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Discovery of drug candidates by using in situ click chemistry

Research Project

Project/Area Number 24689007
Research Category

Grant-in-Aid for Young Scientists (A)

Allocation TypePartial Multi-year Fund
Research Field Drug development chemistry
Research InstitutionKyoto Prefectural University of Medicine

Principal Investigator

SUZUKI Takayoshi  京都府立医科大学, 医学(系)研究科(研究院), 教授 (90372838)

Project Period (FY) 2012-04-01 – 2015-03-31
Project Status Completed (Fiscal Year 2014)
Budget Amount *help
¥26,520,000 (Direct Cost: ¥20,400,000、Indirect Cost: ¥6,120,000)
Fiscal Year 2014: ¥8,580,000 (Direct Cost: ¥6,600,000、Indirect Cost: ¥1,980,000)
Fiscal Year 2013: ¥8,450,000 (Direct Cost: ¥6,500,000、Indirect Cost: ¥1,950,000)
Fiscal Year 2012: ¥9,490,000 (Direct Cost: ¥7,300,000、Indirect Cost: ¥2,190,000)
Keywordsヒストン脱アセチル化酵素 / アイソフォーム / クリックケミストリー / アジド / アルキン / トリアゾール / 阻害薬 / リシン脱アセチル化酵素 / アイソザイム
Outline of Final Research Achievements

In drug discovery, high-throughput screening, structure-based drug design, and ligand-based drug design are generally used. However, these methods take great time and effort.
With the background like this, we tried to identify selective inhibitors using click chemistry. As a result, we rapidly identified promising inhibitors by this method, suggesting the usefulness of this method in drug discovery.

Report

(4 results)
  • 2014 Annual Research Report   Final Research Report ( PDF )
  • 2013 Annual Research Report
  • 2012 Annual Research Report
  • Research Products

    (13 results)

All 2015 2014 2013 2012 Other

All Journal Article (6 results) (of which Peer Reviewed: 6 results,  Acknowledgement Compliant: 1 results) Presentation (5 results) (of which Invited: 2 results) Remarks (2 results)

  • [Journal Article] Identification of Novel SIRT2-Selective Inhibitors Using a Click Chemistry Approach2014

    • Author(s)
      109. Prima R. Tatum, Hideyuki Sawada, Yosuke Ota, Yukihiro Itoh, Peng Zhan, Naoya Ieda, Hidehiko Nakagawa, Naoki Miyata, Takayoshi Suzuki.
    • Journal Title

      Bioorg. Med. Chem. Lett

      Volume: 24 Issue: 8 Pages: 1871-1874

    • DOI

      10.1016/j.bmcl.2014.03.026

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Target-guided Synthesis: Medicinal Chemistry Strategy to Allow Target Enzymes Themselves to Synthesize their Own Inhibitors2014

    • Author(s)
      Yukihiro Itoh, Naoki Miyata, Takayoshi Suzuki
    • Journal Title

      J. Syn. Org. Chem. Jpn.

      Volume: 72 Pages: 702-716

    • NAID

      130004548618

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Design, Synthesis, and Biological Activity of NCC149 Derivatives as Histone Deacetylase 8-Selective Inhibitors.2014

    • Author(s)
      Suzuki T, Muto N, Bando M, Itoh Y, Masaki A, Ri M, Ota Y, Nakagawa H, Iida S, Shirahige K, Miyata N.
    • Journal Title

      ChemMedChem.

      Volume: 9 Issue: 3 Pages: 657-664

    • DOI

      10.1002/cmdc.201300414

    • Related Report
      2013 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Identification of Highly Selective and Potent Histone Deacetylase 3 Inhibitors Using Click Chemistry-Based Combinatorial Fragment Assembly2013

    • Author(s)
      98. Takayoshi Suzuki, Yuki Kasuya, Yukihiro Itoh, Yosuke Ota, Peng Zhan, Kaori Asamitsu, Hidehiko Nakagawa, Takashi Okamoto and Naoki Miyata.
    • Journal Title

      PLoS One

      Volume: 8 Issue: 7 Pages: e68669-e68669

    • DOI

      10.1371/journal.pone.0068669

    • Related Report
      2013 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Small-molecular modulators of cancer-related epigenetic mechanisms2013

    • Author(s)
      Yukihiro Itoh , Takayoshi Suzuki and Naoki Miyata
    • Journal Title

      Mol. Biosyst.

      Volume: 9 Issue: 5 Pages: 873-896

    • DOI

      10.1039/c3mb25410k

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Rapid Discovery of Highly Potent and Selective Inhibitors of Histone Deacetylase 8 Using Click Chemistry to Generate Candidate Libraries2012

    • Author(s)
      Takayoshi Suzuki, Yosuke Ota, Masaki Ri, Masashige Bando, Aogu Gotoh, Yukihiro Itoh, Hiroki Tsumoto, Prima R. Tatum, Tamio Mizukami, Hidehiko Nakagawa, Shinsuke Iida, Ryuzo Ueda, Katsuhiko Shirahige, and Naoki Miyata.
    • Journal Title

      J. Med. Chem.

      Volume: 55 Issue: 22 Pages: 9562-9575

    • DOI

      10.1021/jm300837y

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Presentation] 創薬を目指したエピジェネティクス制御化合物の創製2015

    • Author(s)
      鈴木孝禎
    • Organizer
      天然物ケミカルバイオロジー地区シンポジウム
    • Place of Presentation
      東北大学
    • Year and Date
      2015-01-15
    • Related Report
      2014 Annual Research Report
    • Invited
  • [Presentation] エピジェネティクスのケミカルコントロール2014

    • Author(s)
      鈴木孝禎
    • Organizer
      第18回スクリプス・バイオメディカルフォーラム
    • Place of Presentation
      大阪
    • Year and Date
      2014-11-22
    • Related Report
      2014 Annual Research Report
    • Invited
  • [Presentation] エピジェネティクス制御化合物の開発2014

    • Author(s)
      鈴木孝禎
    • Organizer
      第87回 日本生化学会大会
    • Place of Presentation
      京都国際会館
    • Year and Date
      2014-10-15
    • Related Report
      2014 Annual Research Report
  • [Presentation] クリックケミストリーを用いたHDAC阻害薬の探索研究2013

    • Author(s)
      後藤仰、鈴木孝禎, 他
    • Organizer
      日本薬学会 第133年会
    • Place of Presentation
      パシフィコ横浜(神奈川県)
    • Year and Date
      2013-03-29
    • Related Report
      2012 Annual Research Report
  • [Presentation] Identification of HDAC3-Selective Inhibitors Using Click Chemistry-Based Combinatorial Fragment Assembly2013

    • Author(s)
      Yosuke Ota, Takayoshi Suzuki et al
    • Organizer
      2nd Annual Conference ICBS2013
    • Place of Presentation
      京都大学(京都市)
    • Related Report
      2013 Annual Research Report
  • [Remarks] 京都府立医科大学医薬品化学研究室HP

    • URL

      http://www.kpu-m.ac.jp/y/chemistry/publications.html

    • Related Report
      2013 Annual Research Report
  • [Remarks]

    • URL

      http://www.kpu-m.ac.jp/y/chemistry/publications.html

    • Related Report
      2012 Annual Research Report

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Published: 2012-04-24   Modified: 2019-07-29  

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