Development of novel anticancer agents targeting survival strategy of cancer cells

2016 Fiscal Year Final Research Report

• Project/Area Number: 26460149
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Gifu Pharmaceutical University
• Principal Investigator: Endo Satoshi 岐阜薬科大学, 薬学部, 助教 (60433207)
• Co-Investigator(Renkei-kenkyūsha): TOYOOKA Naoki 富山大学, 大学院理工学研究部(工学), 教授 (10217565) ; GODA Hiroaki 昭和大学, 薬学部, 教授 (60276160) ; TANAKA Nobutada 昭和大学, 薬学部, 准教授 (00286866) ; KUWATA Kazuo 岐阜大学, 大学院連合創薬医療情報研究科, 教授 (00170142)
• Project Period (FY): 2014-04-01 – 2017-03-31
• Keywords: アルドケト還元酵素 / 抗癌剤 / SNP

Outline of Final Research Achievements

In this study, we searched for novel inhibitors of Nrf2-inducible aldo-keto reductase (AKR), which is the core of oxidative stress defense mechanisms, and succeeded in development of the potent and selective AKR1B10 inhibitors at the present time. Since the AKR1B10 inhibitors exhibit both inhibitory effects on proliferation in lung cancer cells and overcoming resistance to chemotherapy in anticancer drug-resistant cells, they are expected to become adjuvant anticancer drugs enabling to overcome tolerance. Furthermore, we found inactive mutants of AKR which protects nerve cells against oxidative stress and elucidated the mechanism of the inactivation.

Free Research Field

創薬科学