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Updated: Jan 23, 2026
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Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases
Published on: October 10, 2020
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A highly selective fluorogenic substrate for imaging glutathione S-transferase P1: development and cellular
Masaya Mori1, Yuuta Fujikawa, Manami Kikkawa
1School of Life Sciences, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo, 192-0392, Japan. yfuji@toyaku.ac.jp.
Chemical Communications (Cambridge, England)
|June 26, 2019
Summary
We developed a novel fluorogenic substrate, Ps-TG, and its derivative Ps-TAc, to specifically detect intracellular activity of pi-class glutathione S-transferase (GSTP1) in cancer cells. This tool aids in visualizing GSTP1 expression, a key marker in malignant tumors.
Area of Science:
- Biochemistry
- Molecular Biology
- Cancer Research
Background:
- Pi-class glutathione S-transferase (GSTP1) is a significant molecular marker.
- Altered GSTP1 expression is observed in various malignant tumor tissues.
Purpose of the Study:
- To develop a highly selective fluorogenic substrate for GSTP1.
- To enable specific visualization of intracellular GSTP1 activity in cancer cells.
- To facilitate the study of epigenetically regulated GSTP1 expression.
Main Methods:
- Design and synthesis of a novel fluorogenic substrate, Ps-TG.
- Development of a membrane-permeable derivative, Ps-TAc.
- Application of these probes for visualizing intracellular GSTP1 activity.
Main Results:
- Ps-TG identified as the first highly selective fluorogenic GSTP1 substrate.
- Ps-TAc demonstrated effective membrane permeability for intracellular visualization.
- Successful specific visualization of intracellular GSTP1 activity in cancer cells.
Conclusions:
- Ps-TG and Ps-TAc are valuable tools for detecting GSTP1 activity.
- These probes can aid in cancer cell research and the study of epigenetic regulation of GSTP1.
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