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Investigation of the mechanism of insulin secretion via Ca

Research Project

Project/Area Number 23659049
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeMulti-year Fund
Research Field Drug development chemistry
Research InstitutionHokkaido University

Principal Investigator

SHUTO Satoshi  北海道大学, 大学院・薬学研究院, 教授 (70241346)

Co-Investigator(Kenkyū-buntansha) SHIMAWAKI Ken  北海道大学, 大学院・薬学研究院, 特任助教 (60451407)
Project Period (FY) 2011 – 2012
Project Status Completed (Fiscal Year 2012)
Budget Amount *help
¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2012: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2011: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
Keywords医薬分子設計 / cADPR / β細胞 / ラジカル反応 / Huisegen反応 / 光反応
Research Abstract

As the key molecule to develop effective biological tools for theidentification of target proteins of cADPR in cells, 4” α-aziceethyl-cADPcR (3) was designedand successfully synthesized. 4” α-Azidoethyl-cADPcR (3) was shown to be biologically activeas we expected.

Report

(3 results)
  • 2012 Annual Research Report   Final Research Report ( PDF )
  • 2011 Research-status Report
  • Research Products

    (19 results)

All 2012 2011 2000 Other

All Journal Article (17 results) (of which Peer Reviewed: 10 results) Presentation (2 results) (of which Invited: 1 results)

  • [Journal Article] Cyclopropane-Based Stereochemical Diversity-Oriented Conformational Restriction Strategy : Histamine Analog swith the4-Amino-2, 3-methano-1-(1H-imidazol-4-yl) butane Structure as Highly PotentHistamine H_3 and/or H4 Receptor Ligands. Org2012

    • Author(s)
      M. Watanabe, T. Kobayashi, T. Hirokawa, A. Yoshida, Y. Ito, S. Yamada, N. Orimoto, Y. Yamasaki, M. Arisawa, S. Shuto
    • Journal Title

      Biomol. Chem

      Volume: 10 Issue: 4 Pages: 736-745

    • DOI

      10.1039/c1ob06496g

    • Related Report
      2012 Annual Research Report 2011 Research-status Report
    • Peer Reviewed
  • [Journal Article] Synthesis and discovery of N-carbonylpyrrolidine- or N-sulfonylpyrrolidine-containing uracil derivatives as potent human deoxyuridine triphosphatase inhibitors.2012

    • Author(s)
      H. Miyakoshi, S. Miyahara, T. Yokogawa, K. T. Chong, J. Taguchi, K. Endoh, W. Yano, T. Wakasa, H. Ueno, Y. Takao, M. Nomura, S. Shuto, H. Nagasawa, M. Fukuoka
    • Journal Title

      J. Med. Chem.

      Volume: 55 Issue: 7 Pages: 2960-2969

    • DOI

      10.1021/jm201627n

    • Related Report
      2012 Annual Research Report 2011 Research-status Report
    • Peer Reviewed
  • [Journal Article] Discovery of a novel class of potent human deoxyuridine triphosphatase inhibitors remarkably enhancing the antitumor activity of thymidylate synthase inhibitors.2012

    • Author(s)
      S. Miyahara, H. Miyakoshi, T. Yokogawa, K. T. Chong, W. Yano, T. Wakasa, H. Ueno, Y. Takao, A. Fujioka, A. Hashimoto, K. Itou, K. Yamamura, M. Nomura, H. Nagasawa, S. Shuto, M. Fukuoka
    • Journal Title

      J. Med. Chem.

      Volume: 55 Issue: 7 Pages: 2970-2980

    • DOI

      10.1021/jm201628y

    • Related Report
      2012 Annual Research Report 2011 Research-status Report
    • Peer Reviewed
  • [Journal Article] Ruthenium-catalyzed cycloisomerization of 1,3-dienes, for example, an N-dienyl-2-vinylaniline derivative, leading to a 3-Exomethylene-2-vinylindole derivative and its application to the synthesis of (±)-cinchonaminone2012

    • Author(s)
      Takao Ogawa
    • Journal Title

      Eur. J. Org. Chem.

