2021 Fiscal Year Final Research Report
Development and evaluation of 2',3'-bridged nucleic acid with constrained conformation of sugar and phosphate backbone
Project/Area Number |
20K15401
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Research Category |
Grant-in-Aid for Early-Career Scientists
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Allocation Type | Multi-year Fund |
Review Section |
Basic Section 37010:Bio-related chemistry
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Research Institution | Osaka University |
Principal Investigator |
Osawa Takashi 大阪大学, 薬学研究科, 助教 (00783226)
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Project Period (FY) |
2020-04-01 – 2022-03-31
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Keywords | 核酸化学 |
Outline of Final Research Achievements |
An artificial nucleic acid that can be synthesized in a short process and that has a strictly fixed conformation of the sugar and the phosphate moieties will be a practical nucleic acid pharmaceutical material that has never existed before. In this study, 2',3'-bridged nucleic acid with a 5,6-trans-fused ring was designed and synthesized. As the results, we succeeded in constructing a bicyclic skeleton with a 1,4-dioxane ring that does not have a phosphate structure. On the other hand, since the nucleoside derivatives with a phosphonate ester was extremely unstable to acidic and basic conditions, 2',3'-bridged nucleic acids having a phosphonate ester could not be synthesized.
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Free Research Field |
核酸化学
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Academic Significance and Societal Importance of the Research Achievements |
糖部2′位と3′位の間で架橋した5員環-6員環トランス縮環骨格を有する人工核酸の合成例は世界初である。合成した2′,3′-架橋型核酸は糖部とリン酸部の配座が高度に固定された特徴的な構造を有しており、核酸医薬をはじめとするオリゴ核酸を基盤とする技術への応用が期待される。
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