Development of a tool for analyzing the mechanism of action of resolvins based on the molecular structure of unsaturated fatty acids
Project/Area Number |
17K08360
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Research Category |
Grant-in-Aid for Scientific Research (C)
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Allocation Type | Multi-year Fund |
Section | 一般 |
Research Field |
Drug development chemistry
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Research Institution | Nagasaki University |
Principal Investigator |
FUKUDA Hayato 長崎大学, 医歯薬学総合研究科(薬学系), 准教授 (30434450)
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Project Period (FY) |
2017-04-01 – 2020-03-31
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Project Status |
Completed (Fiscal Year 2019)
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Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2019: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2018: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2017: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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Keywords | レゾルビン / 安定等価体 / 標的タンパク質 / シクロプロパン / 構造活性相関 / 分子プローブ / レゾルビンE2 / 抗炎症活性 / 標的タンパク / 炎症収束 / 不飽和脂肪酸 / レゾルビンE3 |
Outline of Final Research Achievements |
In this study, we focused on the molecular structure of bioactive polyunsaturated fatty acids for drug discovery research based on stable equivalents of resolvins and started this research for the purpose of developing a tool to analyze the mechanism of action of resolvins using chemical probes. Two units of resolvin E2 (CP-RvE2) with cyclopropane, which is a stable equivalent of resolvin E2, and a new azide unit were prepared. We succeeded in synthesizing 18-azidopropoxy-CP-RvE2 and 20-azidopropoxy-CP-RvE2 using the Sonogashira coupling as the key reaction.
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Academic Significance and Societal Importance of the Research Achievements |
本研究ではレゾルビンE2安定等価体に対してリンカーの接続に成功した。この成果によって、様々なレゾルビン類の分子プローブの開発が期待される。多価不飽和脂肪酸は類似の分子構造を有することから、レゾルビンE2で標的タンパク質を同定できれば、本研究は多価不飽和脂肪酸の標的タンパク質同定法の一般的手法となりうる。また、それらの標的タンパク質を同定することができれば、炎症収束の作用機序の解明に繋がるとともに、新規抗炎症薬開発の端緒となる。
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Report
(4 results)
Research Products
(50 results)
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[Journal Article] Resolvin E3 Attenuates Allergic Airway Inflammation via the interleukin-23-interleukin-17A Pathway2019
Author(s)
Sato M, Aoki-Saito H, Fukuda H, Ikeda H, Koga Y, Yatomi M, Tsurumaki H, Maeno T, Saito T, Nakakura T, Mori T, Yanagawa M, Abe M, Sako Y, Dobashi K, Ishizuka T, Yamada M, Shuto S, Hisada T.
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Journal Title
FASEB J.
Volume: Nov;33(11)
Issue: 11
Pages: 12750-12759
DOI
Related Report
Peer Reviewed / Open Access
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