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Updated: Feb 23, 2026

Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases
Published on: October 10, 2020
A covalent G-site inhibitor for glutathione S-transferase Pi (GSTP1-1)
Yuko Shishido1, Fumiaki Tomoike, Yasuaki Kimura
1Department of Chemistry, Graduate School of Science, Nagoya University, Furo-cho, Chikusa-Ku, Nagoya, 464-8602, Japan. h-abe@chem.nagoya-u.ac.jp.
Abstract:
We herein report the first covalent G-site-binding inhibitor for GST, GS-ESF (1), which irreversibly inhibited the GSTP1-1 function. LC-MS/MS and X-ray structure analyses of the covalently linked GST-inhibitor complex suggested that 1 reacted with Tyr108 of GSTP1-1. The mechanism of covalent bond formation was discussed based on MD simulation results.
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