| Project/Area Number |
16K18914
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | Tokyo University of Pharmacy and Life Science |
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Principal Investigator |
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| Project Period (FY) |
2016-04-01 – 2019-03-31
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| Project Status |
Completed (Fiscal Year 2018)
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| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2018: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2017: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2016: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
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| Keywords | ジスルフィド結合 / 創薬化学 / ペプチド合成 / 固相合成 / 有機化学 / 固相担持試薬 / 3-ニトロ-2-ピリジンスルフェニル基 / ペプチド合成化学 |
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| Outline of Final Research Achievements |
Focused on nicotinic acid derivative (Npys-OMe derivative), the innovative and efficient reagents for disulfide bond formation were developed. In model study using the oxidation of reduced-form peptides, it was found that the Npys-OMe derivative and its resin efficiently function as a mild oxidizing agent. And it was succeeded in providing a unique disulfide bond formation method using this compound. Therefore, it is thought that these results can contribute the synthesis of bioactive disulfide peptides and the development of functional molecules in fields of drug discovery and peptide chemistry.
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| Academic Significance and Societal Importance of the Research Achievements |
本研究課題で着目したNpys-OMe誘導体はその構造中に特徴的なメトキシチオ構造を含むことから、当該化合物に基づくジスルフィド結合形成試薬の創製は、新規性かつ独自性が高い。また、効率的なジスルフィド結合構築手法の確立および提供が可能となり、創薬化学、有機化学、ペプチド・タンパク質化学における学術的なインパクトがある。本研究成果は、ペプチド医薬品の開発および機能性分子の創製にも繋がり、社会的貢献も大きいと考えられる。
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