Development of helical template peptides for post-functionalization
| Project/Area Number |
15K18905
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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 | National Institute of Health Sciences |
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Principal Investigator |
Misawa Takashi 国立医薬品食品衛生研究所, 有機化学部, 主任研究官 (40709820)
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| Project Period (FY) |
2015-04-01 – 2019-03-31
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| Project Status |
Completed (Fiscal Year 2018)
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| Budget Amount *help |
¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2017: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2016: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Keywords | ヘリカルペプチド / post-modification / ジ置換アミノ酸 / 細胞膜透過性 / 抗菌活性 / クリックケミストリー / ヘリカルテンプレート / ペプチド / 固相合成 / 膜透過ペプチド |
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| Outline of Final Research Achievements |
Helical structures in proteins and synthetic bioactive peptides play pivotal roles in biochemistry and chemistry. Methods that regulate the helical structures of peptides are required in order to develop well-defined functional peptides. In this study, we herein developed post-functionalizable helical peptides composed of Leu, Aib, and Azl residues. We show that the synthesized peptides 1 and 2 form helical structures, and may be modified using specific side chain or several functional groups by the click reaction without influencing their secondary structures.
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| Academic Significance and Societal Importance of the Research Achievements |
本研究の特色は、高度に空間制御されたペプチドをテンプレートとして、post-modificationを行うことで様々な生理活性の付与を達成する点である。従来のペプチド合成手法では生理活性に応じて個別に合成しなければならないが、本手法では一つのテンプレートペプチドを合成すれば、様々な生理活性を有するペプチドを得ることが出来る。また、必要な官能基を後から導入することが出来るため、誘導体合成が簡便になる等の利点も挙げられる。
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Report
(5 results)
Research Products
(21 results)
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[Journal Article] Effects of alkyl side chains and terminal hydrophilicity on vitamin D receptor (VDR) agonistic activity based on the diphenylpentane skeleton2015
Author(s)
Takashi Misawa, Momoko Yorioka, Yosuke Demizu, Tomomi Noguchi-Yachide, Nobumichi Ohoka, Megumi Kurashima-Kinoshita, Hitomi Motoyoshi, Hisao Nojiri, Atsushi Kittaka, Makoto Makishima, Mikihiko Naito, Masaaki Kurihara
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Journal Title
Bioorg. Med. Chem. Lett.
Volume: 25
Issue: 22
Pages: 5362-5366
DOI
Related Report
Peer Reviewed / Int'l Joint Research
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