Integrated drug discovery study for conquering Alzheimer's disease
| Project/Area Number |
23590137
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Kobe Pharmaceutical University (2014)
Kobe Gakuin University (2011-2013) |
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Principal Investigator |
HAMADA Yoshio 神戸薬科大学, 薬学部, 研究員 (70424968)
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| Project Period (FY) |
2011-04-28 – 2015-03-31
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| Project Status |
Completed (Fiscal Year 2014)
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| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2013: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2012: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2011: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
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| Keywords | アルツハイマー病 / BACE1 / β-セクレターゼ / 酵素阻害剤 / ペプチド / アミロイドβ / 凝集阻害剤 / アミロイドβペプチド / 阻害剤 米国 |
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| Outline of Final Research Achievements |
The increase of dementia patients is a big issue for Japan as it faces a rapidly aging society. To conquer Alzheimer’s disease, this research project aimed the development of BACE1 and Aβ aggregation inhibitors. Novel BACE1 inhibitors, YHI-309 and YHI-764 (IC50 = 13 nM and 26 nM, respectively), with a nitro or thiadiazole group were designed and synthesized. These compounds appear to have promise as drug candidates because of their increased membrane permeability.
Aβ aggregation inhibitors, YHI-008 and YHI-009, also designed and synthesized. These compounds exhibited potent inhibitory activity against the Aβ aggregation, and could recognize a specific Aβ conformer. These compounds are expected to use a research tool for pathogenic mechanism analysis.
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Report
(5 results)
Research Products
(47 results)
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[Journal Article] Structure-activity relationship study of BACE1 inhibitors possessing a chelidonic or 2,6-pyridinedicarboxylic scaffold at the P2 position2014
Author(s)
Yoshio Hamada, Kenji Suzuki, Tomoya Nakanishi, Diganta Sarma, Hiroko Ohta, Ryoji Yamaguchi, Moe Yamasaki, Koushi Hidaka, Shoichi Ishiura, Yoshiaki Kiso
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Journal Title
Bioorganic & Medicinal Chemistry Letters
Volume: 26
Issue: 2
Pages: 618-623
DOI
Related Report
Peer Reviewed
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