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HIKISHIMA Sadao  疋島 貞雄

ORCIDConnect your ORCID iD *help
Researcher Number 70398816
Other IDs
Affiliation (based on the past Project Information) *help 2007 – 2011: Tokyo University of Pharmacy and Life Science, 薬学部, 助教
2006: 東京薬科大学, 薬学部, 助手
Review Section/Research Field
Principal Investigator
Drug development chemistry
Except Principal Investigator
Drug development chemistry
Keywords
Principal Investigator
創薬化学 / 有機化学 / 薬学 / RNA干渉 / ラジカル反応 / ホスフィン酸 / ゲノム化学 / siRNA / ゲノム創薬 / Hussigen反応 … More / Sonogashira反応 / ジフルオロメチレンボスホン酸 / insituクリックケミストリー / Huisgen反応 / チミジンホスホリラーゼ / ジフルオロメチレンホスホン酸 / in situクリックケミストリー / 医薬分子設計 … More
Except Principal Investigator
PNP阻害剤 / スフィンゴミエリナーゼ / fragment-based drug design / ジフルオロホスホン酸 / ヌクレオチドアナログ / ジフルオロメチレンボスホン酸 / ホスフィン酸 / 速度論的光学分割 / ジペプチドイソスター / X線構造解析 / 遷移状態アナログ / ペプチドイソスター / Huisen反応 / Huisgen反応 / TP阻害剤 / Huisgen 反応 / クリック反応 / TP 阻害剤 / PNP 阻害剤 Less
  • Research Projects

    (4 results)
  • Research Products

    (42 results)
  • Co-Researchers

    (7 People)
  •  Development of biologically active compounds based on features of phosphonyl and phosphinyl functional groups

    • Principal Investigator
      YOKOMATSU Tsutomu
    • Project Period (FY)
      2009 – 2011
    • Research Category
      Grant-in-Aid for Scientific Research (C)
    • Research Field
      Drug development chemistry
    • Research Institution
      Tokyo University of Pharmacy and Life Science
  •  Synthesis of siRNA molecules containing phosphinate type dinucleotide derivativesPrincipal Investigator

    • Principal Investigator
      HIKISHIMA Sadao
    • Project Period (FY)
      2009 – 2010
    • Research Category
      Grant-in-Aid for Young Scientists (B)
    • Research Field
      Drug development chemistry
    • Research Institution
      Tokyo University of Pharmacy and Life Science
  •  Development of biologically active compounds based on features of fluoromethylene phosphonates

    • Principal Investigator
      YOKOMATSU Tsutomu
    • Project Period (FY)
      2007 – 2008
    • Research Category
      Grant-in-Aid for Scientific Research (C)
    • Research Field
      Drug development chemistry
    • Research Institution
      Tokyo University of Pharmacy and Life Science
  •  in situ クリックケミストリーを用いた二基質類縁型酵素阻害剤の創製Principal Investigator

    • Principal Investigator
      疋島 貞雄
    • Project Period (FY)
      2006 – 2007
    • Research Category
      Grant-in-Aid for Young Scientists (B)
    • Research Field
      Drug development chemistry
    • Research Institution
      Tokyo University of Pharmacy and Life Science

All 2010 2009 2008 2007

All Journal Article Presentation

  • [Journal Article] 9-Deazaguanine derivatives connected by a linker to difluoromethylene phosphonic acid are slow-binding picomolar inhibitors of trimeric purine nucleoside phosphorylase2010

    • Author(s)
      K. Breer, L. Glavas-Obrovac, M. Suver, S. Hikishima, M. Hashimoto, T. Yokomatsu, B. Wielgus-Kutrowska, L. Magnowska, A. Bzowska
    • Journal Title

      FEBS Journal

      Volume: 277 Pages: 1747-1760

    • Data Source
      KAKENHI-PROJECT-21590126
  • [Journal Article] 1.45A resolution crystal structure of recombinat PNP in complex with a pM multisubstrate analogue inhibitor bearing one feature of posutulated transition state2010

    • Author(s)
      G. Chojnowski, K. Breer, M. Narczyk, B. Wielgus-Kutrowska, H. Czapinska, M. Hashimoto, S. Hikishima, T. Yokomatsu, M. Bochtler, A. Girstun, K. Staro., A. Bzowska
    • Journal Title

      Biochem. Biophys. Res. Comm

      Volume: 391 Pages: 703-708

    • Data Source
      KAKENHI-PROJECT-21590126
  • [Journal Article] Structural-based design and synthesis of novel 9-deazaguanine derivatives having a phosphate mimic as multi-substrate analogue inhibitors for mammalian PNPs2010

