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Development of nuclear medical imaging probes targeting GSK-3beta for early diagnosis of tauopathy

Research Project

Project/Area Number 24659564
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeSingle-year Grants
Research Field Radiation science
Research InstitutionKyoto University

Principal Investigator

SAJI Hideo  京都大学, 薬学研究科(研究院), 教授 (40115853)

Co-Investigator(Renkei-kenkyūsha) 小野 正博  京都大学, 薬学研究科, 准教授 (80336180)
天満 敬  京都大学, 薬学研究科, 助教 (90378787)
木村 寛之  京都大学, 放射性同位元素総合センター, 助教 (50437240)
上田 真史  岡山大学, 医歯薬学総合研究科, 准教授 (40381967)
Project Period (FY) 2012-04-01 – 2014-03-31
Project Status Completed (Fiscal Year 2013)
Budget Amount *help
¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2013: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2012: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
Keywordsタウオパチー / GSK-3β / 認知症 / イメージング / 診断
Research Abstract

In this study, to develop nuclear medical imaging probes targeting GSK-3beta, we newly designed and synthesized 125I-labeled compound based on maleimide scaffold ([125I]7). In biodistribution study in normal mice, [125I]7 showed high brain uptake sufficient for in vivo imaging of GSK-3beta. In addition, in in vitro binding assay using GSK-3beta, compound 7 displayed higher binding affinity for GSK-3beta than indirubin-3'-oxime reported previously as a GSK-3beta inhibitor. These results in this study suggest that it will be feasible to develop nuclear medical imaging probes targeting GSK-3beta by further optimizing the chemical structure.

Report

(3 results)
  • 2013 Annual Research Report   Final Research Report ( PDF )
  • 2012 Research-status Report
  • Research Products

    (6 results)

All 2013 2012

All Journal Article (6 results) (of which Peer Reviewed: 3 results)

  • [Journal Article] Synthesis and biological evaluation of novel styryl benzimidazole derivatives as probes for imaging of neurofibrillary tangles in Alzheimer's disease2013

    • Author(s)
      Matsumura K, Ono M, Yoshimura M, Kimura H, Watanabe H, Okamoto Y, Ihara M, Takahashi R, Saji H
    • Journal Title

      Bioorganic & Medicinal Chemistry

      Volume: 21(11) Pages: 3356-62

    • Related Report
      2013 Final Research Report
  • [Journal Article] Synthesis and biological evaluation of novel styryl benzimidazole derivatives as probes for imaging of neurofibrillary tangles in Alzheimer's disease.2013

    • Author(s)
      Matsumura K, Ono M, Yoshimura M, Kimura H, Watanabe H, Okamoto Y, Ihara M, Takahashi R, Saji H.
    • Journal Title

      Bioorg Med Chem

      Volume: 21 Issue: 11 Pages: 3356-3362

    • DOI

      10.1016/j.bmc.2013.02.054

    • Related Report
      2013 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Molecular Approaches to the Treatment, Prophylaxis, and Diagnosis of Alzheimer's disease2012

    • Author(s)
      Ono M, Saji H
    • Journal Title

      Journal of Pharmacological Science

      Volume: 118 Pages: 338-344

    • Related Report
      2013 Final Research Report
  • [Journal Article] ^<18>F-Labeled phenyl benzothiazole for in vivo imaging of neurofibrillary tangles in Alzheimer's disease brains2012

    • Author(s)
      Matsumura K, Ono M, Kimura H, Ueda M, Nakamoto Y, Togashi K, Okamoto Y, Ihara M, Takahashi R, Saji H.
    • Journal Title

      ACS Medicinal Chemistry Letter

      Volume: 3 Pages: 58-62

    • Related Report
      2013 Final Research Report
  • [Journal Article] Molecular Approaches to the Treatment, Prophylaxis, and Diagnosis of Alzheimer’s Disease: Novel PET/SPECT imaging probes for diagnosis of Alzheimer’s disease.2012

    • Author(s)
      Ono M, Saji H
    • Journal Title

      Journal of Pharmacological Science

      Volume: 118 Pages: 338-344

    • NAID

      10030455553

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] 18F-Labeled phenyldiazenyl benzothiazole for in vivo imaging of neurofibrillary tangles in Alzheimer’s disease brains.2012

    • Author(s)
      Matsumura K, Ono M, Kimura H, Ueda M, Nakamoto Y, Togashi K, Okamoto Y, Ihara M, Takahashi R, Saji H.
    • Journal Title

      ACS Medicinal Chemistry Letter

      Volume: 3 Pages: 58-62

    • Related Report
      2012 Research-status Report
    • Peer Reviewed

URL: 

Published: 2013-05-31   Modified: 2019-07-29  

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