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Development of the method for screening histone methyl transferase inhibitors utilizing the novel fluorescent probe.

Research Project

Project/Area Number 23790127
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeMulti-year Fund
Research Field Drug development chemistry
Research InstitutionTokyo Medical and Dental University

Principal Investigator

MORI Shuichi  東京医科歯科大学, 生体材料工学研究所, 特任助教 (00467630)

Project Period (FY) 2011 – 2012
Project Status Completed (Fiscal Year 2012)
Budget Amount *help
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2012: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2011: ¥3,250,000 (Direct Cost: ¥2,500,000、Indirect Cost: ¥750,000)
Keywordsエピジェネティクス / ヒストンメチル化酵素 / SNAr反応 / 蛍光プローブ / ヒストンメチル化
Research Abstract

Histone methyltransferase (HMT) plays important roles in physiological conditions. Selective inhibitors of HMT are expected as potent drug candidate. In this study, we developed the inexpensive and easy method to evaluate the HMT activity, which is helpful in developing the HMT inhibitors. We succeeded in estimating the amount of methylated lysine which is the product of HMT-catalyzed reaction, by discriminating the difference of chemical property-between of lysine and of methylated lysine. Furthermore, we tried to develop the method for highly sensitive detection of methylated lysine based on the fluorescent response reflecting the chemical property of methylated lysine.

Report

(3 results)
  • 2012 Annual Research Report   Final Research Report ( PDF )
  • 2011 Research-status Report
  • Research Products

    (10 results)

All 2013 2012 2011

All Journal Article (1 results) (of which Peer Reviewed: 1 results) Presentation (9 results)

  • [Journal Article] 6-Arylcoumarins as novel nonsteroidal type progesterone antagonists : An example with receptor-binding-dependent fluorescence2011

    • Author(s)
      Sakai, H.
    • Journal Title

      J.Med.Chem.

      Volume: 54 Issue: 20 Pages: 7055-7065

    • DOI

      10.1021/jm2005404

    • Related Report
      2011 Research-status Report
    • Peer Reviewed
  • [Presentation] Discrimination between lysine and N-〓-methyllysine using SNAr reactions2013

    • Author(s)
      Shuichi Mori
    • Organizer
      The 2nd HD Physiology International Symposium
    • Place of Presentation
      Tokyo
    • Year and Date
      2013-06-29
    • Related Report
      2012 Final Research Report
  • [Presentation] SNAr反応を利用したリジン・メチル化リジンの識別2013

    • Author(s)
      高口明日香
    • Organizer
      日本薬学会第133年会
    • Place of Presentation
      横浜
    • Year and Date
      2013-03-29
    • Related Report
      2012 Final Research Report
  • [Presentation] SNAr反応を利用したリジン・メチル化リジンの識別2013

    • Author(s)
      藤原敬士
    • Organizer
      日本ケミカルバイオロジー学会第八回年会
    • Place of Presentation
      東京
    • Related Report
      2012 Annual Research Report 2012 Final Research Report
  • [Presentation] SNAr反応を利用したリジン・メチル化リジンの識別2013

    • Author(s)
      高口明日香、森修一、平野智也、影近弘之
    • Organizer
      日本薬学会 第133年会
    • Place of Presentation
      横浜
    • Related Report
      2012 Annual Research Report
  • [Presentation] Discrimination between lysine and N--methyllysine using SNAr reactions2013

    • Author(s)
      Shuichi Mori, Takashi Fujiwara, Asuka Takaguchi, Tomoya Hirano, Hiroyuki Kagechika
    • Organizer
      The 2nd HD Physiology International Symposium
    • Place of Presentation
      東京
    • Related Report
      2012 Annual Research Report
  • [Presentation] リジンとメチル化リジンのSNAr反応における反応性の検討2012

    • Organizer
      日本薬学会第133年会
    • Place of Presentation
      札幌
    • Year and Date
      2012-03-30
    • Related Report
      2012 Final Research Report
  • [Presentation] ホウ素クラスター含有二級アルコールのリパーゼによる光学分割2012

    • Author(s)
      高垣亮平
    • Organizer
      日本化学会
    • Place of Presentation
      横浜
    • Related Report
      2011 Research-status Report
  • [Presentation] リジンとメチル化リジンのSNAr 反応における反応性の検討2012

    • Author(s)
      高口明日香
    • Organizer
      日本薬学会
    • Place of Presentation
      札幌
    • Related Report
      2011 Research-status Report
  • [Presentation] Development of Novel Bisubstrate-Type Inhibitor of Histone Methyltransferase SET7/92011

    • Author(s)
      Mori, S.
    • Organizer
      AIMECS
    • Place of Presentation
      東京
    • Related Report
      2011 Research-status Report

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Published: 2011-08-05   Modified: 2019-07-29  

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