| Project/Area Number |
25670059
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Single-year Grants |
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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) |
2013-04-01 – 2014-03-31
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| Project Status |
Completed (Fiscal Year 2013)
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| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2013: ¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
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| Keywords | ケミカルバイオロジー / 酵素阻害剤 / 薬学 |
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| Research Abstract |
Peptidyl prolyl isomerase, Pin1, is an enzyme that catalyzes isomerization reaction of phosopho-serine-proline and phospho-threonine-proline amide bond. I planned to develop inhibitors for Pin1 enzyme based on thioamide-containing peptides. Proline thioamide has larger rotation energy for isomerization in comparison with normal proline amide bonds in peptides. Thioamide derivatives of the substrate for Pin1 are expected to slow the reaction of Pin1. I synthesized thioamide version of Pin1 substrate peptide derivatives and evaluate its inhibitory activity for Pin1 enzyme. The synthesized thioamide showed larger inhibitory activity against Pin1 in comparison with the simple substrate competition at the active site.
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