverse cellular functions that include, thiolase activities with small electrophilic agents or susceptible cysteine residues on the protein to mediate S-glutathionylation, and chaperone binding with select protein kinases. Preclinical and clinical testing of a nanomolar inhibitor of GSTP, TLK199 (Telintra; Ezatiostat) has indicated a role for the enzyme in hematopoiesis and utility for the drug in the treatment of patients with myelodysplastic syndrome.
Insights
Glutathione S-transferase P (GSTP) is crucial for cellular redox balance and cancer drug resistance. Inhibiting GSTP with TLK199 shows promise for treating myelodysplastic syndrome by impacting hematopoiesis.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Glutathione S-transferase P (GSTP) regulates cellular redox homeostasis.
- GSTP is over-expressed in tumors, contributing to cancer drug resistance.
- GSTP possesses diverse functions, including thiolase activity and protein kinase interactions.
Purpose of the Study:
- To investigate the role of GSTP in cellular pathways.
- To evaluate the therapeutic potential of GSTP inhibition in myelodysplastic syndrome.
Main Methods:
- Preclinical and clinical testing of TLK199 (Ezatiostat), a nanomolar inhibitor of GSTP.
- Analysis of GSTP's enzymatic and chaperone activities.
Main Results:
- TLK199 demonstrated nanomolar inhibition of GSTP.
- Evidence suggests GSTP plays a role in hematopoiesis.
- The drug showed utility in treating myelodysplastic syndrome.
Conclusions:
- GSTP is a significant target for therapeutic intervention.
- Inhibiting GSTP with TLK199 offers a potential treatment strategy for myelodysplastic syndrome.
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