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Development of anti-HIV agents for the viral variants

Research Project

Project/Area Number 21590506
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Virology
Research InstitutionChiba University

Principal Investigator

HOSHINO Tyuji  千葉大学, 大学院・薬学研究院, 准教授 (90257220)

Project Period (FY) 2009 – 2011
Project Status Completed (Fiscal Year 2011)
Budget Amount *help
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2011: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2010: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2009: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Keywords分子 / 阻害剤開発 / 変異体ウイルス / 薬剤耐性 / シミュレーション / 分子動力学計算 / プロテアーゼ阻害剤 / 有機合成 / 薬物設計 / 合成経路
Research Abstract

In order to produce the anti-HIV agents effective for the viral variants, we carried out in silico drug design, organic synthesis, and assay of the compound potency. The designed compounds were intended to be targeted on the I84V and V82A mutants of HIV-1 protease. Several compounds were synthesized, and some of the intermediates of the designed compounds showed anti-viral activity. It is required to enhance the compound potency greatly. Accordingly, the modification of the derivatives should be performed to produce a potent agent in our future work.

Report

(4 results)
  • 2011 Annual Research Report   Final Research Report ( PDF )
  • 2010 Annual Research Report
  • 2009 Annual Research Report
  • Research Products

    (10 results)

All 2012 2011 2010 Other

All Journal Article (6 results) (of which Peer Reviewed: 6 results) Presentation (2 results) Remarks (2 results)

  • [Journal Article] Structural Modulation Study of Inhibitory Compounds for RN ase H Activity of HIV-1 Reverse Transcriptase2012

    • Author(s)
      H. Yanagita, S. Fudo, E. Urano, R. Ichikawa, M. Ogata, M. Yokota, T. Murakami, H. Wu, J. Chiba, J. Komano, T. Hoshino
    • Journal Title

      Chemical and Pharmaceutical Bulletin

      Volume: 60巻(印刷中)

    • Related Report
      2011 Final Research Report
    • Peer Reviewed
  • [Journal Article] Structural Modulation Study of Inhibitory Compounds for RNase H Activity of HIV-1 Reverse Transcriptase2012

    • Author(s)
      H.Yanagita, S.Fudo, E.Urano, R.Ichikawa, M.Ogata, M.Yokota, T.Murakami, H.Wu, J.Chiba, J.Komano, T.Hoshino
    • Journal Title

      Chemical and Pharmaceutical Bulletin

      Volume: 60(in press)

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Structural and Biochemical Study on the Inhibitory Activity of Derivatives of5-nitro-furan-2-carboxylic acid for RNase H Function of HIV-1 Reverse Transcriptase2011

    • Author(s)
      H. Yanagita, E. Urano, K. Matsumoto, R. Ichikawa, Y. Takaesu, M. Ogata, T. Murakami, H. G. Wu, J. Chiba, J. Komano, T. Hoshino
    • Journal Title

      Bioorganic Medicinal Chemistry

      Volume: 19巻 Pages: 816-825

    • Related Report
      2011 Final Research Report
    • Peer Reviewed
  • [Journal Article] Structural and Biochemical Study on the Inhibitory Activity of Derivatives of 5-nitro-furan-2-carboxylic acid for RNase H Function of HIV -1 Reverse Transcriptase2011

    • Author(s)
      H.Yanagita, E.Urano, K.Matsumoto, R.Ichikawa, Y.Takaesu, M.Ogata, T.Murakami, H.G.Wu, J.Chiba, J.Komano, T.Hoshino
    • Journal Title

      Bioorganic Medical Chemistry

      Volume: 19 Pages: 816-825

    • Related Report
      2010 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Structural and Energetic Analysis onthe Complexes of Clinically-isolated Subtype C HIV-1 Proteases and Approved Inhibitors by Molecular Dynamics Simulation2010

    • Author(s)
      S. Matsuyama, A. Aydan, H. Ode, M. Hata, W. Sugiura, T. Hoshino
    • Journal Title

      Journal of Physical Chemistry B

      Volume: 114巻 Pages: 521-530

    • Related Report
      2011 Final Research Report
    • Peer Reviewed
  • [Journal Article] Structural and Energetic Analysis on the Complexes of Clinically-isolated Subtype C HIV-1 Proteases and Approved Inhibitors by Molecular Dynamics Simulation2010

    • Author(s)
      S.Matsuyama, A.Aydan, H.Ode, M.Hata, W.Sugiura, T.Hoshino
    • Journal Title

      Journal of Physical Chemistry B 114

      Pages: 521-530

    • Related Report
      2009 Annual Research Report
    • Peer Reviewed
  • [Presentation] V82A,I84V変異を標的としたHIV-1プロテアーゼ阻害薬の設計2010

    • Author(s)
      藍檀愛, 萩原洋子, 鈴木優章, 根矢三郎, 星野忠次
    • Organizer
      日本薬学会第130年会
    • Place of Presentation
      岡山
    • Year and Date
      2010-03-29
    • Related Report
      2011 Final Research Report
  • [Presentation] V82A, I84V変異を標的としたHIV-1プロテアーゼ阻害薬の設計2010

    • Author(s)
      藍檀愛, 萩原洋子, 鈴木優章, 根矢三郎, 星野忠次
    • Organizer
      日本薬学会第130年会
    • Place of Presentation
      岡山コンベンションセンター(岡山県)
    • Year and Date
      2010-03-29
    • Related Report
      2009 Annual Research Report
  • [Remarks]

    • URL

      http://www.p.chiba-u.ac.jp/lab/bukka/index.html

    • Related Report
      2011 Final Research Report
  • [Remarks]

    • URL

      http://www.p.chiba-u.ac.jp/lab/bukka/index.html

    • Related Report
      2011 Annual Research Report

URL: 

Published: 2009-04-01   Modified: 2016-04-21  

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