      Volume: - Issue: 16 Pages: 3084-3087

    • DOI

      10.1002/ejoc.201200260

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Discovery of Highly Potent Human Deoxyuridine Triphosphatase Inhibitors Based on the Conformation Restriction Strategy.2012

    • Author(s)
      S. Miyahara, H. Miyakoshi, T. Yokogawa, T. Muto, K. Endoh, W. Yano, T. Wakasa, H. Ueno, K. Itou, M. Nomura, H. Nagasawa, S. Shuto
    • Journal Title

      J. Med. Chem.

      Volume: 55, Issue: 11 Pages: 5483-5496

    • DOI

      10.1021/jm300416h

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] 1,2,3-Triazole-Containing Uracil Derivatives with Excellent Pharmacokinetics as a Novel Class of Potent Human Deoxyuridine Triphosphatase Inhibitors.2012

    • Author(s)
      H. Miyakoshi, S. Miyahara, K. Endoh, J. Taguchi, M. Nomura, Y. Takao, A. Fujioka, A. Hashimoto, K Itou, K. Yamamura, S. Shuto, H. Nagasawa, M. Fukuoka
    • Journal Title

      J. Med. Chem.

      Volume: 55 Issue: 14 Pages: 6427-6437

    • DOI

      10.1021/jm3004174

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Structure Formation and Catalytic Activity of DNA in Organic Solvents2012

    • Author(s)
      Hiroshi Abe, Naoko Abe, Aya Shibata, Keiji Ito, Yoshiyuki Tanaka, Mika Ito, Hisao Saneyoshi, Satoshi Shuto, and Yoshihiro Ito
    • Journal Title

      Angewandte Chemie International Edition

      Volume: 51 Issue: 26 Pages: 6475-6479

    • DOI

      10.1002/anie.201201111

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Ligand-Free Buchwald-Hartwig Aromatic Aminations of Aryl Halides Catalyzed by Low-Leaching and Highly Recyclable Sulfur-Modified Gold-Supported Palladium Material2012

    • Author(s)
      Mohammad Al-Amin, Tetsuo Honma, Naoyuki Hoshiya, Takatoshi Sato, Satoshi Shuto, Mitsuhiro Arisawa
    • Journal Title

      Adv.Synth.Catal.

      Volume: 354 Issue: 6 Pages: 1061-1068

    • DOI

      10.1002/adsc.201100761

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Design and Synthesis of Indomethacin Analogues That Inhibit P-Glycoprotein and/or Multidrug Resistant Protein without Cox Inhibitory Activity2012

    • Author(s)
      Mitsuhiro Arisawa, Yayoi Kasaya, Tohru Obata, Takuma Sasaki, Tomonori Nakamura, Takuya Araki, Koujirou Yamamoto, Akito Sasaki, Akihito Yamano, Mika Ito, Hiroshi Abe, Yoshihiro Ito, and Satoshi Shuto
    • Journal Title

      Journal of Medicinal Chemistry

      Volume: 55 Issue: 18 Pages: 8152-8163

    • DOI

      10.1021/jm301084z

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] A Conformational Restriction Approach to β-secretase (BACE1) Inhibitors: Effect of a Cyclopropane Ring to Induce an Alternative Binding Mode2012

    • Author(s)
      Shuji Yonezawa
    • Journal Title

      J. Med. Chem.

      Volume: 55 Issue: 20 Pages: 8838-8858

    • DOI

      10.1021/jm3011405

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] One-pot ring-closing metathesis(RCM)/oxidation by an assisted tandem rutheniumcatalysis for the synthesis of 2-quinolones.2012

    • Author(s)
      H. Kato, T. Ishigame, N. Oshima, K. Shimawaki, M. Arisawa, S. Shuto
    • Journal Title

      Adv. Synth. Cat.

