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2011 Fiscal Year Final Research Report

Development of anti-HIV agents for the viral variants

Research Project

  • PDF
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
Keywords分子 / 阻害剤開発
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.

  • Research Products

    (5 results)

All 2012 2011 2010 Other

All Journal Article (3 results) (of which Peer Reviewed: 3 results) Presentation (1 results) Remarks (1 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)

    • 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

    • 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

    • 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
  • [Remarks]

    • URL

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

URL: 

Published: 2013-07-31  

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