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Development of molecular probe for GST

Research Project

Project/Area Number 15K12751
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeMulti-year Fund
Research Field Chemical biology
Research InstitutionNagoya University

Principal Investigator

Abe Hiroshi  名古屋大学, 理学研究科, 教授 (80415067)

Project Period (FY) 2015-04-01 – 2017-03-31
Project Status Completed (Fiscal Year 2016)
Budget Amount *help
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2016: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2015: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywords酵素 / 生理活性 / イメージング / グルタチオントランスフェラーゼ / 蛍光 / グルタチオン / プローブ
Outline of Final Research Achievements

Glutathione S transferase (GST) is one of highly expressed enzymes in cancer cells. The subtype of this enzyme depends on the cancer species. Tough the determination of the cancer species by detecting GST subtype is thought to contribute to cancer therapy, the GST probe with subtype specificity remains to be developed. As fundamental step for developing the subtype-specific probe, glutathione derivatives were designed and synthesized and those subtype specificities were evaluated.
We synthesize glutathione derivatives with fluorescent group or the functional group forming covalent bond with amino-acid residue. Using this derivative, we discovered the structure for the subtype-specificity. In addition, we succeeded in a synthesis of derivatives with several chemical groups at glycine residue in glutathione without reduction of GST binding ability. These results are thought to promote the development of probes with GST substrate specificity.

Report

(3 results)
  • 2016 Annual Research Report   Final Research Report ( PDF )
  • 2015 Research-status Report
  • Research Products

    (17 results)

All 2017 2016

All Journal Article (4 results) (of which Int'l Joint Research: 3 results,  Peer Reviewed: 3 results,  Acknowledgement Compliant: 2 results) Presentation (12 results) Patent(Industrial Property Rights) (1 results) (of which Overseas: 1 results)

  • [Journal Article] Diastereoselective Synthesis of 6" (Z)- and 6" (E) Fluoro Analogues of Anti-hepatitis B Virus Agent Entecavir and Its Evaluation of the Activity and Toxicity Profile of the Diastereomers2016

    • Author(s)
      Hiroki Kumamoto, Misato Fukano, Tomohiko Nakano, Keito Iwagami, Chiaki Takeyama, Satoru Kohgo, Shuhei Imoto, Masayuki Amano, Nobuyo Kuwata-Higashi, Manabu Aoki, Hiroshi Abe, Hiroaki Mitsuya, Kiyoshi Fukuhara, Kazuhiro Haraguchi
    • Journal Title

      Journal of Organic Chemistry

      Volume: 81 Issue: 7 Pages: 2827-2836

    • DOI

      10.1021/acs.joc.6b00105

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Catalytic Conversion of Lipophilic Substrates by Phase constrained Enzymes in the Aqueous or in the Membrane Phase2016

    • Author(s)
      Marcus Cebula, Ilke Simsek Turan, Birgitta Sjoudin, Madhuranayaki Thulasingam, Joseph Brock, Volodymyr Chmyrov, Jerker Widengren, Hiroshi Abe, Bengt Mannervik, Jesper Haeggstroum, Agnes Rinaldo-Matthis, Engin Akkaya, Ralf Morgenstern
    • Journal Title

      Scientific Reports

      Volume: 6 Issue: 1 Pages: 38316-38316

    • DOI

      10.1038/srep38316

    • Related Report
      2016 Annual Research Report
    • Int'l Joint Research
  • [Journal Article] Design and Synthesis of Cyclopropane Congeners of Resolvin E2, an Endogenous Proresolving Lipid Mediator, as Its Stable Equivalents2016

    • Author(s)
      Fukuda, H; Muromoto, R.; Takakura, Y.; Ishimura, K.; Kanada, R.; Fushihara, D.; Tanabe, M.; Matsubara, K.; Hirao, T.; Hirashima, K.; Abe, Arisawa, M.; Matsuda, T.; Shuto, S.
    • Journal Title

      Org. Lett.

      Volume: 18 Issue: 24 Pages: 6224-6227

    • DOI

      10.1021/acs.orglett.6b02612

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Int'l Joint Research / Acknowledgement Compliant
  • [Journal Article] A chemical reactivity window determines prodrug efficiency towards glutathione transferase overexpressing cancer cells2016

    • Author(s)
      Van Gisbergen, Marik, et.al.
    • Journal Title

      Molecular Pharmaceutics

      Volume: x Issue: 6 Pages: 2010-2025

    • DOI

      10.1021/acs.molpharmaceut.6b00140

    • Related Report
      2015 Research-status Report
    • Peer Reviewed / Int'l Joint Research / Acknowledgement Compliant
  • [Presentation] 高効率な核酸検出を可能にする核酸鋳型反応の開発2017

    • Author(s)
      伊藤 真央, 柴田 綾, 阿部 奈保子, 木村 康明、阿部 洋
    • Organizer
      日本薬学会第137年会
    • Place of Presentation
      仙台
    • Year and Date
      2017-03-24
    • Related Report
      2016 Annual Research Report
  • [Presentation] 糖部三員環型ヌクレオシドアナログの創成2017