    • Author(s)
      S.Hikishima, T.Yokomatsu, 他
    • Journal Title

      Bioorg.Med.Chem. 18

      Pages: 2275-2284

    • Peer Reviewed
    • Data Source
      KAKENHI-PROJECT-21590126
  • [Journal Article] Structural-based design and synthesis of novel 9-deazaguanine derivatives having a phosphate mimic as multi-substrate analogue inhibitors for mammalian PNPs2010

    • Author(s)
      S. Hikishima, M. Hashimoto, L. Magnowska, A. Bzowska and T. Yokomatsu
    • Journal Title

      Bioorg. Med. Chem

      Volume: 18 Pages: 2275-2284

    • Data Source
      KAKENHI-PROJECT-21590126
  • [Journal Article] 9-Deazaguanine Derivatives Connected by a Linker to Difluoromethylene Phosphonic Acid Are Slow-binding Picomolar Inhibitors of Trimeric Purine Nucleoside Phosphorylase2010

    • Author(s)
      K.Breer, L.Glavas-Obrovac, M.Suver, S.Hikishima, M.Hashimoto, T.Yokomatsu, B.Wielgus-Kutrowska, L.Magnowska, A.Bzowska
    • Journal Title

      FEBS Journal

      Volume: 277 Pages: 1747-1760

    • Peer Reviewed
    • Data Source
      KAKENHI-PROJECT-21590126
  • [Journal Article] Structural-based Design and Synthesis of Novel 9-Deazaguanine Derivatives having a Phosphate Mimic as Multi-substrate Analogue Inhibitors for Mammalian PNPs2010

    • Author(s)
      S.Hikishima, M.Hashimoto, L.Magnowska, A.Bzowska, T.Yokomatsu
    • Journal Title

      Bioorg.Med.Chem.

      Volume: 18 Pages: 2275-2284

    • Peer Reviewed
    • Data Source
      KAKENHI-PROJECT-21590126
  • [Journal Article] Antiproliferative avtivity of purine nucleoside phosphorylase multisubstrate analogu inhibitors containing difluoromethyl phosphonic acid against leukaemia and lymphoma cells2010

    • Author(s)
      L. Glava.-Obrovac, M. Suver, S. Hikishima, M. Hashimoto, T. Yokomatsu, L. Magnowska, A. Bzowska
    • Journal Title

      Chem. Bio. Drug. Des

      Volume: 75 Pages: 392-399

    • Data Source
      KAKENHI-PROJECT-21590126
  • [Journal Article] Antiproliferative Activity of Purine Nucleoside Phosphorylase Multisubstrate Analogue Inhibitors containing Difluoromethyl Phosphonic Acid against Leukaemia and Lymphoma Cells2010

    • Author(s)
      L.Glavas-Obrovac, M.Suver, S.Hikishima, M.Hashimoto, T.Yokomatsu, L.Magnowska, A.Bzowska
    • Journal Title

      Chem.Bio.Drug.Des.

      Volume: 75 Pages: 399-399

    • Peer Reviewed
    • Data Source
      KAKENHI-PROJECT-21590126
  • [Journal Article] Overexpressed protein may act as mops removing their ligands from host cells : A case study of calf PNP2010

    • Author(s)
      K. Breer, B. Wielgus-Kutrowska, A. Girstun, K. Staro., M. Hashimoto, S. Hikishima, T. Yokomatsu, A. Bzowska
    • Journal Title

      Biochem. Biophys. Res. Comm

      Volume: 391 Pages: 1203-1209

    • Data Source
      KAKENHI-PROJECT-21590126
  • [Journal Article] Diastereoselective synthesis of γ-amino-δ-hydroxy-α, α-difluorophosphonates : A vehiclefor for the structure-activity relationship of SMA-7, a potent sphingomyelinase inhibitor2009

    • Author(s)
      T. Yamagishi, S. Muronoi, S. Hikishima, H. Shimeno, S. Soeda, and T. Yokomatsu
    • Journal Title

      J. Org. Chem

      Volume: 74 Pages: 6350-6353

    • Data Source
      KAKENHI-PROJECT-21590126
  • [Journal Article] Sphingomyelinease inhibition suggests a possible new strategy for the treatment of inflammatory bowel disease2008

    • Author(s)
      S. Soeda, A. Sakata, T. Ochiai, K. Yasuda, Y. Kuramoto, H. Shimeno, A. Toda, R. Eyanagi, S. Hikishima, T. Yokomatsu, and S. Shibuya
    • Journal Title

