| Project/Area Number |
21K05269
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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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| Review Section |
Basic Section 37010:Bio-related chemistry
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| Research Institution | Tokyo Institute of Technology |
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Principal Investigator |
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| Project Period (FY) |
2021-04-01 – 2024-03-31
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| Project Status |
Completed (Fiscal Year 2023)
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| Budget Amount *help |
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2023: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2022: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2021: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
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| Keywords | アクロレイン / アジド / プロドラッグ / がん治療 / 化学療法 / 環化付加反応 / クリック反応 / Acrolein / Azide / Prodrug / Cycloaddition / Cancer |
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| Outline of Research at the Start |
This applicant set out to utilize a bioorthogonal prodrug activation reaction based on the 1,3-dipolar cycloaddition between aryl azide and endogenous acrolein that is generally overproduced by cancer cells. If it succeeds, this method eliminates the need for pretreatments to accumulating exogenous enzymes or other activating agents on the cancerous tissues before prodrug administration, making it more realistic for practical application.
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| Outline of Final Research Achievements |
Chemotherapy is essential in cancer treatment, but a significant challenge is that common cancer drugs also attack healthy cells, causing severe side effects. To address this problem, prodrug technology has been developed. Prodrugs are initially inactive and are designed to activate only in the specific environment of cancer cells. This research introduces a new type of prodrug that reacts only with acrolein, a metabolite overly produced by cancer cells. This means the prodrug only becomes active through a chemical reaction with acrolein, significantly reducing the impact on healthy cells. This approach does not require the addition of exogenous enzymes or activators, making it a safer and more practical option for use in treatment settings.
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| Academic Significance and Societal Importance of the Research Achievements |
現在のがん化学療法で使用される抗がん剤は、正常細胞にも作用するため多くの副作用が生じる問題がある。これを解決するため、我々はがん細胞内でのみ活性化されるプロドラッグを設計した。このプロドラッグは、特定の化学反応によりがん組織でのみ抗がん活性分子を放出し、副作用のない効果的な治療を実現した。この技術は将来、がん治療へ応用されることで、患者の生活の質の向上と医療現場での治療選択肢の拡大に寄与すると期待される。
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