      Volume: in press

    • Related Report
      2011 Research-status Report
  • [Journal Article] Alkene isomerization/enamide-ene and diene metathesis for the construction of indoles, quinolines, benzofurans and chromenes with a chiral cyclopropane substituent.2011

    • Author(s)
      T. Kobayashi, M. Arisawa, S. Shuto
    • Journal Title

      Org. Biomol. Chem.

      Volume: 9 Pages: 1219-1224

    • Related Report
      2011 Research-status Report
  • [Journal Article] Design and synthesis of conformationally restricted indomethacin analogues that enhance doxorubicin cytotoxicity in multidrug resistant cells without cyclooxygenase inhibitory activity.2011

    • Author(s)
      M. Arisawa, Y. Kasaya, T. Obata, T. Sasaki, M. Ito, H. Abe, Y. Ito, A. Yamano, S. Shuto
    • Journal Title

      ACS Med. Chem. Lett.

      Volume: 2 Pages: 353-357

    • Related Report
      2011 Research-status Report
  • [Journal Article] Synthesis and characterization of a series of highly fluorogenic substrates for glutathione transferases, a general strategy.2011

    • Author(s)
      J. Zhang, A. Shibata, M. Ito, S. Shuto, Y. Ito, B. Mannervik, H. Abe. R. Morgenstern
    • Journal Title

      J. Am. Chem. Soc.

      Volume: 133 Pages: 14109-14119

    • Related Report
      2011 Research-status Report
  • [Journal Article] Characterization of new potential anti-cancer drugs designed to overcome glutathione transferase mediated resistance.2011

    • Author(s)
      K. Johansson, M. Ito, C. M. S. Schophuizen, S. Mathew, V. Heuser, J. Zhang, M. Shimoji, M. E. Vahter, W. H. Ang, P. J. Dyson, A. Shibata, S. Shuto, Y. Ito, H. Abe, R. Morgenstern
    • Journal Title

      Mol. Pharmaceut.

      Volume: 8 Pages: 1698-1708

    • Related Report
      2011 Research-status Report
  • [Journal Article] Synthesis of a series of 3,4-methanoarginines as side-chain conformationally restricted analogues of arginine.2011

    • Author(s)
      M. Watanabe, K. Yamaguchi, W. Tang, K. Yoshida, R. B. Silverman, M. Arisawa, S. Shuto
    • Journal Title

      Bioorg. Med. Chem.

      Volume: 19 Pages: 5984-5988

    • Related Report
      2011 Research-status Report
  • [Journal Article] Design and Synthesis of Cyclic ADP-4-Thioribose as a Stable Equivalent of Cyclic ADP-Ribose, a Ca-Mobilizing Second Messenger

    • Author(s)
      T. Tsuzuki, N. Sakaguchi, T. Kudoh, S. Takano, M. Uehara, T. Murayama, T. Sakurai, M. Hashii, H. Higashida, K. Weber, A. H. Guse, T. Kameda, T. Hirokawa, Y. Kumaki, B. V. L. Potter,H. Fukuda, M. Arisawa, S. Shuto
    • Journal Title

      Angew.Chem. Int. Ed

      Volume: (印刷中)

    • Related Report
      2012 Final Research Report
  • [Presentation] Ca動員セカンドメッセンジャーの化学 ―細胞内情報伝達系の創薬標的化を目指してー2012

    • Author(s)
      周東 智
    • Organizer
      産業総合研究所・分子標的創薬セミナー2000.12.6
    • Place of Presentation
      産業技術総合研究所生命情報工学研究センター( 東京都)
    • Related Report
      2012 Annual Research Report
    • Invited
  • [Presentation] Ca動員セカンドメッセンジャーの化学-細胞内情報伝達系の創薬標的化を目指して2000

    • Author(s)
      周東智
    • Organizer
      産業総合研究所・分子標的創薬セミナー
    • Place of Presentation
      産業技術総合研究所生命情報工学研究センター(東京都江東区)
    • Year and Date
      2000-12-06
    • Related Report
      2012 Final Research Report

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Published: 2011-08-05   Modified: 2019-07-29  

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