| Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2017: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2016: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2015: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
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| Outline of Final Research Achievements |
Axially chiral 16-chloro and 16-bromolamellarins N have been developed for the creation of selective kinase inhibitors. The kinase inhibitory activities of these enantiomers were evaluated on seven protein kinases. The (aR)-isomers of 16-chloro and 16-bromolamellarins N exhibited potent but non-selective inhibition on five protein kinases except for CK1ε and CLK3. On the other hand, the (aS)-isomers showed selective inhibition against only DYRK1A, GSK-3β, and PIM1.
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