Issue 81, 2017
From the journal:

Chemical Communications

A covalent G-site inhibitor for glutathione S-transferase Pi (GSTP1-1)†

Yuko Shishido,ab   Fumiaki Tomoike, ORCID logo a   Yasuaki Kimura, ORCID logo a   Keiko Kuwata,c   Takato Yano,d   Kenji Fukui,d   Haruka Fujikawa,a   Yoshitaka Sekido,e   Yuko Murakami-Tonami,e   Tomoshi Kameda,f   Satoshi Shutob  and  Hiroshi Abe ORCID logo *a  

* Corresponding authors

a Department of Chemistry, Graduate School of Science, Nagoya University, Furo-cho, Chikusa-Ku, Nagoya, Japan
E-mail: h-abe@chem.nagoya-u.ac.jp

b Faculty of Pharmaceutical Science, Hokkaido University, Kita-12, Nishi-6, Kita-Ku, Sapporo, Japan

c Institute of Transformative Bio-Molecules (WPI-ITbM), Nagoya University, Furo-cho, Chikusa-Ku, Nagoya, Japan

d Department of Biochemistry, Osaka Medical College, 2-7, Daigakumachi, Takatsuki, Osaka, Japan

e Division of Molecular Oncology, Aichi Cancer Center Research Institute, 1-1, Kanokoden, Chikusa-Ku, Nagoya, Japan

f Artificial Intelligence Research Center, National Institute of Advanced Industrial Science and Technology, 2-4-7, Aomi, Koutou-ku, Tokyo, Japan

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.

Graphical abstract: A covalent G-site inhibitor for glutathione S-transferase Pi (GSTP1-1)

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Article information

DOI
https://doi.org/10.1039/C7CC05829B
Article type
Communication
Submitted
26 Jul 2017
Accepted
19 Aug 2017
First published
21 Aug 2017

Chem. Commun., 2017,53, 11138-11141

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A covalent G-site inhibitor for glutathione S-transferase Pi (GSTP1-1)

Y. Shishido, F. Tomoike, Y. Kimura, K. Kuwata, T. Yano, K. Fukui, H. Fujikawa, Y. Sekido, Y. Murakami-Tonami, T. Kameda, S. Shuto and H. Abe, Chem. Commun., 2017, 53, 11138 DOI: 10.1039/C7CC05829B

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