| Budget Amount *help |
¥90,350,000 (Direct Cost: ¥69,500,000、Indirect Cost: ¥20,850,000)
Fiscal Year 2021: ¥18,460,000 (Direct Cost: ¥14,200,000、Indirect Cost: ¥4,260,000)
Fiscal Year 2020: ¥18,460,000 (Direct Cost: ¥14,200,000、Indirect Cost: ¥4,260,000)
Fiscal Year 2019: ¥18,460,000 (Direct Cost: ¥14,200,000、Indirect Cost: ¥4,260,000)
Fiscal Year 2018: ¥18,460,000 (Direct Cost: ¥14,200,000、Indirect Cost: ¥4,260,000)
Fiscal Year 2017: ¥16,510,000 (Direct Cost: ¥12,700,000、Indirect Cost: ¥3,810,000)
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| Outline of Final Research Achievements |
Protein kinase (PKC) isozymes involved in cell surface signal transduction are one of the targets of intractable diseases such as cancer, Alzheimer's disease, and HIV infection. 10-Me-Aplog-1, the simplified analog of proinflammatory aplysiatoxin, is a potent PKC ligand with little tumor-promoting and proinflammatory activities. We showed that 10-Me-Aplog-1 becomes a promising medicinal lead for the above-mentioned intractable diseases through activation of PKCα and δ. In addition, its further structural modification paved the way for development of PKC isozyme-selective ligands. On the other hand, new PKC ligands were searched by machine-learning, and the alotaketals isolated from marine sponge were identified as new PKC ligand candidates. Their simplified analogs designed by the docking simulation against PKCδ-C1B were synthesized to be assayed for PKC isozyme surrogate binding. One of the ligands exhibited a higher affinity for PKCα-C1A than for PKCδ-C1B.
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