| Budget Amount *help |
¥18,070,000 (Direct Cost: ¥13,900,000、Indirect Cost: ¥4,170,000)
Fiscal Year 2019: ¥5,720,000 (Direct Cost: ¥4,400,000、Indirect Cost: ¥1,320,000)
Fiscal Year 2018: ¥5,720,000 (Direct Cost: ¥4,400,000、Indirect Cost: ¥1,320,000)
Fiscal Year 2017: ¥6,630,000 (Direct Cost: ¥5,100,000、Indirect Cost: ¥1,530,000)
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| Outline of Final Research Achievements |
Inhibitors targeting the ubiquitin-proteasome system have been used for drug leads and research tools. However, comprehensive search of inhibitors from natural sources have not been performed in the world. In this research, we proposed the construction of a new screening method using FRET, a search for specific inhibitors of trypsin-like and caspase-like activities of the proteasome, and a search for specific inhibitors of the immunoproteasome. We isolated new inhibitors of the proteasome and USP7 from marine sponges and plants. The most potent USP7 inhibitor showed an IC50 value of 94 nM.
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