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Chemical biology aimed at the development of new thrombolytics

Research Project

Project/Area Number 20200037
Research Category

Grant-in-Aid for Scientific Research on Innovative Areas (Research a proposed research project)

Allocation TypeSingle-year Grants
Research Field Living organism molecular science
Drug development chemistry
Research InstitutionAkita University

Principal Investigator

KOIZUMI Yukio  秋田大学, 大学院・医学系研究科, 助教 (80353465)

Co-Investigator(Kenkyū-buntansha) NAGAI Kenichiro  北里大学, 薬学部, 助教 (30321649)
Project Period (FY) 2008 – 2010
Project Status Completed (Fiscal Year 2010)
Budget Amount *help
¥25,740,000 (Direct Cost: ¥19,800,000、Indirect Cost: ¥5,940,000)
Fiscal Year 2010: ¥7,020,000 (Direct Cost: ¥5,400,000、Indirect Cost: ¥1,620,000)
Fiscal Year 2009: ¥8,060,000 (Direct Cost: ¥6,200,000、Indirect Cost: ¥1,860,000)
Fiscal Year 2008: ¥10,660,000 (Direct Cost: ¥8,200,000、Indirect Cost: ¥2,460,000)
Keywordsケミカルバイオロジー / 血栓溶解 / 微生物二次代謝産物
Research Abstract

Structure-activity relationships of cyclic pentapeptide, malformin A1 (MA1), showed that the formation of intramolecular disulfide bond and the existence of hydrophobic side-chains were essential for the enhancement of fibrinolysis by MA1. In addition, the correlation between enhancement of fibrinolysis and cytotoxicity was not observed, suggesting that the separation of each activity is possible. The studies using radioisotope-labeling and fluorescence-labeling revealed the intracellular localization of MA1. Moreover, malformin-affinity beads detected 65 kDa and 22 kDa cellular malformin-high affinity proteins.

Report

(4 results)
  • 2010 Annual Research Report   Final Research Report ( PDF )
  • 2009 Annual Research Report
  • 2008 Annual Research Report
  • Research Products

    (25 results)

All 2011 2010 2009

All Journal Article (13 results) (of which Peer Reviewed: 13 results) Presentation (12 results)

  • [Journal Article] Fibrinolytic Activation Promoted by the Cyclopentapeptide Malformin: Involvement of Cytoskeletal Reorganization2011

    • Author(s)
      Koizumi Y, Fukudome H, Hasumi K.
    • Journal Title

      Biological and Pharmaceutical Bulletin

      Volume: 34 Issue: 9 Pages: 1426-1431

    • DOI

      10.1248/bpb.34.1426

    • NAID

      130001872435

    • ISSN
      0918-6158, 1347-5215
    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Sexual dimorphism in LEC rat liver: Suppression of carbonic anhydrase III by copper accumulation during hepatocarcinogenesis2011

    • Author(s)
      Kuhara M, Wang J, Flores MJ, Zhiwei Q, Koizumi Y, Koyota S, Taniguchi N, Sugiyama T.
    • Journal Title

      Biomedical Research

      Volume: 32 Issue: 2 Pages: 111-117

    • DOI

      10.2220/biomedres.32.111

    • NAID

      130004470770

    • ISSN
      0388-6107, 1880-313X
    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Sexual dimorphism in LEC rat liver : Suppression of carbonic anhydrase III by copper accumulation during hepatocarcinogenesis2011

    • Author(s)
      Kuhara M, Wang J, Flores MJ, Zhiwei Q, Koizumi Y, Koyota S, Taniguchi N, Sugiyama T
    • Journal Title

      Biomed.Res.

      Volume: 32 Pages: 111-117

    • NAID

      130004470770

    • Related Report
      2010 Annual Research Report
    • Peer Reviewed
  • [Journal Article] A highly sensitive probe detecting low pH area of HeLa cells based on rhodamine B modified beta-cyclodextrins2009

    • Author(s)
      Hasegawa T, Kondo Y, Koizumi Y, Sugiyama T, Takeda A, Ito S, Hamada F.
    • Journal Title

      Bioorg. Med. Chem.

