2017 Fiscal Year Final Research Report
Preparation of histone demethylase inhibitors based on substrate specificity
| Project/Area Number |
26460159
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Waseda University |
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Principal Investigator |
Kakizawa Taeko 早稲田大学, 理工学術院, 講師(任期付) (60445963)
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| Project Period (FY) |
2014-04-01 – 2018-03-31
|
| Keywords | 酵素阻害剤 |
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| Outline of Final Research Achievements |
Lysine-specific demethylase 1 (LSD1) is a flavin-dependent enzyme that removes methyl groups from lysine residues at the fourth position of histone H3. Several substrate-based LSD1 inhibitors that have LSD1 inactivator motifs on the side chain of the lysine residue in histone H3 peptide were prepared. Inhibitory activity of the synthesized compounds was evaluated using recombinant LSD1.
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| Free Research Field |
創薬化学
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