Development of anti-HIV agents targeting weak points of viral replication mechanism
| Project/Area Number |
26670053
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | Tokyo Medical and Dental University |
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Principal Investigator |
Tamamura Hirokazu 東京医科歯科大学, 生体材料工学研究所, 教授 (80217182)
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| Project Period (FY) |
2014-04-01 – 2016-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2015: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2014: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
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| Keywords | 抗HIV薬 / 多量体形成 / カプシドタンパク質 / エンベロープタンパク質gp41 / ペプチドライブラリー / 治療標的 / HIV感染症 / エイズ / 薬剤耐性ウイルス / フォワードケミカルゲノミクス / 抗エイズ薬 / 耐性ウイルス / 部分ペプチドライブラリー / ペプチドミミック |
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| Outline of Final Research Achievements |
In this study we tried to develop novel anti-HIV agents based on our new concept. HIV proteins have some structures required for function maintenance involving oligomerization, which might be difficult to mutate. It is important to search these targets in the development of drug seeds. Capsid proteins and an envelope protein gp41 relevant to oligomer formation might have conformationally weak regions against mutation. We tried to search these regions. In consideration of these weal points as our targets, anti-HIV leads were found using peptide libraries. Finally, treatment targets were elucidated and breakthrough for creation of anti-HIV agents was accomplished.
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Report
(3 results)
Research Products
(18 results)
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[Journal Article] A minimally cytotoxic CD4 mimic as an HIV entry inhibitor2016
Author(s)
Takaaki Mizuguchi, Shigeyoshi Harada, Tomoyuki Miura, Nami Ohashi, Tetsuo Narumi, Hiromi Mori, Yu Irahara, Yuko Yamada, Wataru Nomura, Shuzo Matsushita, Kazuhisa Yoshimura, Hirokazu Tamamura
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Journal Title
Bioorganic & Medicinal Chemistry Letters
Volume: 26
Issue: 2
Pages: 397-400
DOI
Related Report
Peer Reviewed / Open Access / Int'l Joint Research
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[Journal Article] Development of a Traceable Linker Containing a Thiol-responsive Amino Acid for the Enrichment and Selective Labelling of Target Proteins.2014
Author(s)
Yamamoto J, Denda M, Maeda N, Kita M, Komiya C, Tanaka T, Nomura W, Tamamura H, Sato Y, Yamauchi A, Shigenaga A, Otaka A.
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Journal Title
Org Biomol Chem
Volume: 12-23
NAID
Related Report
Peer Reviewed / Open Access
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