Development of mid-size drugs based on peptidomimetic
| Project/Area Number |
15H04652
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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 | 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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| Co-Investigator(Kenkyū-buntansha) |
野村 渉 東京医科歯科大学, 生体材料工学研究所, 准教授 (80463909)
水口 貴章 東京医科歯科大学, 生体材料工学研究所, 助教 (30732557)
大橋 南美 東京医科歯科大学, 生体材料工学研究所, 助教 (90707051)
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| Research Collaborator |
YOSHIMURA Kazuhisa
MURAKAMI Tsutomu
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| Project Period (FY) |
2015-04-01 – 2018-03-31
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| Project Status |
Completed (Fiscal Year 2017)
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| Budget Amount *help |
¥17,030,000 (Direct Cost: ¥13,100,000、Indirect Cost: ¥3,930,000)
Fiscal Year 2017: ¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2016: ¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2015: ¥7,540,000 (Direct Cost: ¥5,800,000、Indirect Cost: ¥1,740,000)
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| Keywords | 中分子 / ペプチドミメティック / 環状ペプチド / HIV / がん / ステープルペプチド / CXCR4 / GPCR / ヒト免疫不全ウイルス / 医薬品開発 / 中分子創薬 / 二次構造 / 2価型 / 二量体 / 高次構造模倣型 / 2価結合型GPCRリガンド |
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| Outline of Final Research Achievements |
Peptidomimetics that mimic conformation such as secondary and tertiary structures of peptides/proteins have led to the recent development of anti-cancer and anti-HIV agents. Some examples are described as follows. Chemokine receptor CXCR4 antagonists based on cyclic peptides having conformationally constrained structures have been synthesized as agents with anti-chemotactic activity against cancer cells and inhibitory activity against HIV entry. HIV protein-derived stapled peptides with helix mimetics have been developed as HIV integrase inhibitors. Dimer and trimer mimetics of a C-terminal helical region (CHR/C34) of an envelope protein gp41 have been developed as HIV fusion inhibitors. In addition, bivalent ligands based on the above CXCR4 antagonists such as 14-mer peptide T140 derivatives have been synthesized to produce effective metastatic inhibition with the therapeutic potential. Taken together, these advantaged of mid-size drugs were shown.
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Report
(4 results)
Research Products
(26 results)
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[Journal Article] A minimally cytotoxic CD4 mimic as an HIV entry inhibitor.2016
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
Bioorg Med Chem Lett.
Volume: 26
Pages: 397-400
DOI
Related Report
Peer Reviewed / Open Access / Int'l Joint Research / Acknowledgement Compliant
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