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2010 Fiscal Year Final Research Report

Molecular design and chemical genetic approach of bio-probe for anti-angiogenic therapy

Research Project

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Project/Area Number 21390033
Research Category

Grant-in-Aid for Scientific Research (B)

Allocation TypeSingle-year Grants
Section一般
Research Field Drug development chemistry
Research InstitutionGifu Pharmaceutical University

Principal Investigator

NAGASAWA Hideko  岐阜薬科大学, 薬学部, 教授 (90207994)

Co-Investigator(Kenkyū-buntansha) OKUDA Kensuke  岐阜薬科大学, 薬学部, 講師 (00311796)
UEDA Satoshi  岐阜薬科大学, 薬学部, 助教 (50453056)
HARA Hideaki  岐阜薬科大学, 薬学部, 教授 (20381717)
Project Period (FY) 2009 – 2011
Keywords医薬分子設計 / 血管新生阻害剤 / がん / HIF-1 / VEGF / 構造活性相関
Research Abstract

Novel angiogenesis inhibitors were developed based on natural product chemistry-based approach using Brazilian green propolis and SAR study of arylidene thiazolidinedione(TZD) analogs library. They inhibited in vitro and in vivo angiogenesis significantly without cytotoxicity through reducing HIF-1-VEGF signaling pathway. They are promising candidates as nontoxic and selective anti-angiogenesis agents applicable to inhibit tumor and retinal angiogenesis. Now we are investigating their target protein for angiogenesis inhibition.

  • Research Products

    (29 results)

All 2012 2011 2010 2009

All Journal Article (13 results) (of which Peer Reviewed: 10 results) Presentation (16 results)

  • [Journal Article] The novel hypoxic cytotoxin, TX-2098 has antitumor effect in pancreatic cancer ; possible mechanism through inhibiting VEGF and hypoxia inducible factor-1a targeted gene expression2012

    • Author(s)
      Kotaro Miyake, Hideko Nagasawa, Mitsuo Shimada
    • Journal Title

      Exp. Cell. Res

      Volume: (in press)

    • DOI

      DOI:10.1016/j.yexcr

  • [Journal Article] Development of a Hypoxia-Selective Near-Infrared Fluorescent Probe for Non-invasive Tumor Imaging2012

    • Author(s)
      Bahaa Gamal Mohamed Youssif, Kensuke Okuda, Hideko Nagasawa
    • Journal Title

      Chem. Pharm. Bull

      Volume: 60(3) Pages: 402-407

    • DOI

      DOI:10.1248/cpb.60.402

    • Peer Reviewed
  • [Journal Article] 2-Nitroimidazole-tricarbocyanine conjugate as a near-infrared fluorescent probe for in vivo imaging of tumor hypoxia2012

    • Author(s)
      Kensuke Okuda, Hideko Nagasawa
    • Journal Title

      Bioconjug. Chem

      Volume: 23(3) Pages: 324-329

    • Peer Reviewed
  • [Journal Article] Isolation, identification, and biological evaluation of HIF-1-modulating compounds from Brazilian green propolis2011

    • Author(s)
      Hisanori Hattori, Kensuke Okuda, Hideko Nagasawa
    • Journal Title

      Bioorg. Med. Chem

      Volume: 19(18) Pages: 5392-5401

    • DOI

      DOI:10.1016/j.bmc.2011.07.060

    • Peer Reviewed
  • [Journal Article] An Arylidene-Thiazolidinedione Derivative, GPU-4, without PPARγActivation, Reduces Retinal Neovascularization2011

    • Author(s)
      Shinsuke Nakamura, Hideko Nagasawa, Hideaki Hara
    • Journal Title

      Curr. Neurovasc. Res

      Volume: 8(1) Pages: 25-34

    • URL

      http://www.benthamdirect.org/pages/b_viewarticle.php?articleID=3165504

    • Peer Reviewed
  • [Journal Article] Drug discovery for targeting tumor microenvironment2011

