| Budget Amount *help |
¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2016: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2015: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2014: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
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| Outline of Final Research Achievements |
It has been reported that ubiquitin-activating enzyme is highly expressed in leukemic cells and that inhibition of the enzyme disturbs their proliferation.
Therefore, ubiquitin-activating enzymes are interesting as a drug target. In this study, we attempted to discover ubiquitin-activating enzyme inhibitors. Based on the catalytic mechanism of ubiquitin-activating enzyme, we designed and synthesized several compounds which were expected to show inhibitory activity dependent on enzyme reaction. As a result of their biological evaluation, we succeeded in identification of a compound inhibiting ubiquitin-activing enzyme.
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