Budget Amount *help |
¥42,250,000 (Direct Cost: ¥32,500,000、Indirect Cost: ¥9,750,000)
Fiscal Year 2018: ¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2017: ¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2016: ¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2015: ¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2014: ¥21,450,000 (Direct Cost: ¥16,500,000、Indirect Cost: ¥4,950,000)
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Outline of Final Research Achievements |
Marine macrolide, aplyronine A exhibits extremely strong antitumor activity by inducing protein-protein interaction (PPI) between two major cytoskeletons, actin and tubulin. In this study, we aimed to clarify structural factors for PPI and to develop the artificial analogs. Because the side-chain moiety binds to actin and the trimethylserine moiety in the macrolactone moiety interacts with tubulin, we design two hybrids from aplyronine A and the other actin-deplymerizing marine macrolides. Among them, hybrid from alyronine A and swinholide A shows same biological activity as aplyronine A, which is a simplified analog of aplyronine A.
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