| Project/Area Number |
26670060
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | Nagoya City University |
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Principal Investigator |
Nakagawa Hidehiko 名古屋市立大学, 薬学研究科(研究院), 教授 (80281674)
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| Co-Investigator(Renkei-kenkyūsha) |
Ieda Naoya 名古屋市立大学, 大学院薬学研究科, 助教 (00642026)
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| Project Period (FY) |
2014-04-01 – 2016-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2015: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2014: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
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| Keywords | ケミカルバイオロジー / 酵素阻害剤 |
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| Outline of Final Research Achievements |
Design and exploration of fluorescence probe compounds for the Pin1 binding pocket were performed, in which the molecules were expected to increase the fluorescence when binding to Pin1 proteins. By replacement of heteroaromatic moiety of a known Pin1 inhibitor with the fluorescent moiety which is responding to the environmental polarity. One of the inhibitory compound bearing fluorescence molecular showed good environmental response in low-polarity organic solvents and slight increase of the fluorescence in the presence of Pin1 proteins. However, the compound was assumed to have a significant amount of non-specific binding to Pin1 other than the substrate binding pocket.
Other potent Pin1 inhibitors were also explored for future development of the probe, and the compound bearing azocanyl moiety for the proline pocket was found to have potent Pin1 inhibiting activity.
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