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Mechanistic study on the Bradykinin B1 receptor

Research Project

Project/Area Number 20710172
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeSingle-year Grants
Research Field Living organism molecular science
Research InstitutionNigata University of Phermacy and Applied Life Sciences

Principal Investigator

TAMIYA Minoru  Nigata University of Phermacy and Applied Life Sciences, 応用生命科学部, 助教 (10468960)

Project Period (FY) 2008 – 2009
Project Status Completed (Fiscal Year 2009)
Budget Amount *help
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2009: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2008: ¥2,600,000 (Direct Cost: ¥2,000,000、Indirect Cost: ¥600,000)
Keywords有機合成 / コンピュータシミュレーション
Research Abstract

The Bradykinin B1 receptor (B1R), belonging to GPCR family, plays an important role in the pathophysiological process of pain and inflammation. Because of these reasons, we aimed to the clarification of the mechanism of action of B1R. First, we constructed the structural models of the B1 receptor. Then, velutinol A was docked in the models of the B1 receptor, followed by energy-minimization and structure-optimization with molecular dynamic calculations. From this docking simulation, we could anticipate the important substituent of velutinol A for the binding to B1R. On the other hand, we have also started the synthesis of velutinol A. Finally we could synthesize the key intermediate for the following synthesis and SAR study. Now we are pushing on the total synthesis of velutinol A and its analogs for the study of mechanism of action of B1R.

Report

(3 results)
  • 2009 Annual Research Report   Final Research Report ( PDF )
  • 2008 Annual Research Report
  • Research Products

    (16 results)

All 2009 2008 Other

All Journal Article (2 results) (of which Peer Reviewed: 2 results) Presentation (14 results)

  • [Journal Article] Total Synthesis of Amphidinolide B1, B4, G1, H1 and Structure Revision of Amphidinolide H22009

    • Author(s)
      A. Farstner, L. C. Bouchez, L. Morency, J. -A. Funel, V. Liepins, F. -H. Pored, R. Gilmour, F. Eleaufi Is, D. Laurich, F. BeaufiIs, M. Tamiya
    • Journal Title

      Chemistry A European Journal 15

      Pages: 3983-4010

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Enthusiastic Renovation of Laboratory and Bench2008

    • Author(s)
      田宮実
    • Journal Title

      有機合成化学 66

      Pages: 808-809

    • NAID

      10024278567

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed
  • [Presentation] Velutinol Aの合成研究(口頭発表)2009

    • Author(s)
      ○井坂修久、高田楓太、田宮実、米田照代、石黒正路
    • Organizer
      第58回有機合成化学協会関東支部シンポジウム
    • Place of Presentation
      長岡技術化学大学
    • Year and Date
      2009-11-28
    • Related Report
      2009 Final Research Report
  • [Presentation] Velutinol Aの合成研究(口頭発表)2009

    • Author(s)
      ○井坂修久、高田楓太、田宮実、米田照代、石黒正路
    • Organizer
      日本薬学会第129年会
    • Place of Presentation
      国立京都国際会館
    • Year and Date
      2009-03-28
    • Related Report
      2009 Final Research Report
  • [Presentation] ATR阻害剤ゴミシン, シザンドリン類縁体の合成研究2009

    • Author(s)
      五十嵐久未、田宮実、熊倉美佳、米田照代、石黒正路
    • Organizer
      日本薬学会第129年会
    • Place of Presentation
      国立泉区国祭会館
    • Year and Date
      2009-03-28
    • Related Report
      2008 Annual Research Report
  • [Presentation] Velutinol Aの含成研究2009

    • Author(s)
      井坂修久、高田楓太、田宮実、米田照代、石黒正路
    • Organizer
      日本薬学会129年会
    • Place of Presentation
      国立京都国際会館
    • Year and Date
      2009-03-28
    • Related Report
      2008 Annual Research Report
  • [Presentation] 核酸塩基を側鎖に持つペプチド誘導体の合成研究2009