    • Author(s)
      Hideko Nagasawa
    • Journal Title

      J. Pharmacol. Sci

      Volume: 115(4) Pages: 446-52

    • DOI

      DOI:10.1254/jphs.10R25FM

    • Peer Reviewed
  • [Journal Article] Structural Investigation of the Binding of 5-Substituted Swainsonine Analogues to Golgi alpha-Mannosidase II2010

    • Author(s)
      Douglas A. Kuntz, Hideko Nagasawa, David R. Rose
    • Journal Title

      Chem Bio Chem

      Volume: 11(5) Pages: 673-80

    • DOI

      DOI:10.1002/cbic.200900750

  • [Journal Article] Design of novel hypoxia-targeting IDO hybrid inhibitors conjugated with an unsubstituted L-TRP as an IDO affinity moiety2010

    • Author(s)
      Hitomi Nakashima, Hideko Nagasawa, Hitoshi Hori
    • Journal Title

      Adv Exp Med Biol

      Volume: 662 Pages: 415-21

    • DOI

      DOI:10.1007/9'18-1-4419-1241-l_60

    • Peer Reviewed
  • [Journal Article] Facile Synthesis of 1, 2, 4-Triazoles via a Copper-Catalyzed Tandem Addition-Oxidative Cyclization2009

    • Author(s)
      Satoshi Ueda, Hideko Nagasawa
    • Journal Title

      J. Am. Chem

      Volume: 131(42) Pages: 15080-1

    • DOI

      DOI:10.1021/ja905056z

    • Peer Reviewed
  • [Journal Article] Copper-Catalyzed Synthesis of Benzoxazoles via a Regioselective C-H Functionalization/C-O Bond Formation under an Air Atmosphere2009

    • Author(s)
      Satoshi Ueda, Hideko Nagasawa
    • Journal Title

      J. Org. Chem

      Volume: 74(11) Pages: 4272-7

    • DOI

      DOI:10.1021/jo900513z

  • [Journal Article] A chemical biosynthesis design for an antiatherosclerosis drug by acyclic tocopherol intermediate analogue based on "isoprenomics"2009

    • Author(s)
      Yoshihiro Uto, Hideko Nagasawa, Hitoshi Hori
    • Journal Title

      Adv Exp Med Biol

      Volume: 645 Pages: 109-14

    • DOI

      DOI:10.1007/978-0-387-85998-9_17

    • Peer Reviewed
  • [Journal Article] Downregulation of matrix metalloprotease-9 and urokinase plasminogen activator by TX-1877 results in decreased tumor growth and metastasis on xenograft model of rectal cancer2009

    • Author(s)
      Kotaro Miyake, Hideko Nagasawa, Hitoshi Hori
    • Journal Title

      Cancer Chemother Pharmacol

      Volume: 64(5) Pages: 885-92

    • DOI

      DOI:10.1007/s00280-009-0937-5

    • Peer Reviewed
  • [Journal Article] Correlation between antiangiogenic activity and antioxidant activity of various components from propolis2009

    • Author(s)
      Mok-Ryeon Ahn, Hideko Nagasawa, Toshiro Ohta
    • Journal Title

      Mol. Nutr. Food Res

      Volume: 53(5) Pages: 643-51

    • DOI

      DOI:10.1002/mnfr.200800021

    • Peer Reviewed
  • [Presentation] がんのin vivoイメージングを目指す低酸素応答性光誘起電子移動(PET)機構を有する近赤外蛍光プローブの論理的分子設計と合成2012

    • Author(s)
      奥田健介
    • Organizer
      日本薬学会第132回年会
    • Place of Presentation
      札幌
    • Year and Date
      20120328-20120331
  • [Presentation] Pepducin膜透過プロセスを可視化するFRET蛍光プローブの開発2012

    • Author(s)
      辻美恵子
    • Organizer
      日本薬学会第132回年会
    • Place of Presentation
      札幌
    • Year and Date
      20120328-20120331
  • [Presentation] SAR Studies of Arylidene Thiazolidinediones as Potent Angiogenesis Inhibitors2011