      Volume: 17 Issue: 16 Pages: 6015-6019

    • DOI

      10.1016/j.bmc.2009.06.046

    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Lys17 in the 'lasso' peptide lariatin A is responsible for anti-mycobacterial activity2009

    • Author(s)
      Iwatsuki M, Koizumi Y, Gouda H, Hirono S, Tomoda H, Omura S.
    • Journal Title

      Bioorg. Med. Chem. Lett.

      Volume: 19 Issue: 10 Pages: 2888-2890

    • DOI

      10.1016/j.bmcl.2009.03.033

    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Expression and localization of regenerating gene I in a rat liver regeneration model2009

    • Author(s)
      Wang J, Koyota S, Zhou X, Ueno Y, Ma L, Kawagoe M, Koizumi Y, Okamoto H, Sugiyama T.
    • Journal Title

      Biochem. Biophys. Res. Commun.

      Volume: 380 Issue: 3 Pages: 472-477

    • DOI

      10.1016/j.bbrc.2009.01.126

    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Niemann-Pick C1 protein transports copper to the secretory compartment from late endosomes where ATP7B resides2009

    • Author(s)
      Yanagimoto C, Harada M, Kumemura H, Koga H, Kawaguchi T, Terada K, Hanada S, Taniguchi E, Koizumi Y, Koyota S, Ninomiya H, Ueno K, Sugiyama T, Sata M.
    • Journal Title

      Exp. Cell Res.

      Volume: 315 Issue: 2 Pages: 119-126

    • DOI

      10.1016/j.yexcr.2008.10.022

    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Simaomicin α, a Polycyclic Xanthone, Induces G1 Arrest with Suppression of pRb Phosphorylation2009

    • Author(s)
      Koizumi Y, Tomoda H, Kumagai A, Zhou XP, Koyota S, Sugiyama T.
    • Journal Title

      Cancer Sci.

      Volume: 100 Issue: 2 Pages: 322-326

    • DOI

      10.1111/j.1349-7006.2008.01033.x

    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Lys17 in the 'lasso' peptide lariatin A is responsible for anti-mycobacterial activity2009

    • Author(s)
      Iwatsuki M, 他
    • Journal Title

      Bioorg.Med.Chem.Lett. 19

      Pages: 2888-2890

    • Related Report
      2009 Annual Research Report
    • Peer Reviewed
  • [Journal Article] A highly sensitive probe detecting low pH area of HeLa cells based on rhodamine B modified beta-cyclodextrins2009

    • Author(s)
      Hasegawa T, 他
    • Journal Title

      Bioorg.Med.Chem. 17

      Pages: 6015-6019

    • Related Report
      2009 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Simaomicin a, a Polycyclic Xanthone, Induces G1 Arrest with Suppression of pRb Phosnhorvlation2009

    • Author(s)
      Koizumi Y、他
    • Journal Title

      Cancer Sci 100

      Pages: 322-326

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Niemann-Pick C1 protein transports copper to the secretory compartment from late endosomes where ATP7B resides2009

    • Author(s)
      Harada M、他
    • Journal Title

      Exp. Cell Res 315

      Pages: 119-126

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Expression and localization of regenerating gene I in a rat liver regene ration model2009

    • Author(s)
      Wang J、他
    • Journal Title

      Biochem. Biophys. Res. Commun 380

      Pages: 472-477

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed
  • [Presentation] 血栓溶解を促進するマルホルミンの構造活性相関2011

    • Author(s)
      小泉幸央、長井賢一郎、蓮見惠司、小代田宗一、杉山俊博
    • Organizer
      日本農芸化学会2010年度大会
    • Place of Presentation
      京都
    • Year and Date
      2011-03-27
    • Related Report
      2010 Final Research Report
  • [Presentation] 血栓溶解を促進するマルホルミンの構造活性相関2011

    • Author(s)
      小泉幸央、長井賢一郎、蓮見恵司、小代田宗一、杉山俊博
    • Organizer
      日本農芸化学会2011年度大会
    • Place of Presentation
      京都
    • Year and Date
      2011-03-27
    • Related Report
      2010 Annual Research Report
  • [Presentation] Cosmc阻害による乳ガン細胞の増殖・転移抑制2010

    • Author(s)
      明円 悠、小代田宗一、馬 莉、小泉幸央、杉山俊博
    • Organizer
      BMB2010(第3 回日本分子生物学会年会 第83 回日本生化学会大会合同大会)
    • Place of Presentation
      神戸
    • Year and Date
      2010-12-10
    • Related Report
      2010 Final Research Report
  • [Presentation] Generation and characterization of intracellular single chain fragment variable (scFv) antibodies against ppGalNacTs2010

