| Budget Amount *help |
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2017: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2016: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2015: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
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| Outline of Final Research Achievements |
The structural analysis of bafilomycin (Baf), a specific inhibitor towards vacuolar-type ATPase (V-ATPase), was performed based on synthetic chemistry. First, the preparation of bioactive 19F-labelled Baf required for solid-state NMR measurement was achieved by synthesizing several Baf derivatives and evaluating their V-ATPase inhibitory effect. Next, behavior analysis of active and inactive F-Baf derivatives in model membrane resulted in finding the remarkable difference of their mobility, which may probably relate to the difference of their activity. Moreover, a large-scale preparation of V-ATPase as proteoliposomes was successfully accomplished and the structural analysis of F-Baf bound to V-ATPase was examined by solid-state NMR.
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