| Project/Area Number |
24390023
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Partial 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 | Hokkaido University |
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Principal Investigator |
SHUTO Satoshi 北海道大学, 大学院薬学研究院, 教授 (70241346)
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| Co-Investigator(Kenkyū-buntansha) |
FUKUDA Hayato 北海道大学, 大学院薬学研究院, 助教 (30434450)
有澤 光弘 北海道大学, 大学院・薬学研究院, 准教授 (40312962)
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| Co-Investigator(Renkei-kenkyūsha) |
MINAMI Masabumi 北海道大学, 大学院薬学研究院, 教授 (20243040)
HIGASHIDA Haruhiro 金沢大学, 子どものこころの発達研究センター, 特任教授 (30093066)
HIROKAWA Takatugu 国立研究開発法人産業技術総合研究所, 創薬分子プロファイリング研究センター, 分子シミュレーションチームチーム長 (20357867)
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| Project Period (FY) |
2012-04-01 – 2015-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥15,990,000 (Direct Cost: ¥12,300,000、Indirect Cost: ¥3,690,000)
Fiscal Year 2014: ¥3,380,000 (Direct Cost: ¥2,600,000、Indirect Cost: ¥780,000)
Fiscal Year 2013: ¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2012: ¥7,410,000 (Direct Cost: ¥5,700,000、Indirect Cost: ¥1,710,000)
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| Keywords | シクロプロパン / 配座制御 / 三次元的多様性 / 分子設計 / BGT-1 阻害剤 / プロテアソーム阻害剤 / BASE阻害剤 |
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| Outline of Final Research Achievements |
Cyclopropane is very effective for conformational restriction of compounds due to the characteristic steric and stereoelectronic features, which are sic/trans-restriction, cyclopropylic strain, and bisected conformational preference. We devised the three-dimensional structural diversity-oriented conformational restriction strategy based on the characteristic features of cyclopropane, by which a variety of conformationally restricted analogs of conformationally flexible biologically active prototype compounds were designed and synthesized. Thus, we successfully identified highly potent compounds, which are a GABA transporter subtype BGT-1 inhibitor, proteasome inhibitors, and β-secretase (BASE) inhibitors.
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