Synthetic study of membrane permeable inhibitor of HTLV-I protease
| Project/Area Number |
18590110
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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 | Kyoto Pharmaceutical University |
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Principal Investigator |
KIMURA Tooru Kyoto Pharmaceutical University, 薬学部, 准教授 (70204980)
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| Project Period (FY) |
2006 – 2008
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| Project Status |
Completed (Fiscal Year 2008)
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| Budget Amount *help |
¥3,310,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥510,000)
Fiscal Year 2008: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2007: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2006: ¥1,100,000 (Direct Cost: ¥1,100,000)
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| Keywords | 医薬品化学 / プロテアーゼ阻害剤 / HTLV-I / レトロウイルス / プロテアーゼ / 阻害剤 / 遷移状態ミメティック |
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| Research Abstract |
アスパルティックプロテアーゼ阻害剤の設計は, 基質遷移状態概念誘導体を基質の切断部位に組み込み, これを基に構造変換を行うといった手法が一般的である. 我々が既に合成したHTLV-Iプロテアーゼの基質部位p19/p24に相当するオクタペプチド(PQVL*PVMH)にHMCを導入し多少の構造変換を行った化合物KMI-10162は, HTLV-Iプロテアーゼ阻害活性を有していた. そこでこの化合物をリードに, 膜透過性を上昇させるようデザインした阻害剤を合成した.
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Report
(4 results)
Research Products
(28 results)
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[Journal Article] β-Secretase inhibitors : Modification at the P4 position and improvement of inhibitory activity in cultured cell2006
Author(s)
Yoshio Hamada, Naoto Igawa, Hayato Ikari, Zyta Ziora, Jeffrey-Tri Nguyen, Abdellah Yamani, Koushi Hidaka, Tooru Kimura, Kazuki Saito, Yoshio Hayashi, Maiko Ebina, Shoichi Ishiura, Yoshiaki Kiso
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Journal Title
Bioorg. Med. Chem. Lett 16(16)
Pages: 4354-4359
Related Report
Peer Reviewed
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[Journal Article] Design and synthesis of potent β-secretase (BACE1) inhibitors with P1' carboxylic acid bioisosteres2006
Author(s)
Tooru Kimura, Yoshio Hamada, Monika Stochaj, Hayato Ikari, Ayaka Nagamine, Hamdy Abdel-Rahman, Naoto Igawa, Koushi Hidaka, Jeffrey-Tri Nguyen, Kazuki saito, Yoshio Hayashi, Yoshiaki Kiso
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Journal Title
Bioorg. Med. Chem. Lett 16(9)
Pages: 2380-2386
Related Report
Peer Reviewed
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[Presentation] Road to HTLV-I protease inhibition2008
Author(s)
Jeffrey-Tri Nguyen, Meihui Zhang, Ayako Itami, Hikoichiro Maegawa, Keiji Nishiyama, Tooru Kimura, Yoshio Hayashi, Maosheng Cheng, Yoshiaki Kiso
Organizer
International Symposium on Integrated Medicinal Science
Place of Presentation
Kyoto, Japan
Related Report
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