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Development of a ganma-tubulin targeting diketopiperazine and its study on chemical biology

Research Project

Project/Area Number 16K15145
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeMulti-year Fund
Research Field Drug development chemistry
Research InstitutionTokyo University of Pharmacy and Life Science

Principal Investigator

Hayashi Yoshio  東京薬科大学, 薬学部, 教授 (10322562)

Project Period (FY) 2016-04-01 – 2018-03-31
Project Status Completed (Fiscal Year 2017)
Budget Amount *help
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2017: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2016: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywordsジケトピペラジン / γ-チューブリン / プリナブリン / 抗がん剤 / 水溶性プロドラック / γ―チューブリン / 薬学 / 有機化学 / 創薬化学 / チューブリン
Outline of Final Research Achievements

In this study we focus on a novel diketopiperazine (DKP) derivative "KPU-406" targeting γ-tubulin. To elucidate the function of γ-tubulin, a potential target molecule for cancer therapy, we synthesized fragment derivatives having a partial structure of KPU-406 and biotinylated derivative of KPU-406 as a chemical probe.
From now on, through determination of the interaction between obtained derivatives and γ-tubulin, it is expected that the function of γ-tubulin is elucidated, leading to the new anticancer drug development.

Report

(3 results)
  • 2017 Annual Research Report   Final Research Report ( PDF )
  • 2016 Research-status Report
  • Research Products

    (9 results)

All 2017 2016

All Journal Article (1 results) (of which Peer Reviewed: 1 results) Presentation (8 results) (of which Int'l Joint Research: 3 results)

  • [Journal Article] Click strategy using disodium salts of amino acids improves the water solubility of plinabulin and KPU-3002017

    • Author(s)
      Fumika Yakushiji, Kyohei Muguruma, Yoshiki Hayashi, Takuya Shirasaka, Ryosuke Kawamata, Hironari Tanaka, Yushi Yoshiwaka, Akihiro Taguchi, Kentaro Takayama, Yoshio Hayashi
    • Journal Title

      Bioorganic Medicinal Chemistry

      Volume: 25 Issue: 14 Pages: 3623-3630

    • DOI

      10.1016/j.bmc.2017.04.024

    • Related Report
      2017 Annual Research Report
    • Peer Reviewed
  • [Presentation] KPU-300を基盤とした微小管重合阻害剤の構造活性相関研究2017

    • Author(s)
      久保木 里衣、林 良樹、中澤 大樹、知念 拓実、田口 晃弘、谷口 敦彦、高山 健太郎、臼井 健郎、林 良雄
    • Organizer
      日本薬学会第 137 年会
    • Place of Presentation
      東北大学川内キャンパス、仙台
    • Year and Date
      2017-03-24
    • Related Report
      2016 Research-status Report
  • [Presentation] Structure-Activity Relationship Study of Anti-Microtubule Agent KPU-300 and Improvement of Its Solubility2017

    • Author(s)
      Y. Hayashi, R. Kuboki, C. Sakuma, T. Chinen, A. Taguchi, K. Takayama, A. Taniguchi, T. Usui, Y. Hayashi
    • Organizer
      The EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry (EFMC-ASMC’17)
    • Related Report
      2017 Annual Research Report
    • Int'l Joint Research
  • [Presentation] Solid-phase assisted synthesis of hydrophobic plinabulin-hydrophilic peptide conjugate2017

    • Author(s)
      T. Shirasaka, K. Muguruma D. Akiyama, A. Taguchi, K. Takayama, A. Taniguchi, Y. Hayashi
    • Organizer
      21st Korean Peptide Protein Society Symposium(21st KPPS)
    • Related Report
      2017 Annual Research Report
    • Int'l Joint Research
  • [Presentation] Structure-Activity Relationship Study of Anti-microtubule Agent based on KPU-300 Structur2017

    • Author(s)
      R. Kuboki, Y. Hayashi, C. Sakuma, M. Kobayashi, T. Chinen, A. Taguchi, K. Takayama, A. Taniguchi, T. Usui, Y. Hayashi
    • Organizer
      21st Korean Peptide Protein Society Symposium(21st KPPS)
    • Related Report
      2017 Annual Research Report
    • Int'l Joint Research
  • [Presentation] 微小管重合阻害剤KPU-300を基盤とした構造活性相関研究2017

    • Author(s)
      林 良樹,久保木 里衣,佐久間 千尋,中澤 大輝,六車 共平,知念 拓実,田口 晃弘,高山 健太郎,薬師寺 文華,谷口 敦彦,臼井 健郎,林 良雄
    • Organizer
      第35回メディシナルケミストリーシンポジウム
    • Related Report
      2017 Annual Research Report
  • [Presentation] 固相担持型ジスルフィド化試薬を応用したPlinabulinプロドラッグの創製研究2017

    • Author(s)
      白坂 拓也、六車 共平、秋山 大地、田口 晃弘、高山 健太郎、谷口 敦彦、林 良雄
    • Organizer
      創薬懇話会2017 in 加賀
    • Related Report
      2017 Annual Research Report
  • [Presentation] ジケトピペラジン型微小管重合阻害剤KPU-300の構造活性相関研究2017

    • Author(s)
      久保木 里衣、林 良樹、佐久間 千尋、中澤 大輝、知念 拓実、田口 晃弘、高山 健太郎、谷口 敦彦、臼井 健郎、林 良雄
    • Organizer
      創薬懇話会2017 in 加賀
    • Related Report
      2017 Annual Research Report
  • [Presentation] ジケトピペラジン型有糸分裂阻害剤KPU-300の構造活性相関研究2016

    • Author(s)
      林 良樹、六車 共平、臼井 健郎、林 良雄
    • Organizer
      第20回日本がん分子標的治療学会学術集会
    • Place of Presentation
      別府国際コンベンションセンター、大分
    • Year and Date
      2016-05-30
    • Related Report
      2016 Research-status Report

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Published: 2016-04-21   Modified: 2019-03-29  

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