      Curr. Drug Therapy 3

      Pages: 218-225

    • Peer Reviewed
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Journal Article] Inhibition of lipopolysaccharide-induced Release of Interleukin-8 from Intestinal Epithelial Cells by SMA, a Novel Inhibitor of Sphingomyelinase and its Therapeutic Effect on Dextran Sulphate Sodium-induced Colitis in Mice2007

    • Author(s)
      A. Sakata, K. Yasuda, T. Ochiai, H. Shimeno, S. Hikishima, T. Yokomatsu, S. Shibuya, and S. Soeda
    • Journal Title

      Cell Immunology 245

      Pages: 24-31

    • Peer Reviewed
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Journal Article] Inhibitory Properties of Nucleotides with Difluoromethy lenephosphonic Acid as a Phosphate Mimic versus Calf Spleen Purine Nucleoside Phosphorylase and Effect of These Analogues on the Viability of Human Blood Lymphocytes2007

    • Author(s)
      L. Glavas-Obrovac, M. Suver ; S. Hikishima, T. Yokomatsu, and A. Bzowska
    • Journal Title

      ucleosides, Nucleotides & Nucleic Acids 26

      Pages: 989-993

    • Peer Reviewed
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Journal Article] Synthesis and biological evaluation of 9-deazaguanine derivatives connec-ted by a Linker to difluoromethylene phosphonic acid as multi-substrate analogue Inhibitors of PNP2007

    • Author(s)
      S. Hikishima, M. Hashimoto, L. Magnowska, A. Bzowska, andT. Yokomatsu
    • Journal Title

      Bioorganic Medicinal Chemistry Letters 17

      Pages: 4173-4177

    • Peer Reviewed
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Journal Article] Synthesis and Biological Evalution of 9-Deazaguanine Derivatives connected by a Linker to Difluoromethylene phosphonic Acid as Multi-substrate Analogue Inhibitors of PNP2007

    • Author(s)
      S. Hikishima, M. Hashimoto, L. Magnowska, A. Bzowska, and T. Yokomatsu
    • Journal Title

      Bioorg. Med. Chem. Lett. 17

      Pages: 4173-4177

    • Peer Reviewed
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Journal Article] Acid Sphingomyelinase Inhibition Suppresses Lipopolysaccharide-mediated Release of Inflammatory Cytokines from Macrophages and Protects against Disease Pathology in Dextran Sulphate Sodium-induced Colitis in Mices2007

    • Author(s)
      A. Sakata, T. Ochiai, H. Shimeno, S. Hikishima, T. Yokomatsu, S. Shibuya, A. Toda, R. Eyanagi, and S. Soeda
    • Journal Title

      Immunology 122

      Pages: 54-64

    • Peer Reviewed
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Journal Article] Synthesis and biological evaluation of 9-deazagunine derivatives connected by a linker to difluoromethylene phoshponic acid as multi-substrate analogue inhibitors of PNP2007

    • Author(s)
      S. Hikishima, M. Hashimoto, L. Magnowska, A. Bzowska, and T. Yokomatsu
    • Journal Title

      Bioorganic Medicinal Chemistry Lettters 17

      Pages: 4273-4277

    • Peer Reviewed
    • Data Source
      KAKENHI-PROJECT-18790091
  • [Presentation] SBDDを用いた新規PNP阻害剤の創製研究2010

    • Author(s)
      谷津智之, 疋島貞雄, Agnieszka Bzowska, 横松力
    • Organizer
      日本薬学会第130年会
    • Place of Presentation
      岡山
    • Data Source
      KAKENHI-PROJECT-21590126
  • [Presentation] ベンゼン環をスキャホールドとする二基質類縁型PNP阻害剤の創製研究2009

    • Author(s)
      谷津智之, 疋島貞雄, 横松力
    • Organizer
      日本薬学会第129年会
    • Place of Presentation
      京都
    • Year and Date
      2009-03-27
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] SMase阻害剤を指向した新規SMA-7類縁体の合成研究2009

    • Author(s)
      野田祐介, 室野井真, 疋島貞雄, 山岸丈洋, 横松力
    • Organizer
      第35回反応と合成の進歩シンポジウム
    • Place of Presentation
      金沢
    • Data Source
      KAKENHI-PROJECT-21590126
  • [Presentation] ベンゼン環をスキャホールドとする二基質類縁型PNP 阻害剤の創製研究2009

    • Author(s)
      谷津智之, 疋島貞雄, 横松力
    • Organizer
      日本薬学会第129年会
    • Place of Presentation
      京都
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] SBDDを用いた新規PNP阻害剤の創製研究2009