    • Author(s)
      Ma L、Koyota S、Myoen Y、Koizumi Y、Sugiyama T
    • Organizer
      BMB2010(第33回日本分子生物学会年会第83回日本生化学会大会合同大会)
    • Place of Presentation
      神戸
    • Year and Date
      2010-12-10
    • Related Report
      2010 Final Research Report
  • [Presentation] マウスエナメル芽細胞前駆細胞と象牙芽細胞前駆細胞の共培養による石灰化促進2010

    • Author(s)
      小代田宗一、小代田理恵、堀川彩夏、牧野晃大、遊佐和之、小泉幸央、杉山俊博
    • Organizer
      BMB2010(第33回日本分子生物学会年会第83回日本生化学会大会合同大会)
    • Place of Presentation
      神戸
    • Year and Date
      2010-12-10
    • Related Report
      2010 Final Research Report
  • [Presentation] Cosmc阻害による乳ガン細胞の増殖・転移抑制2010

    • Author(s)
      明円悠、小代田宗一、馬莉、小泉幸央、杉山俊博
    • Organizer
      第33回日本分子生物学会年会第83回日本生化学会大会合同大会
    • Place of Presentation
      神戸
    • Year and Date
      2010-12-10
    • Related Report
      2010 Annual Research Report
  • [Presentation] Generation and characterization of intracellular single chain fragment variable (scFv) antibodies against ppGalNacTs2010

    • Author(s)
      Ma L, Koyota S, Myoen Y, Koizumi Y, Sugiyama T
    • Organizer
      第33回日本分子生物学会年会第83回日本生化学会大会合同大会
    • Place of Presentation
      神戸
    • Year and Date
      2010-12-10
    • Related Report
      2010 Annual Research Report
  • [Presentation] マウスエナメル芽細胞前駆細胞と象牙芽細胞前駆細胞の共培養による石灰化促進2010

    • Author(s)
      小代田宗一、小代田理恵、堀川彩夏、牧野晃大、遊佐和之、小泉幸央、杉山俊博
    • Organizer
      第33回日本分子生物学会年会第83回日本生化学会大会合同大会
    • Place of Presentation
      神戸
    • Year and Date
      2010-12-10
    • Related Report
      2010 Annual Research Report
  • [Presentation] チアカリックス[4]アレーンテトラスルホン酸-Cd(II)錯体による抗腫瘍効果2010

    • Author(s)
      小泉幸央、周 小平、濱田文男、近藤良彦、小代田宗一、杉山俊博
    • Organizer
      日本農芸化学会2009年度大会
    • Place of Presentation
      東京
    • Year and Date
      2010-03-29
    • Related Report
      2010 Final Research Report 2009 Annual Research Report
  • [Presentation] 4',6,7-トリヒドロキシイソフラボンによる細胞周期G1期停止作用とアポトーシス誘導2009

    • Author(s)
      小泉幸央、鄒 暁元、濱田文男、杉山俊博
    • Organizer
      日本生化学会東北支部第75回例会・シンポジウム
    • Place of Presentation
      仙台
    • Year and Date
      2009-05-09
    • Related Report
      2010 Final Research Report
  • [Presentation] 4',6,7-トリヒドロキシイソフラボンによる細胞周期G1期停止作用とアポトーシス誘導2009

    • Author(s)
      小泉幸央, 他
    • Organizer
      日本生化学会東北支部 第75回例会・シンポジウム
    • Place of Presentation
      仙台
    • Year and Date
      2009-05-09
    • Related Report
      2009 Annual Research Report
  • [Presentation] ヒト非小細胞肺がん細胞株A549に対する緑茶カテキン類の細胞増殖抑制効果2009

    • Author(s)
      熊谷彩子、長岡康夫、小泉幸央、飯田和樹、小代田宗一、上里新一、杉山俊博
    • Organizer
      日本薬学会第129年会
    • Place of Presentation
      京都
    • Year and Date
      2009-03-28
    • Related Report
      2010 Final Research Report 2008 Annual Research Report

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Published: 2008-04-01   Modified: 2018-03-28  

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