| Budget Amount *help |
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2019: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2018: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2017: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
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| Outline of Final Research Achievements |
To improve the treatment of castration-resistant prostate cancer (CRPC), we developed potent and specific inhibitors of AKR1C3, a novel target of prostate cancer. We also succeeded in X-ray crystallographic analysis of the enzyme-coenzyme-inhibitor tertiary complex and clarified the binding mode the inhibitors with AKR1C3. In addition, the AKR1C3 inhibitors exhibited potentiating effects on the anticancer activity of the existing CRPC agents and overcoming effects against the resistance, suggesting that the novel AKR1C3 inihibitors may be an effective novel adjuvant drugs for overcoming the resistance in CRPC agents-resistant prostate cancer.
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