title: A practical fluorogenic substrate for high-throughput screening of glutathione S-transferase inhibitors.
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.
authors.affiliation: School of Life Sciences, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan. yfuji@toyaku.ac.jp.
authors.forename: Yuuta
authors.initials: Y
authors.lastname: Fujikawa
authors.forename: Fumika
authors.initials: F
authors.lastname: Morisaki
authors.forename: Asami
authors.initials: A
authors.lastname: Ogura
authors.forename: Kana
authors.initials: K
authors.lastname: Morohashi
authors.forename: Sora
authors.initials: S
authors.lastname: Enya
authors.forename: Ryusuke
authors.initials: R
authors.lastname: Niwa
authors.forename: Shinji
authors.initials: S
authors.lastname: Goto
authors.forename: Hirotatsu
authors.initials: H
authors.lastname: Kojima
authors.forename: Takayoshi
authors.initials: T
authors.lastname: Okabe
authors.forename: Tetsuo
authors.initials: T
authors.lastname: Nagano
authors.forename: Hideshi
authors.initials: H
authors.lastname: Inoue
mesh_terms: D000818:Animals; D029721:Drosophila Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004331:Drosophila melanogaster / Q000201:enzymology*; D004353:Drug Evaluation, Preclinical; D057075:Enzyme Assays; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005456:Fluorescent Dyes / Q000737:chemistry / Q000378:metabolism*; D005978:Glutathione / Q000737:chemistry / Q000378:metabolism; D005982:Glutathione Transferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D057166:High-Throughput Screening Assays; D006801:Humans; D013050:Spectrometry, Fluorescence; D013379:Substrate Specificity
chemical_list: D029721:Drosophila Proteins; D004791:Enzyme Inhibitors; D005456:Fluorescent Dyes; D005982:Glutathione Transferase; C000602619:Gste14 protein, Drosophila; D005978:Glutathione