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Identification of artificial ubiquitin compounds and their application study

Research Project

Project/Area Number 17K08367
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Drug development chemistry
Research InstitutionKyoto Prefectural University of Medicine

Principal Investigator

Itoh Yukihiro  京都府立医科大学, 医学(系)研究科(研究院), 准教授 (30636402)

Project Period (FY) 2017-04-01 – 2020-03-31
Project Status Completed (Fiscal Year 2019)
Budget Amount *help
¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2019: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2018: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2017: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Keywords創薬化学 / 分子設計 / ケミカルバイオロジー / ドラッグデザイン / 低分子化合物
Outline of Final Research Achievements

It has been reported that protein ubiquitination plays an important role for regulation of biological functions. However, it is difficult to analyze protein ubiquitination in cell. In this study, we attempted to identify artificial ubiquitin compounds for development of the method to detect and to quantify cellular levels of protein ubiquitination. As a result, we identified compounds recognized as substrates by ubiquitin activating enzyme like a ubiquitin molecule.

Academic Significance and Societal Importance of the Research Achievements

タンパク質のユビキチン化異常はがんや神経変性疾患などに関与し、死や健康寿命低下の一因となっていることも多数報告されている。そのため、細胞レベルでユビキチン化タンパク質を検出・定量する方法が求められている。本研究では、タンパク質のユビキチン化を検出するための足掛かりとなる人工ユビキチン化合物の創製に着手した。その結果、ユビキチンのようにユビキチン活性化酵素に認識されることが示唆された化合物の創製に成功した。

Report

(4 results)
  • 2019 Annual Research Report   Final Research Report ( PDF )
  • 2018 Research-status Report
  • 2017 Research-status Report
  • Research Products

    (6 results)

All 2020 2019 2018

All Journal Article (3 results) (of which Int'l Joint Research: 1 results,  Peer Reviewed: 3 results) Presentation (3 results) (of which Invited: 2 results)

  • [Journal Article] Drug Discovery Researches on Modulators of Lysine-Modifying Enzymes Based on Strategic Chemistry Approaches2020

    • Author(s)
      Itoh Yukihiro
    • Journal Title

      Chemical and Pharmaceutical Bulletin

      Volume: 68 Issue: 1 Pages: 34-45

    • DOI

      10.1248/cpb.c19-00741

    • NAID

      130007778877

    • ISSN
      0009-2363, 1347-5223
    • Year and Date
      2020-01-01
    • Related Report
      2019 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Chemical Protein Degradation Approach and its Application to Epigenetic Targets2018

    • Author(s)
      Itoh Yukihiro
    • Journal Title

      The Chemical Record

      Volume: 18 Issue: 12 Pages: 1681-1700

    • DOI

      10.1002/tcr.201800032

    • Related Report
      2018 Research-status Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Design, synthesis, and biological evaluation of novel ubiquitin-activating enzyme inhibitors2018

    • Author(s)
      Itoh Yukihiro、Suzuki Miki
    • Journal Title

      Bioorganic & Medicinal Chemistry Letters

      Volume: 印刷中 Issue: 16 Pages: 2723-2727

    • DOI

      10.1016/j.bmcl.2018.03.004

    • Related Report
      2017 Research-status Report
    • Peer Reviewed
  • [Presentation] 合理的な分子設計と独特な創薬方法論が導くリシン修飾酵素制御化合物の創製2019

    • Author(s)
      伊藤幸裕
    • Organizer
      日本薬学会 第139年会
    • Related Report
      2018 Research-status Report
    • Invited
  • [Presentation] 新規ユビキチン活性化酵素阻害薬の創製2018

    • Author(s)
      伊藤幸裕、鈴木美紀
    • Organizer
      第36回メディシナルケミストリーシンポジウム
    • Related Report
      2018 Research-status Report
  • [Presentation] リシン 修飾酵素を制御する低分子化合物の 修飾酵素を制御する低分子化合物の 修飾酵素を制御する低分子化合物の 創製 ~化学 的発想を活かした創薬~2018

    • Author(s)
      伊藤幸裕
    • Organizer
      第4回近畿薬学シンポジウム:化学系の若い力
    • Related Report
      2018 Research-status Report
    • Invited

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Published: 2017-04-28   Modified: 2021-02-19  

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