    • Author(s)
      伏原 大地, 福田 隼, 阿部 洋, 周東 智
    • Organizer
      日本薬学会第137年会
    • Place of Presentation
      仙台
    • Year and Date
      2017-03-24
    • Related Report
      2016 Annual Research Report
  • [Presentation] 共有結合型グルタチオンS-転移酵素阻害剤の創薬研究2017

    • Author(s)
      宍戸 裕子, 藤川 遥加, 木村 康明, 友池 史明, 桑田 啓子, 矢野 貴人, 福井 健二, 関戸 好孝, 村上 優子, 周東 智, 阿部 洋
    • Organizer
      日本薬学会第137年会
    • Place of Presentation
      仙台
    • Year and Date
      2017-03-24
    • Related Report
      2016 Annual Research Report
  • [Presentation] 求電子的ホスホロチオエステルによる核酸の化学的連結反応2017

    • Author(s)
      木村 康明, 丸山豪斗, 笈川涼太, 早川真由, 阿部奈保子, 松田彰, 周東智, 伊藤嘉浩, 阿部洋
    • Organizer
      日本化学会第97春季年会
    • Place of Presentation
      横浜
    • Year and Date
      2017-03-16
    • Related Report
      2016 Annual Research Report
  • [Presentation] ビルドアップ型核酸分子の開発2017

    • Author(s)
      吉永 静也, 辻 厳一郎, 阿部 奈保子, 友池 史明, 木村 康明, 阿部 洋
    • Organizer
      統合物質創製化学研究推進機構 第2回国内シンポジウム
    • Place of Presentation
      北海道
    • Year and Date
      2017-01-26
    • Related Report
      2016 Annual Research Report
  • [Presentation] 光解除性保護基を有するヌクレオシドを利用した長鎖RNAのケミカルライゲーション2017

    • Author(s)
      辻 厳一郎, 笈川涼太, 早川真由, 木村康明, 阿部洋
    • Organizer
      統合物質創製化学研究推進機構 第2回国内シンポジウム
    • Place of Presentation
      北海道
    • Year and Date
      2017-01-26
    • Related Report
      2016 Annual Research Report
  • [Presentation] 共有結合型グルタチオン S-転移酵素阻害剤の創薬研究2016

    • Author(s)
      宍戸 裕子, 藤川 遥加, 木村 康明, 友池 史明, 桑田 啓子, 矢野 貴人, 福井 健二, 関戸 好孝, 村上 優子, 周東 智, 阿部 洋
    • Organizer
      第34回 メデシナルケミストリーシンポジウム
    • Place of Presentation
      つくば
    • Year and Date
      2016-11-30
    • Related Report
      2016 Annual Research Report
  • [Presentation] 合成環状RNAからのタンパク質発現2016

    • Author(s)
      児玉 亜有実, 阿部 奈保子, 友池 史明, 伊藤 嘉浩, 松本 健, 吉田 稔, 清水 義宏, 亀田 倫史, 阿部 洋
    • Organizer
      第39回 分子生物学会
    • Place of Presentation
      横浜
    • Year and Date
      2016-11-30
    • Related Report
      2016 Annual Research Report
  • [Presentation] 細胞内ビルドアップ型SiRNAを指向した新規核酸連結反応2016

    • Author(s)
      早川 真由, 笈川 涼太, 丸山 豪斗, 阿部 奈保子, 木村 康明, 周東 智, 松田 彰, 阿部 洋
    • Organizer
      日本核酸医薬学会第二回年会
    • Place of Presentation
      東京
    • Year and Date
      2016-11-15
    • Related Report
      2016 Annual Research Report
  • [Presentation] Development of novel chemical ligation reaction for RNA strands2016

    • Author(s)
      笈川 涼太, 丸山 豪斗, 早川 真由, 阿部 奈保子, 木村 康明, 阿部 洋
    • Organizer
      第43回 国際核酸化学シンポジウム
    • Place of Presentation
      熊本
    • Year and Date
      2016-09-27
    • Related Report
      2016 Annual Research Report
  • [Presentation] Nile Blueを基本骨格とした脂肪滴検出プローブの創製2016

    • Author(s)
      戸田 直宏, 伊藤 美香, 石田 綾乃, 鬼頭 宏任, 横川 大輔, Stephan Irle, 木村 康明, 友池 史明, 西村 智, 阿部 洋
    • Organizer
      第31回生体機能関連化学シンポジウム
    • Place of Presentation
      金沢
    • Year and Date
      2016-09-07
    • Related Report
      2016 Annual Research Report
  • [Presentation] Si-Si結合の特性を利用した光分解性保護基の開発2016

    • Author(s)
      伊藤 真央, 金田 龍太郎, 木村 康明, 周東 智, 阿部 洋
    • Organizer
      第31回生体機能関連化学シンポジウム
    • Place of Presentation
      金沢
    • Year and Date
      2016-09-07
    • Related Report
      2016 Annual Research Report
  • [Patent(Industrial Property Rights)] グルタチオンS-トランスフェラーゼ阻害剤2016

    • Inventor(s)
      阿部洋、宍戸裕子
    • Industrial Property Rights Holder
      阿部洋、宍戸裕子
    • Industrial Property Rights Type
      特許
    • Filing Date
      2016-07-05
    • Related Report
      2016 Annual Research Report
    • Overseas

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Published: 2015-04-16   Modified: 2018-03-22  

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