    • Author(s)
      谷津智之, 疋島貞雄, Agnieszka Bzowska, 横松力
    • Organizer
      第28回メディシナルケミストリーシンポジウム
    • Place of Presentation
      東京
    • Data Source
      KAKENHI-PROJECT-21590126
  • [Presentation] SMase阻害剤を指向した機能性分子の創製研究2009

    • Author(s)
      野田裕介, 疋島貞雄, 横松力
    • Organizer
      日本薬学会第129年会
    • Place of Presentation
      京都
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] Huisgen反応を用いた新規二基質複合類縁型TP阻害剤の創製研究2008

    • Author(s)
      橘 真純, 疋島 貞雄, 横松 力
    • Organizer
      日本薬学会第128年会
    • Place of Presentation
      横浜
    • Year and Date
      2008-03-26
    • Data Source
      KAKENHI-PROJECT-18790091
  • [Presentation] Huisgen反応を用いた新規2基質複合類縁型TP阻害剤の創製研究2008

    • Author(s)
      橘 真純, 疋島 貞雄, 横松 力
    • Organizer
      日本薬学会第128年会
    • Place of Presentation
      横浜
    • Year and Date
      2008-03-26
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] Thermodynamic studies of interactions of calf spleen PNP with acyclic phosphonate inhibitors2008

    • Author(s)
      K. Breer, M. Hashimoto, S. Hikishima, A. Bzowska, 他
    • Organizer
      Joint Symposium of the 18th International Roundtable on Nucleosides, Nucleotides and Nucleic Acids and the 35th International Symposium on Nucleic Acids Chemistry
    • Place of Presentation
      京都
    • Year and Date
      2008-09-08
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] 9-Deazaguanine derivatives : synthesis and inhibitory properties as multi-substrate analogue inhibitors of mammalian PNPs Joint Symposium of the 18th International Roundtable on Nucleosides2008

    • Author(s)
      T. Yatsu, M. Hashimoto, S. Hikishima, L. Magnowska, A. Bzowska, and T. Yokomatsu
    • Organizer
      Nucleotides and Nucleic Acids and the 35th International Symposium on Nucleic Acids Chemistry
    • Place of Presentation
      Kyoto
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] Huisgen 反応を用いた新規2基質複合類縁型TP阻害剤の創製研究2008

    • Author(s)
      橘真純, 疋島貞雄, 横松力
    • Organizer
      日本薬学会第128年会
    • Place of Presentation
      横浜
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] ホスホノジフルオロメチレン基を有するアジト誘導体とω-アルキニルピリミジン誘導体とのHuisgen反応2008

    • Author(s)
      橘真純, 橋本真梨子, 疋島貞雄, 横松力
    • Organizer
      第38回複素環化学討論会
    • Place of Presentation
      福山
    • Year and Date
      2008-11-21
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] リン酸等価体を有する新規2基質複合類縁型PNP阻害剤の創製研究2008

    • Author(s)
      橋本真梨子, 疋島貞雄, 横松力
    • Organizer
      日本薬学会第128年会
    • Place of Presentation
      横浜
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] SMase阻害剤SMA-7誘導体の新規合成法の開発2008

    • Author(s)
      室野井真, 山岸丈洋, 疋島貞雄, 横松力
    • Organizer
      日本薬学会第128年会
    • Place of Presentation
      横浜
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] Thermodynamic studies of interactions of calf spleen PNP with acyclic phosphonate inhibitors, Joint Symposium of the 18th International Roundtable on Nucleosides2008

    • Author(s)
      K. Breer, B. Wielgus-Kutrowska, M. Hashimoto, S. Hikishima, T. Yokomatsu, R. H. Szczepanowski, M. Bochtler, A. Girstun, K. Staron, and A. Bzowska
    • Organizer
      Nucleotides and Nucleic Acids and the 35th International Symposium on Nucleic Acids Chemistry
    • Place of Presentation
      Kyoto
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] ホスホノジフルオロメチレン基を有するアジド誘導体と・-アルキニルピリミジン誘導体とのHuisgen反応2008

    • Author(s)
      橘真純, 橋本真梨子, 疋島貞雄, 横松力
    • Organizer
      第38回複素環化学討論会
    • Place of Presentation
      福山
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] Synthetic Studies for Difluoromethylenephosphonate Analogues of MRS2216, a Selective P2Y_1 Receptor Antagonist2007