    • Author(s)
      井坂修久、安達晃弘、納富勇輔、田宮実、米田照代、石黒正路
    • Organizer
      日本薬学会第129年会
    • Place of Presentation
      国立京都国際会館
    • Year and Date
      2009-03-26
    • Related Report
      2008 Annual Research Report
  • [Presentation] Velutinol Aの合成研究2009

    • Author(s)
      井坂修久、田宮実
    • Organizer
      有機合成化学協会関東支部シンポジウム
    • Place of Presentation
      長岡
    • Related Report
      2009 Annual Research Report
  • [Presentation] ペプチド核酸の合成研究2009

    • Author(s)
      田宮佳奈、田宮実
    • Organizer
      有機合成化学協会関東支部シンポジウム
    • Place of Presentation
      長岡
    • Related Report
      2009 Annual Research Report
  • [Presentation] ATRフロテインキナーゼ阻害剤シザンドリン、ゴミシン類の合成研究2008

    • Author(s)
      熊倉美佳、田宮実、五十嵐久未、米田照代、石黒正路
    • Organizer
      第56回有機合成化学協会関部シンポジウム
    • Place of Presentation
      新潟大学工学部
    • Year and Date
      2008-11-29
    • Related Report
      2008 Annual Research Report
  • [Presentation] Structural Models for Bradykinin B1 Receptor-ligand Complexes(ポスター発表)2008

    • Author(s)
      ○井坂修久、安達晃弘、納富勇輔、田宮実、米田照代、石黒正路
    • Organizer
      The Eighth China-Japan Joint Symposium On Drug and Development
    • Place of Presentation
      神戸国際会議場
    • Year and Date
      2008-11-03
    • Related Report
      2009 Final Research Report
  • [Presentation] Structural Models for Bradykinin B1 R eceptor-ligand Complexes2008

    • Author(s)
      井坂修久、安達晃弘、納富勇輔、田宮、米田照代、石黒正路
    • Organizer
      The Eighth China -Japan Joint Symposium On Drug and Development
    • Place of Presentation
      戸国際会議場
    • Year and Date
      2008-11-03
    • Related Report
      2008 Annual Research Report
  • [Presentation] ブラジキニンB1およびB2受容体とリガンドの複合モデリングによる相互作用の解析(ポスター発表)2008

    • Author(s)
      井坂修久、○安達晃弘、納富勇輔、田宮実、米田照代、石黒正路
    • Organizer
      第36回構造活性相関シンポジウム
    • Place of Presentation
      神戸国際会議場
    • Year and Date
      2008-11-02
    • Related Report
      2009 Final Research Report
  • [Presentation] ブラジキニンB1およびB2受谷とリカンドの複合モデリングによる相互作用の解析2008

    • Author(s)
      井坂修久、安達晃弘、納富勇輔、田宮実、米田照代、石黒正路
    • Organizer
      36回構造活性相関シンポジウム
    • Place of Presentation
      戸国際会議場
    • Year and Date
      2008-11-02
    • Related Report
      2008 Annual Research Report
  • [Presentation] Amphidinolide Bの合成研究2008

    • Author(s)
      田宮実、A, Furstner、 L. C. Bouchez、J.-A Funel、 V. Liepins、 F.-H. Poree、 R. Gilmour、 F. Beaufils、 D. Laurich
    • Organizer
      第55回有機合成化学協会関部シンホジウム
    • Place of Presentation
      東京理科大学野田キャンパス薬学校舎
    • Year and Date
      2008-05-10
    • Related Report
      2008 Annual Research Report
  • [Presentation] パラジウムを用いた新規Baeyer-Villiger型環拡大反応

    • Author(s)
      高田楓太、田宮実
    • Organizer
      日本薬学会第130年会
    • Place of Presentation
      岡山
    • Related Report
      2009 Annual Research Report

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Published: 2008-04-01   Modified: 2016-04-21  

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