2011 Fiscal Year Final Research Report
Useful β-turn mimetics having three-dimensional diversity
| Project/Area Number |
21390028
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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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 | Hokkaido University |
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Principal Investigator |
SHUTO Satoshi 北海道大学, 大学院・薬学研究院, 教授 (70241346)
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| Co-Investigator(Kenkyū-buntansha) |
ARISAWA Mitsuhiro 北海道大学, 大学院・薬学研究院, 准教授 (40312962)
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| Project Period (FY) |
2009 – 2011
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| Keywords | βターン / ペプチドミメティック / シクロプロパン / MC4 / Grb2 |
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| Research Abstract |
The stereochemical diversity-oriented b-turn mimetics were designed and efficient and stereoselective synthetic method of them have been developed. Applying the mimetics to the development of melanocortin receptor ligands, we discovered a highly potent non-peptidic lead. Thus, the stereochemical diversity-oriented b-turn mimetics were shown to be useful in developing a non-peptidic lead, especially in cases where the binding conformation of the ligand and the structural data of the receptors are lacking or are poorly documented.
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Research Products
(17 results)
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[Journal Article] Cyclopropane-Based Stereochemical Diversity-Oriented Conformational Restriction Strategy : Histamine Analog swith the4-Amino-2, 3-methano-1-(1H-imidazol-4-yl) butane Structure as Highly PotentHistamine H_3 and/or H4 Receptor Ligands. Org2012
Author(s)
M. Watanabe, T. Kobayashi, T. Hirokawa, A. Yoshida, Y. Ito, S. Yamada, N. Orimoto, Y. Yamasaki, M. Arisawa, S. Shuto
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Journal Title
Biomol. Chem
Volume: 10
Pages: 736-745
DOI
Peer Reviewed
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[Presentation] Structure-Activity Relationship Study of Unnatural cis-Isomer of Belactosin A, a Potent Proteasome Inhibitor2011
Author(s)
Shuhei, Kawamura, Yuka, Unno, Motohiro, Tanaka, Takuma, Sasaki, Akira, Asai, Mitsuhiro, Arisawa, and Satoshi, Shuto
Organizer
AIMECS 11 8t AFMC International Medicinal Chemistry Symposium Frontier of Medicinal Science
Place of Presentation
京王プラザホテル東京(東京都)
Year and Date
20111129-1202
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[Presentation] Investigation of the bioactive conformation of Histamine H3/H4 receptor antagonists by the conformational restriction strategy2011
Author(s)
Kobayashi, T. , Watanabe, M., Hirokawa, T., Yamada, S., Arisawa, M., Shuto, S.
Organizer
8th AFMC International Medicinal Chemistry Symposium (AIMECS11)
Place of Presentation
京王プラザホテル東京(東京都)
Year and Date
20111100
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