    • Author(s)
      Sadao Hikishima, Arihiro Takatori, Atsushi Kojima, and Tsutomu Yokomatsu
    • Organizer
      6^<th> AFMC International Medicinal Chemistry Symposium
    • Place of Presentation
      イスタンブール(トルコ)
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] 脂肪細胞でのPPAR・2発現におけるセラミドシグナルの役割2007

    • Author(s)
      鍋山卓志, 藏元佑嘉子, 落合敬史, 林田諭, 添田秦司, 疋島貞雄, 横松力, 渋谷皓, 占野廣司
    • Organizer
      第24回日本薬学会九州支部大会
    • Place of Presentation
      福岡
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] PNP阻害剤を指向した新規ヌクレオチドアナログの設計と評価2007

    • Author(s)
      疋島 貞雄, 橋本 真梨子, 添田 秦司, 占野 廣司, L. Magnowaka, A. Bzowska, 渋谷 皓, 横松 力
    • Organizer
      日本ケミカルバイオロジー研究会 第2回年会
    • Place of Presentation
      京都
    • Year and Date
      2007-05-09
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] 日本ケミカルバイオロジー研究会第2回年会2007

    • Author(s)
      疋島貞雄, 橋本真梨子, 添田秦司, 占野廣司, Magnowaka Lucya, AgnieszkaBzowska, 渋谷皓, 横松力
    • Place of Presentation
      京都
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] Synthesis and evaluation of 9-deazaguanine derivatives as multi-substrate analogue inhibitors of PNP2007

    • Author(s)
      M. Hashimoto, S. Hikishima, L. Magnowska, A. Bzowska, and T. Yokomatsu
    • Organizer
      第5回国際核酸化学シンポジウム
    • Place of Presentation
      東京
    • Year and Date
      2007-11-20
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] T細胞受容体を介した・産生におけるセラミドシグナルの役割2007

    • Author(s)
      東みお, 落合敬史, 藏元佑嘉子, 添田秦司, 坂田晃, 疋島貞雄, 横松力, 渋谷皓, 占野廣司
    • Organizer
      第24回日本薬学会九州支部大会
    • Place of Presentation
      福岡
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] Synthesis and evaluation of 9-deazaguanine derivatives as multi-substrate analogue inhibitors of PNP2007

    • Author(s)
      Mariko Hashimoto, Sadao Hikishima, Lucyna Magnowska, Angieszka Bzowska, and Tsutomu Yokomatsu
    • Organizer
      Fifth Inetrnational Symposium on Nucleic Acids Chemistry
    • Place of Presentation
      東京
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] Synthesis and Biological Evaluation of 9-Deazaguanine Derivatives connected by a Linker to Difluoromethylene Phosphonic Acid2007

    • Author(s)
      S. Hikishima, M. Hashimoto, L. Magnowska, A. Bzowska, and T. Yokomatsu
    • Organizer
      第6回 AFMC国際メディシナルケミストリーシンポジウム
    • Place of Presentation
      イスタンブール(トルコ)
    • Year and Date
      2007-07-08
    • Data Source
      KAKENHI-PROJECT-19590109
  • [Presentation] Synthesis and Biological Evaluation of 9-Deazaguanine Derivatives connected by a Linker to Difluoromethylene Phosphonic Acid2007

    • Author(s)
      Sadao Hikishima, Mariko Hashimoto, Lucyna Magnowska, Agnieszka Bzowska, Tsutomu Yokomatsu
    • Organizer
      6^<th> AFMC International Medicinal Chemistry Symposium
    • Place of Presentation
      イスタンブール(トルコ)
    • Data Source
      KAKENHI-PROJECT-19590109
  • 1.  YOKOMATSU Tsutomu (70158369)
    # of Collaborated Projects: 2 results
    # of Collaborated Products: 39 results
  • 2.  YAMAGISHI Takehiro (90297606)
    # of Collaborated Projects: 2 results
    # of Collaborated Products: 3 results
  • 3.  ANGIESKA Bzowska
    # of Collaborated Projects: 2 results
    # of Collaborated Products: 0 results
  • 4.  SOEDA Shinji (20078695)
    # of Collaborated Projects: 1 results
    # of Collaborated Products: 7 results
  • 5.  TACHIBANA Masumi
    # of Collaborated Projects: 1 results
    # of Collaborated Products: 4 results
  • 6.  YATSU Tomoyuki
    # of Collaborated Projects: 1 results
    # of Collaborated Products: 3 results
  • 7.  NODA Yusuke
    # of Collaborated Projects: 1 results
    # of Collaborated Products: 1 results

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※ この処理は、研究者本人だけが実行できます。

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