2018 Fiscal Year Final Research Report
Development of cell penetrating peptide utilizing the charactaristic of disubstituted amino acid
| Project/Area Number |
17H07269
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| Research Category |
Grant-in-Aid for Research Activity Start-up
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| Allocation Type | Single-year Grants |
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| Research Field |
Drug development chemistry
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| Research Institution | Osaka University of Pharmaceutical Sciences |
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Principal Investigator |
Kato Takuma 大阪薬科大学, 薬学部, 助教 (20805296)
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| Research Collaborator |
Tanaka Masakazu (00227175)
Oba Makoto (20396716)
Doi Mitsunobu (10183500)
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| Project Period (FY) |
2017-08-25 – 2019-03-31
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| Keywords | 非天然型アミノ酸 / ペプチド / 二次構造解析 / 膜透過性ペプチド / ヘリックス構造 |
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| Outline of Final Research Achievements |
We developed cell-penetrating peptides (CPPs) having properties different from the well-known CPPs with alpha, alpha-disubstituted alpha-amino acids (dAAs), which are one of the unnatural amino acids. Introduction of dAAs into the peptides stabilized their helical structures compared to the peptides composed of natural amino acids. The dAAs-containing peptides showed high cell-penetrating ability compared to conventional CPPs especially in the longer incubation time.
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| Free Research Field |
ペプチド化学
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| Academic Significance and Societal Importance of the Research Achievements |
α,α-ジ置換アミノ酸は、含有ペプチドの二次構造の安定性を向上させる、生体内の加水分解酵素に対するの安定性を増加させる、などの天然のアミノ酸にはない特徴を有している。ペプチド創薬においてはこれらの安定性が重要であり、今回長時間の培養で高い膜透過性を示すペプチドを作成できたことは、これからの膜透過性ペプチドの創薬研究において重要な知見として利用できるものと考えている。
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