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2013 Fiscal Year Final Research Report

Development of new therapeutic reagents for trypanosoma disease based on the irreversible enzyme inhibition mechanism

Research Project

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Project/Area Number 24651254
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeSingle-year Grants
Research Field Chemical biology
Research InstitutionHokkaido University

Principal Investigator

NISHIMURA Shinichiro  北海道大学, 先端生命科学研究科(研究院), 教授 (00183898)

Project Period (FY) 2012-04-01 – 2014-03-31
KeywordsChargas' disease / Trypanosoma cruzi / sialydase / inhibitor / suicide substrate / nanoparticle / nanomedicine
Research Abstract

Cardiopathy caused by the protozoan Trypanosoma cruzi, the etiologic agent of Chargas' disease, is the main cause of death in endemic regions of Latin America. Since nifurtimox and benznidazole are approved as therapeutic reagents for this disease, the efficacy is limited and serious side effects and toxicity were reported. Therefore, advent of novel therapeutic reagents has been strongly required.
We have discovered by collaborative research with a team at University of Rio de Janeiro that some suicide substrate-based derivatives of sialidases become a new class of leads toward drugs for the treatment of infectious diseases related to the Chargas' disease. In the present study, we aimed to establish for the general protocol for the assembling suicide substrate-based derivatives on the surface of nanoparticles that can convert into practically promising level of therapeutic reagents candidates as "nanomedicine".

  • Research Products

    (6 results)

All 2014 2013 2012

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

  • [Journal Article] Synthesis of neoglycosphingolipid from nethoxyamino-functionalized ceramide2014

    • Author(s)
      Ishida J., Hinou H., Naruchi K., Nishimura S-I.
    • Journal Title

      Bioorg. Med. Chem. Lett

      Volume: 24巻 Pages: 1197-1200

    • DOI

      10.1016/j.bmcl.2013.12.091

    • Peer Reviewed
  • [Journal Article] A New Approach for the Synthesis of Hyper-Branched N-Glycan Core Structures from Locust Bean Gum2013

    • Author(s)
      Kumar R., Naruchi K., Miyoshi R., Hinou H., Nishimura S-I.
    • Journal Title

      Org. Lett

      Volume: 15巻 Pages: 6278-6281

    • DOI

      10.1021/ol403140h

    • Peer Reviewed
  • [Journal Article] Attomolar Detection of Influenza A Virus Hemagglutinin Human H1 and Avian H5 Using Glycan-blotted Field Effect Transistor Biosensor2013

    • Author(s)
      Hideshima S., Hinou H., Ebihara D., Sato R., Kuroiwa S., Nakanishi T., Nishimura S-I., Osaka T.
    • Journal Title

      Anal. Chem

      Volume: 85巻 Pages: 5641-5644

    • DOI

      10.1021/ac401085c

    • Peer Reviewed
  • [Journal Article] Fluorescence polarization-based assay using N-glycan-conjugated quantum dots for screening in hemagglutinin blockers for influenza A viruses2013

    • Author(s)
      Okamatsu M., Feng F., Ohyanagi T., Nagahori N., Someya K., Sakoda Y., Miura N., Nishimura S-I., Kida H.
    • Journal Title

      J. Virol. Methods

      Volume: 187巻 Pages: 390-394

    • DOI

      10.1016/j.jviromet.2012.11.004

    • Peer Reviewed
  • [Journal Article] Macrocyclic Mechanism-based Inhibitor for Neuraminidases2013

    • Author(s)
      Kai H, Hinou H, Naruchi K., Matsushita T., Nishimura S-I.
    • Journal Title

      Chem. Eur. J

      Volume: 19巻 Pages: 1364-1372

    • DOI

      10.1002/chem.201200859

    • Peer Reviewed
  • [Journal Article] Aglycone-focused randomization of 2-difluoromethylphenylsialoside-type suicide substrates for neuraminidases2012

    • Author(s)
      Kai H, Hinou H, Nishimura S-I.
    • Journal Title

      Bioorgan. Med. Chem

      Volume: 20巻 Pages: 3729-2746

    • DOI

      10.1016/j.bmc.2012.02.001

    • Peer Reviewed

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Published: 2015-06-25  

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