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Analysis of molecular targets and development into drug discovery for cyclic peptides possessing thrombolysis-enhancing action

Research Project

Project/Area Number 26350969
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Chemical biology
Research InstitutionAkita University

Principal Investigator

KOIZUMI Yukio  秋田大学, 医学(系)研究科(研究院), 助教 (80353465)

Co-Investigator(Kenkyū-buntansha) 長井 賢一郎  北里大学, 薬学部, 助教 (30321649)
Project Period (FY) 2014-04-01 – 2017-03-31
Project Status Completed (Fiscal Year 2016)
Budget Amount *help
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2016: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2015: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2014: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Keywords抗血栓薬 / 線溶系 / マルホルミン / RSK / ウロキナーゼ / ケミカルバイオロジー / 創薬 / CRISPR/Cas9 / ゲノム編集
Outline of Final Research Achievements

Treatment and prevention of thrombotic diseases such as cerebral infarction and myocardial infarction are extremely important. As a result of searching thrombolysis-enhancing substances using in vitro thrombolytic activity evaluation system, we have discovered cyclic pentapeptide malformin. The purpose of this study is to elucidate the mechanism of action for malformin. In this study, we showed that malformin induces the activation of RSK1, raises the expression of urokinase and promotes fibrinolytic activity via plasminogen activation in plasma fluid. From the results of this study, it is expected to create the next generation thrombolytic agent based on the molecular structure of malformin.

Report

(4 results)
  • 2016 Annual Research Report   Final Research Report ( PDF )
  • 2015 Research-status Report
  • 2014 Research-status Report

Research Products

(10 results)

All 2017 2016 2015 2014 Other

All Int'l Joint Research (1 results) Journal Article (4 results) (of which Int'l Joint Research: 1 results,  Peer Reviewed: 4 results,  Open Access: 3 results,  Acknowledgement Compliant: 2 results) Presentation (5 results)

  • [Int'l Joint Research] Jilin University(中国)

    • Related Report
      2015 Research-status Report
  • [Journal Article] Structure-activity relationship of cyclic pentapeptide malformins as fibrinolysis enhancers.2016

    • Author(s)
      Koizumi Y, Nagai K, Hasumi K, Kuba K, Sugiyama T
    • Journal Title

      Bioorg. Med. Chem. Lett.

      Volume: 26 Pages: 5267-5271

    • DOI

      10.1016/j.bmcl.2016.09.045

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Open Access / Int'l Joint Research / Acknowledgement Compliant
  • [Journal Article] Cadmium-coordinated supramolecule suppresses tumor growth of T-cell leukemia in mice.2015

    • Author(s)
      Zhou X, Koizumi Y, Zhang M, Natsui M, Koyota S, Yamada M, Kondo Y, Hamada F, Sugiyama T
    • Journal Title

      Cancer Sci.

      Volume: 印刷中 Pages: 635-641

    • DOI

      10.1111/cas.12651

    • Related Report
      2015 Research-status Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Journal Article] Stimulation of the hair growth by α2-blocker SST-VED2014

    • Author(s)
      Natsui M, Kawagoe M, Somei M, Koizumi Y, Koyota S, Sugiyama T
    • Journal Title

      Akita J Med

      Volume: 41 Pages: 23-33

    • NAID

      110009839555

    • Related Report
      2014 Research-status Report
    • Peer Reviewed / Open Access
  • [Journal Article] Mangromicins A and B: Structure and Anti-trypanosomal Activity of two new Cyclopentadecane Compounds from Lechevalieria aerocolonigenes K10-02162014

    • Author(s)
      Nakashima T, Iwatsuki M, Ochiai J, Kamiya Y, Nagai K, Matsumoto A, Ishiyama A, Otoguro K, Shiomi K, Takahashi Y, Omura S
    • Journal Title

      J Antibiot

      Volume: 67 Pages: 253-260

    • DOI

      10.1038/ja.2013.129

    • Related Report
      2014 Research-status Report
    • Peer Reviewed
  • [Presentation] ゲノムワイドCRISPR/Cas9ノックアウトライブラリーを用いた細胞毒性耐性遺伝子スクリーニングの試み2017

    • Author(s)
      小泉 幸央、福島 淳、夏井 美幸、門脇 歩美、山口 智和、今井 由美子、久場 敬司
    • Organizer
      日本農芸化学会 2017年度大会
    • Place of Presentation
      京都
    • Year and Date
      2017-03-17
    • Related Report
      2016 Annual Research Report
  • [Presentation] Cnot3によるES細胞の細胞周期制御機構の解析2016

    • Author(s)
      小泉幸央、山口智和、門脇歩美、夏井美幸、佐藤チトセ、今井由美子、久場敬司
    • Organizer
      第89回日本生化学会大会
    • Place of Presentation
      仙台
    • Year and Date
      2016-09-25
    • Related Report
      2016 Annual Research Report
  • [Presentation] CCR4-NOT複合体による心臓のアデニン核酸代謝機構の解析2016

    • Author(s)
      山口智和、鈴木享、佐藤輝紀、夏井美幸、門脇歩美、佐藤チトセ、小泉幸央、高橋明格、山本雅、今井由美子、久場敬司
    • Organizer
      第89回日本薬理学会年会
    • Place of Presentation
      横浜
    • Year and Date
      2016-03-09
    • Related Report
      2015 Research-status Report
  • [Presentation] CCR4-NOT複合体によるアデニン核酸制御機構の解析2015

    • Author(s)
      山口智和、鈴木 享、佐藤輝紀、夏井美幸、門脇歩美、佐藤チトセ、小泉幸央、高橋明格、山本 雅、今井由美子、久場敬司
    • Organizer
      第17回日本RNA学会
    • Place of Presentation
      札幌
    • Year and Date
      2015-07-15
    • Related Report
      2015 Research-status Report
  • [Presentation] CNOT3によるES細胞増殖、初期発生制御の分子機構の解析2015

    • Author(s)
      小泉幸央、山口智和、門脇歩美、夏井美幸、佐藤ちとせ、今井由美子、久場敬司
    • Organizer
      第88回日本薬理学会年会
    • Place of Presentation
      名古屋
    • Year and Date
      2015-03-18 – 2015-03-20
    • Related Report
      2014 Research-status Report

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Published: 2014-04-04   Modified: 2018-03-22  

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