Design, synthesis and functional studies of small molecules that modulate protein-protein interactions
Project/Area Number |
24590136
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Research Category |
Grant-in-Aid for Scientific Research (C)
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Allocation Type | Multi-year Fund |
Section | 一般 |
Research Field |
Drug development chemistry
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Research Institution | Hoshi University |
Principal Investigator |
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Project Period (FY) |
2012-04-01 – 2015-03-31
|
Project Status |
Completed (Fiscal Year 2014)
|
Budget Amount *help |
¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2014: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2013: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2012: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
|
Keywords | 天然物合成 / タンパク質間相互作用 / 創薬化学研究 / 8員環形成 / コチレニン / Cotylenin / 14-3-3タンパク質 / PCSK9 / LDL受容体 / 構造活性相関 / 全合成 |
Outline of Final Research Achievements |
Synthetic study of cotylenin A, a natural product which stabilize protein-protein interactions was carried out. A-ring part was synthesized with intramolecular aldol reaction from optically active perillyl alcohol stereoselectively. Furthermore, Construction of 8-membered ring of B-ring part was accomplished by ring closing metathesis reaction via the coupling reaction of A-ring and C-ring and the subsequent functionalizations. Now we are working on stereoselective incorporation of two hydroxyl groups. On the other hand, we are almost finished synthesis of two parts of sugar-moiety. We will assemble these two parts by double acetalization reaction. And we are planning to complete total synthesis of cotylenin A, synthesize derivatives and analyze functions of synthesized compounds.
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Report
(4 results)
Research Products
(21 results)
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[Journal Article] Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton.2015
Author(s)
Taki Sakai, Yotaro Matsumoto, Minoru Ishikawa, Kazuyuki Sugita, Yuichi Hashimoto, Nobuhiko Wakai, Akio Kitao, Era Morishita, Chikashi Toyoshima, Tomoatsu Hayashi, Tetsu Akiyama
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Journal Title
Bioorg Med Chem.
Volume: 23
Issue: 2
Pages: 328-339
DOI
Related Report
Peer Reviewed / Open Access
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[Journal Article] Discovery of DF-461, a Potent Squalene Synthase Inhibitor2013
Author(s)
Masanori Ichikawa, Masami Ohtsuka, Hitoshi Ohki, Masahiro Ota, Noriyasu Haginoya, Masao Itoh, Yoshihiro Shibata, Yutaka Ishigai, Koji Terayama, Akira Kanda, and Kazuyuki Sugita
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Journal Title
ACS Med. Chem. Lett.
Volume: 4
Issue: 9
Pages: 932-936
DOI
NAID
Related Report
Peer Reviewed
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