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Search for specific inhibitors of the ubiquitin-conjugating enzyme E2

Research Project

Project/Area Number 26670047
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeMulti-year Fund
Research Field Natural medicines
Research InstitutionKumamoto University

Principal Investigator

Tsukamoto Sachiko  熊本大学, 生命科学研究部(薬), 教授 (40192190)

Co-Investigator(Renkei-kenkyūsha) YOKOSAWA Hideyoshi  愛知学院大学, 薬学部, 教授 (90012765)
Project Period (FY) 2014-04-01 – 2016-03-31
Project Status Completed (Fiscal Year 2015)
Budget Amount *help
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2015: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2014: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywordsユビキチン結合酵素E2 / UBE2S / Ubc13 / ユビキチン修飾系 / E2
Outline of Final Research Achievements

Ubiquitin chain in different topologies related to distinct functional consequences, including protein degradation, NF-κB activation, and DNA repair. The ubiquitin chain assembly is mostly promoted by E2s, but the linkage specificity by E2s is hardly understood. In this study, we searched for UBE2S inhibitors from natural sources as bio-probes to study the mechanisms of K11-ubiquitin chain elongation. We established the in-house screening system for UBE2S inhibitors and found the several positive extracts from our library of extracts of natural sources. The isolation and structure determination of the inhibitors are in progress.

Report

(3 results)
  • 2015 Annual Research Report   Final Research Report ( PDF )
  • 2014 Research-status Report
  • Research Products

    (7 results)

All 2016 2015 Other

All Int'l Joint Research (1 results) Journal Article (1 results) (of which Peer Reviewed: 1 results,  Open Access: 1 results) Presentation (4 results) (of which Int'l Joint Research: 2 results,  Invited: 4 results) Remarks (1 results)

  • [Int'l Joint Research] Sam Ratulangi University(Indonesia)

    • Related Report
      2015 Annual Research Report
  • [Journal Article] Search for Inhibitors of the Ubiquitin–Proteasome System from Natural Sources for Cancer Therapy2016

    • Author(s)
      S. Tsukamoto
    • Journal Title

      Chemical and Pharmaceutical Bulletin

      Volume: 64 Issue: 2 Pages: 112-118

    • DOI

      10.1248/cpb.c15-00768

    • NAID

      130005121724

    • ISSN
      0009-2363, 1347-5223
    • Related Report
      2015 Annual Research Report
    • Peer Reviewed / Open Access
  • [Presentation] p53を安定化させる脱ユビキチン化酵素USP7阻害物質の探索2016

    • Author(s)
      塚本佐知子
    • Organizer
      日本薬学会第136年会シンポジウム「創薬研究における天然物化学のミッションと新潮流」
    • Place of Presentation
      横浜(パシフィコ横浜)
    • Year and Date
      2016-03-26
    • Related Report
      2015 Annual Research Report
    • Invited
  • [Presentation] Drug discovery targeting the ubiquitin-proteasome system from marine organisms2015

    • Author(s)
      Sachiko Tsukamoto
    • Organizer
      PACIFICHEM 2015
    • Place of Presentation
      Honolulu (USA) (Hilton Hawaiian Village)
    • Year and Date
      2015-12-15
    • Related Report
      2015 Annual Research Report
    • Int'l Joint Research / Invited
  • [Presentation] 海洋生物は薬用資源の宝庫2015

    • Author(s)
      塚本佐知子
    • Organizer
      平成27年度熊本大学東京オフィスセミナー「天然物創薬のフロンティア~熊本大学から世界に発信する拠点形成研究~」
    • Place of Presentation
      東京(東京工業大学キャンパスイノベーションセンター1階 国際会議室)
    • Year and Date
      2015-11-23
    • Related Report
      2015 Annual Research Report
    • Invited
  • [Presentation] Search for inhibitors of the ubiquitin-proteasome system from the natural sources for drug development2015

    • Author(s)
      Sachiko Tsukamoto
    • Organizer
      Organic Seminar in Colorado State University
    • Place of Presentation
      Fort Collins (CO, USA) (Colorado State University)
    • Year and Date
      2015-07-24
    • Related Report
      2015 Annual Research Report
    • Int'l Joint Research / Invited
  • [Remarks] 熊本大学大学院生命科学研究部天然薬物学分野ホームページ

    • URL

      http://kumamoto-natmed.net/index.html

    • Related Report
      2015 Annual Research Report 2014 Research-status Report

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Published: 2014-04-04   Modified: 2019-04-12  

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