2021 Fiscal Year Final Research Report
Development of robust functionalization methods for biological applications
Project/Area Number |
19K06992
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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 |
Review Section |
Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
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Research Institution | The University of Tokyo |
Principal Investigator |
Takita Ryo 東京大学, 大学院薬学系研究科(薬学部), 准教授 (50452321)
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Project Period (FY) |
2019-04-01 – 2022-03-31
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Keywords | 銅触媒 / 水酸基化反応 / DFT計算 / 直鎖脂肪酸 / 重水素化反応 / アシルトランスフェラーゼ |
Outline of Final Research Achievements |
The development of robust functionalization methods for biological applications has been investigated in this research. Copper-catalyzed arene hydroxylation has been developed using water as an oxygen source as well as a sole solvent. Mechanistic investigations experimentally and theoretically revealed the dual role of sucrose. A concise protocol for the precisely controlled tetradeuteration of straight-chain fatty acids at the α- and β- positions has been also developed. The use of four deuterium atoms in fatty acids as well as a diagnostic peak of phosphatidylcholines thus obtained enabled the identification of acyltransferases that transfer the acyl moiety derived from an oxidized linoleic acid, hydroxyoctadecadienoic acid (HODE), to lysophosphatidylcholine.
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Free Research Field |
有機合成化学
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Academic Significance and Societal Importance of the Research Achievements |
水中で遷移金属触媒を用いた炭素―酸素結合形成反応を実現した。特に水溶性の生物活性分子に適用可能な反応の礎となる。また、脂肪酸の選択的重水素化反応を開発し、これを用いて酸化脂肪酸由来のホスファチジルコリン合成に関与するアシルトランスフェラーゼを同定した。酸化脂肪酸は生体内の代謝で生成するため、これを追跡することは困難であった。多様な脂肪酸に適用可能なプロセスであり、多彩な機能を示す脂質・脂肪酸の機能解明に貢献できる。
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