    • Author(s)
      村瀬哲司
    • Organizer
      AIMECS11
    • Place of Presentation
      東京
    • Year and Date
      20111129-1202
  • [Presentation] がん微小環境モジュレータの創製を目指す創薬研究2011

    • Author(s)
      永澤秀子
    • Organizer
      第9回がんとハイポキシア研究会
    • Place of Presentation
      東京
    • Year and Date
      20111126-20111127
  • [Presentation] 微小環境モジュレーターGPU-231のグルコース飢餓選択的細胞毒性と血管新生阻害作用2011

    • Author(s)
      成瀬康介
    • Organizer
      第9回がんとハイポキシア研究会
    • Place of Presentation
      東京
    • Year and Date
      20111126-20111127
  • [Presentation] 新規UPRモジュレーターGPU-231のグルコース飢餓選択的細胞毒性と血管新生阻害作用2011

    • Author(s)
      成瀬康介
    • Organizer
      第70回日本癌学会学術総会
    • Place of Presentation
      名古屋
    • Year and Date
      20111003-20111005
  • [Presentation] 低酸素がん微小環境を標的とする創薬研究2011

    • Author(s)
      永澤秀子
    • Organizer
      第15回酸素ダイナミクス研究会
    • Place of Presentation
      佐賀
    • Year and Date
      20110910-20110911
  • [Presentation] がんのin vivoイメージングを目指す低酸素応答性PET型近赤外蛍光プローブの論理的分子設計と合成2011

    • Author(s)
      河野樹
    • Organizer
      第20回バイオイメージング学会
    • Place of Presentation
      千歳
    • Year and Date
      20110901-20110902
  • [Presentation] 低酸素がんイメージングを目指す近赤外蛍光プローブの論理的分子設計と合成2011

    • Author(s)
      奥田健介
    • Organizer
      第17回国際癌治療増感研究会
    • Place of Presentation
      仙台
    • Year and Date
      20110624-25
  • [Presentation] 低酸素がんのin vivoイメージングを目指す近赤外蛍光プローブの開発2011

    • Author(s)
      坂井良輔
    • Organizer
      平成23年度日本薬学会東海支部例会
    • Place of Presentation
      名古屋
    • Year and Date
      2011-11-23
  • [Presentation] チアゾリジンジオン誘導体GPU-4の網膜血管新生抑制作用2011

    • Author(s)
      中村信介
    • Organizer
      第120回日本薬理学会近畿部会
    • Place of Presentation
      京都
    • Year and Date
      2011-11-11
  • [Presentation] Development of anticancer drugs targeting the tumor microenvironment2010

    • Author(s)
      成瀬康介
    • Organizer
      第69回日本癌学会学術総会
    • Place of Presentation
      大阪
    • Year and Date
      20100922-24
  • [Presentation] がん微小環境を標的としたブラジル産プロポリス成分の創薬化学研究2010

    • Author(s)
      服部久範
    • Organizer
      第14回日本がん分子標的治療学会学術集会
    • Place of Presentation
      東京
    • Year and Date
      20100706-08
  • [Presentation] Drug Discovery for Targeting The Tumor Microenvironment from Propolis2010

    • Author(s)
      服部久範
    • Organizer
      AACR 101st Annual Meeting
    • Place of Presentation
      アメリカワシントンDC
    • Year and Date
      20100417-21
  • [Presentation] 低酸素・低栄養微小環境を標的とした新規がん治療薬の開発2010

    • Author(s)
      榎本幸浩
    • Organizer
      第130回日本薬学会年会
    • Place of Presentation
      岡山
    • Year and Date
      20100328-30
  • [Presentation] がんの低酸素・低栄養微小環境を標的とした新規治療薬の開発2009

    • Author(s)
      榎本幸浩
    • Organizer
      創薬懇話会
    • Place of Presentation
      岐阜
    • Year and Date
      2009-12-10

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Published: 2013-07-31  

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