Development of the sensitive methods for detection of the fluorinated compounds bound to the target proteins
| Project/Area Number |
18K05185
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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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| Review Section |
Basic Section 34020:Analytical chemistry-related
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| Research Institution | Meisei University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
吉村 悦郎 放送大学, 教養学部, 特任栄誉教授 (10130303)
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| Project Period (FY) |
2018-04-01 – 2021-03-31
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| Project Status |
Completed (Fiscal Year 2020)
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| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2020: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2019: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2018: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Keywords | フッ素医薬品 / タンパク質 / 分子間相互作用 / 核磁気共鳴スペクトル / フッ素化合物 / リガンド / 選択的検出 / 標的タンパク質 / 核磁気共鳴 / 核磁気共鳴法 |
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| Outline of Final Research Achievements |
In the present research, the NMR-based screening techniques with selective 19F detections were applied to a protein-ligand complex. The highly sensitive and selective methods to observe ligands at the atomic level were developed. In purpose of identifying the 19F as well as 1H binding epitopes of the fluorinated compounds, the combinatorial analysis using 1H{1H} and 19F{1H} saturation transfer difference (STD) experiments and were carried out. The 19F-T1 and 19F-diffusion coefficients were also measured to observe the intermolecular interaction between fluorinated compounds and proteins.
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| Academic Significance and Societal Importance of the Research Achievements |
薬剤とタンパク質との相互作用は、酵素―阻害剤など生体反応において重要な役割を果たす。本研究では、フッ素を含む薬剤とタンパク質との相互作用解析に焦点を当てた。通常、フッ素はタンパク質には含まれないため、フッ素検出が直接的に含フッ素薬剤の検出になる。この選択制を利用し、フッ素原子核および水素原子核を観測し、含フッ素薬剤の構造において、どの部分がタンパク質との相互作用に強く関与するかを解析した。抗ウイルス薬など、酵素阻害剤としての機能を有する含フッ素医薬品の作用機序の解析に役立つ分析手法と考えられ、社会的要請度の高い研究と思われる。
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Report
(4 results)
Research Products
(11 results)
