2016 Fiscal Year Final Research Report
Development of specific inhibitors targeting a deubiquitinating enzyme CYLD and application of these inhibitors for chemical probe.
| Project/Area Number |
15K18468
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
System genome science
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| Research Institution | Ehime University |
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Principal Investigator |
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| Project Period (FY) |
2015-04-01 – 2017-03-31
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| Keywords | CYLD / 脱ユビキチン化酵素 / NF-kBシグナル / 低分子阻害剤探索 / Subquinocin |
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| Outline of Final Research Achievements |
Many deubiquitinating enzymes (DUBs) are involved in NF-kB signal transduction. To clarify the individual role of CYLD, which is one of a main negative regulators of the NF-kB signal, we aimed to develop small chemical compounds specifically inhibited CYLD activity.
Using a cleavage assay system based on wheat cell-free protein expression system and AlphaScreen technology, one chemical compound with high inhibitory activity to CYLD and low cytotoxicity was identified from 9,600 chemical compound library. This compound significantly inhibited NF-kB signal transduction in cultured cell, but not in CYLD-knockout cells. These results indicated that we succeeded in development of small chemical compound inhibitor targeting the activity of CYLD.
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| Free Research Field |
ユビキチン化経路
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