2012 Fiscal Year Final Research Report
Design of a stabilized short helical peptide and its application
| Project/Area Number |
22590114
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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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 |
KURIHARA Masaaki 国立医薬品食品衛生研究所, 有機化学部, 部長 (20205206)
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| Co-Investigator(Renkei-kenkyūsha) |
DEMIZU Yosuke 国立医薬品食品衛生研究所, 有機化学部 (90389180)
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| Project Period (FY) |
2010 – 2012
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| Keywords | ヘリカルペプチド / 核内レセプター / コアクチベータ |
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| Research Abstract |
We synthesized stapled helical leucine-based peptides containing 2-aminoisobutyric acid and a covalent cross-linked unit as inhibitors of vitamin D receptor (VDR)-coactivator interactions. The effects of these peptides on the human VDR were examined in an inhibition assay based on the receptor cofactor assay system, and one of them, exhibited potent inhibitory activity.
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[Journal Article]2013
Author(s)
Y. Demizu, S. Nagoya, M. Shirakawa, M. Kawamura, N. Yamagata, Y. Sato, M. Doi, M. Kurihara
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Journal Title
Bioorg. Med. Chem. Lett
Volume: 23
URL
Peer Reviewed
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[Journal Article] Twisted Structure of a Cyclic Hexapeptide Containing a Combination of Alternating L-Leu-D-Leu- Aib Segments2012
Author(s)
Demizu, Y., Nagoya, S., Doi, M., Sato, Y., Tanaka, M., Kurihara, M
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Journal Title
J. Org. Chem
Volume: 77
Pages: 9361-9365
Peer Reviewed
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[Journal Article] Design of a stabilized short helical peptide and its application to catalytic enantioselective epoxidation of (E)-chalcone2011
Author(s)
Yamagata, N., Demizu, Y., Sato, Y., Doi, M., Tanaka, M., Nagasawa, K., Okuda, H., Kurihara, M
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Journal Title
Tetrahedron Letters
Volume: 52
Pages: 798-801
Peer Reviewed
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[Journal Article] Controlling the helical screw sense of peptides with C-terminal L-valine2010
Author(s)
Demizu, Y., Yamagata, N., Sato, Y., Doi, M., Tanaka, M., Okuda, H., Kurihara, M
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Journal Title
J. Pept. Sci.
Volume: 16
Pages: 153-158
Peer Reviewed
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[Journal Article] Three-Dimensional Structural Control of Diastereomeric Leu-Leu-Aib-Leu-Leu-Aib Sequences in the Solid State2010
Author(s)
Demizu, Y., Doi, M., Sato, Y., Tanaka, M., Okuda, H., Kurihara, M
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Journal Title
J. Org. Chem
Volume: 75
Pages: 5234-5239
Peer Reviewed
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