A practical fluorogenic substrate for high-throughput screening of glutathione S-transferase inhibitors

Yuuta Fujikawa; Fumika Morisaki; Asami Ogura; Kana Morohashi; Sora Enya; Ryusuke Niwa; Shinji Goto; Hirotatsu Kojima; Takayoshi Okabe; Tetsuo Nagano; Hideshi Inoue

doi:10.1039/C5CC02067K

A practical fluorogenic substrate for high-throughput screening of glutathione S-transferase inhibitors†

Yuuta Fujikawa,*^a Fumika Morisaki,^a Asami Ogura,^a Kana Morohashi,^b Sora Enya,^b Ryusuke Niwa,^bc Shinji Goto,^d Hirotatsu Kojima,^e Takayoshi Okabe,^e Tetsuo Nagano^e and Hideshi Inoue^a

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^a School of Life Sciences, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan
E-mail: yfuji@toyaku.ac.jp
Fax: +81-42-676-5391
Tel: +81-42-676-5391

^b Graduate School of Life and Environmental Sciences, University of Tsukuba, 1-1-1 Tennoudai, Tsukuba, Ibaraki 305-8572, Japan

^c PRESTO, JST, 4-1-8 Honcho Kawaguchi, Saitama 332-0012, Japan

^d Department of Stem Cell Biology, Atomic Bomb Disease Institute, Nagasaki University, 1-12-4 Sakamoto, Nagasaki 852-8523, Japan

^e Open, innovation Center for Drug Discovery, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan

Abstract

We report a new fluorogenic substrate for glutathione S-transferase (GST), 3,4-DNADCF, enabling the assay with a low level of nonenzymatic background reaction. Inhibitors against Noppera-bo/GSTe14 from Drosophila melanogaster were identified by high throughput screening using 3,4-DNADCF, demonstrating the utility of this substrate.

Chemical Communications

A practical fluorogenic substrate for high-throughput screening of glutathione S-transferase inhibitors†

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A practical fluorogenic substrate for high-throughput screening of glutathione S-transferase inhibitors

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