Drug development of novel anti-mitotic agent with unique phenotype and elucidation of the mechanism of action
Project/Area Number |
17K08371
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Research Category |
Grant-in-Aid for Scientific Research (C)
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Allocation Type | Multi-year Fund |
Section | 一般 |
Research Field |
Drug development chemistry
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Research Institution | Kogakuin University |
Principal Investigator |
MATSUNO Kenji 工学院大学, 先進工学部, 教授 (50433214)
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Co-Investigator(Kenkyū-buntansha) |
大野 修 工学院大学, 先進工学部, 准教授 (20436992)
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Project Period (FY) |
2017-04-01 – 2021-03-31
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Project Status |
Completed (Fiscal Year 2020)
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Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2019: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2018: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2017: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
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Keywords | 抗がん剤 / リード化合物 / 細胞周期 / プローブ分子 / 創薬 / 標的分子探索 / 医薬化学 / ケミカルバイオロジー / 創薬化学 / 薬学 |
Outline of Final Research Achievements |
Compound 1 suppressed cell cycle with unique phenotype to induce apoptosis. Analogue synthesis of compound 1 revealed the structure activity relationships (SARs), and provided enhanced potent analogues. Also, we designed and synthesized the probe molecule to identify the target molecule of compound 1 based on the SARs. Elucidation of the target molecule is on going.
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Academic Significance and Societal Importance of the Research Achievements |
既存の細胞周期阻害剤とは全く異なる性質を有する化合物1の医薬化学研究により、抗がん剤リード化合物へと進化させた。また、化合物1のプローブ分子を設計・合成し、細胞内の標的分子を探索した。 本研究成果により、細胞周期を標的とした新規抗がん剤研究開発における化学基盤を構築した。
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Report
(5 results)
Research Products
(17 results)
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[Journal Article] Cyclic analogue of S-benzylisothiourea that suppresses kynurenine production without inhibiting indoleamine 2,3-dioxygenase activity.2018
Author(s)
Fukuda, M.; Sasaki, T.; Hashimoto, T.; Miyachi, H.; Waki, M.; Asai, A.; Takikawa, O.; Ohno, O.; Matsuno, K.
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Journal Title
Bioorg. Med. Chem. Lett.
Volume: 28
Pages: 2846-2849
Related Report
Peer Reviewed
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[Presentation] Synthtic studies on GPR35 agonist without species-specificity2019
Author(s)
Koide, T.; Watanabe, T.; Naganuma, M. Hashimoto, T.; Akaki, S.; Furuta, K.; Yamamoto, Y.; Nagashima, S.; Tokiwa, H.; Tanaka, S.; Ohno, O.; Matsuno, K.
Organizer
27th International Society of Heterocyclic Chemistry Congress
Related Report
Int'l Joint Research
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