Synthesis and conformational studies of N-substituted beta-peptides toward development of inhibitors against intracellular proteins
| Project/Area Number |
17K13265
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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 |
Chemical biology
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| Research Institution | The University of Tokyo |
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Principal Investigator |
Morimoto Jumpei 東京大学, 大学院工学系研究科(工学部), 助教 (70754935)
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| Project Period (FY) |
2017-04-01 – 2019-03-31
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| Project Status |
Completed (Fiscal Year 2018)
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| Budget Amount *help |
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2018: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2017: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Keywords | ペプチド / N置換βペプチド / 配座制御 / 構造解析 / 固相合成法 / 生体膜透過性 / フォルダマー / ペプトイド / 量子化学計算 / N置換型βペプチド / 細胞膜透過性 / 立体構造解析 / ペプチドミメティクス / 細胞膜透過 / スクリーニング / 生理活性 |
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| Outline of Final Research Achievements |
Peptoid is emerging as a new therapeutic candidate that potentially overcomes the limitations of peptides for therapeutic applications such as poor membrane permeability.
In this study, we conducted a study on N-substituted β-peptide that is a derivative of regular peptoid. We established a new synthetic method for N-substituted β-peptide and developed a molecular design in which substituents are introduced on backbone carbons of the oligomers to realize conformationally constrained N-substituted β-peptides. As a result, we successfully produced new N-substituted β-peptides that form stable secondary structures.
The new synthetic oligomers produced in this study are potentially useful as scaffolds for inhibitors of intramolecular proteins.
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| Academic Significance and Societal Importance of the Research Achievements |
本研究で得られたN置換ペプチドの構造解析に関する知見は、人工オリゴマーの化学構造と配座制御の関係について新たな知見を与えるものであり、今後様々な生体模倣型のオリゴマー分子のフォールティング研究していく上での設計指針を与えるものとして学術的意義がある。
また、本研究で開発したN置換ペプチドは、生体膜透過性が高いことから、近年注目を集めるペプチドの課題を克服し新たな創薬の可能性を拓く分子として社会的意義が高い。
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Report
(3 results)
Research Products
(9 results)
