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Day 3, June 12(Wed.) Room P1 (Multipurpose Hall)・Room P2 (Conference Room 101+102)
- 3P-15
Evaluation Method for Inhibitors of Enzyme Activity Using Substrate Specificity of Aldo-Keto Reductase by LC-MS
(1Mukogawa Women's Univ., 2Kobe Pharm. Univ., 3ORIST)
Chihiro Fukuda1, oShizuyo Horiyama1, Fumiko Hara1, Shinya Takada1, Masayori Hagimori1, Shihoko Sano2, Hirofumi Sato3, Motohiro Shizuma3
The human aldo-keto reductase (AKR) superfamily plays an important role in a variety of biological functions. However, it is also associated with diseases such as diabetic neuropathy and breast cancer, so that these AKRs are a therapeutic target enzyme for these diseases. Unfortunately, due to the high homology of the AKR family, inhibiting only the target enzyme is not possible, resulting in side effects. In this study, we focused on AKR1B1 and AKR1B10, enzymes known to be involved in diseases such as diabetic neuropathy and breast cancer, and glutathione-conjugated carbonyl compounds (GSH-CA) were synthesized with substrate specificity for these enzymes. The study evaluates the inhibitory effect of AKR1B1 or AKR1B10 selective inhibitors on the enzyme activity using this substrate by LC/MS method.