| Project/Area Number |
18H02685
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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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| Review Section |
Basic Section 50010:Tumor biology-related
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| Research Institution | National Defense Medical College |
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Principal Investigator |
Shinomiya Nariyoshi 防衛医科大学校(医学教育部医学科進学課程及び専門課程、動物実験施設、共同利用研究施設、病院並びに防衛, 分子生体制御学, 教授 (40505260)
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| Co-Investigator(Kenkyū-buntansha) |
田沼 靖一 東京理科大学, 研究推進機構総合研究院, 教授 (10142449)
中村 浩之 東京工業大学, 科学技術創成研究院, 教授 (30274434)
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| Project Period (FY) |
2018-04-01 – 2021-03-31
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| Project Status |
Completed (Fiscal Year 2020)
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| Budget Amount *help |
¥17,420,000 (Direct Cost: ¥13,400,000、Indirect Cost: ¥4,020,000)
Fiscal Year 2020: ¥5,070,000 (Direct Cost: ¥3,900,000、Indirect Cost: ¥1,170,000)
Fiscal Year 2019: ¥5,850,000 (Direct Cost: ¥4,500,000、Indirect Cost: ¥1,350,000)
Fiscal Year 2018: ¥6,500,000 (Direct Cost: ¥5,000,000、Indirect Cost: ¥1,500,000)
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| Keywords | c-Met / 受容体型チロシンキナーゼ / 分子創薬 / 阻害剤 / 刺激剤 / COSMOS法 / ｃ-Met / In silico創薬 / Kinase阻害剤 / Met stimulator / 低分子阻害薬 / Met ｓtimulator / 低分子医薬 / 抑制剤 / ｃ－Met / in silico創薬 / キナーゼ阻害剤 / Stimulator |
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| Outline of Final Research Achievements |
Met is a membrane receptor tyrosine kinase involved in liver regeneration and tissue repair. Based on the structures of the candidate low molecular weight compounds of Met stimulator obtained so far, we designed and synthesized new compounds with lower toxicity, and confirmed their Met stimulating activity on cells. In addition, through the investigation of the relationship between the molecular structure and Met stimulating activity, it was confirmed that the dimethyl-amino group in the side chain is important for the expression of activity. Currently, we are trying to further improve the structure from the viewpoint of in silico drug designing for practical use.
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| Academic Significance and Societal Importance of the Research Achievements |
本研究において、in silico創薬（コンピュータを用いた薬剤デザイン）に構造－活性解析の観点を加えることにより、薬剤活性と結合部位の関係が徐々に明らかになってきている。合成された低分子Met Stimulatorが、標的分子であるMetを活性化し生物学的機能を十分に発揮することが証明できれば、本研究が今後の新薬開発に向けての重要なステップを示したことになる。
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