Poster Presentations
Day 2, June 11(Thu.) Room P (5F 501+502)
- 2P-39
Development of a Novel Evaluation Method Using LC/MS for Cancer Target Enzyme Aldo-Keto Reductase Inhibitors
(1Mukogawa Women's Univ., 2Kobe Pharm. Univ., 3ORIST)
Yuri Ohshima1, Fumiko Hara1, Shinya Takada1, Masayori Hagimori1, Shihoko Sano2, Yomi Watanabe3, Motohiro Shizuma3, oShizuyo Horiyama1
Aldo-keto reductases (AKR) superfamily plays an important role in a variety of biological functions. AKR1B10 and AKR1B1 are key therapeutic targets for breast cancer and diabetic neuropathy, respectively. For inhibitors to minimize side effects, high isoform selectivity is essential. Therefore, an accurate method is required to distinguish an inhibitor's efficacy between AKR1B1 and AKR1B10. While AKR activity is typically evaluated by NADPH absorbance at 340 nm, this conventional method can be compromised by other NADPH-dependent enzymes. In this study, we developed a novel evaluation method using LC/MS to analyze metabolites of substrates such as GSH-CA and P3A. This LC/MS-based approach provides a more direct and specific assessment of inhibitory efficiency compared to traditional UV method.
