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Development of novel probes for in vivo imaging of b-secretase activity in the brain

Research Project

Project/Area Number 15K19785
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeMulti-year Fund
Research Field Radiation science
Research InstitutionKyoto University

Principal Investigator

Watanabe Hiroyuki  京都大学, 薬学研究科, 助教 (40710786)

Project Period (FY) 2015-04-01 – 2017-03-31
Project Status Completed (Fiscal Year 2016)
Budget Amount *help
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2016: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2015: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Keywordsβセクレターゼ / アルツハイマー / イメージング / SPECT / アルツハイマー病 / 分子イメージング / PET/SPECT
Outline of Final Research Achievements

The deposition of amyloid β (Aβ) aggregates is the key neurodegenerative event of Alzheimer’s disease (AD). The cleavage of amyloid precursor protein (APP) by β-secretase is the first step of Aβ formation. Therefore, in vivo imaging of β-secretase activity would be useful for the diagnosis of AD. The aim of this study is to develop novel probes for in vivo imaging of β-secretase activity in the brain. We designed and synthesized [125I]PSCP based on the strategy of metabolic trapping. In vitro cleavage assay, [125I]PSCP was cleaved by β-secretase in a time dependent manner. In order to evaluate brain uptake of [125I]PSCP, in vivo biodistribution study using normal mice was performed. [125I]PSCP showed higher brain uptake compared with [125I]SCP, which has no cell penetrating peptide. These results suggest that [125I]PSCP has a potential as a probe for imaging β-secretase activity in the brain.

Report

(3 results)
  • 2016 Annual Research Report   Final Research Report ( PDF )
  • 2015 Research-status Report
  • Research Products

    (6 results)

All 2016 2015 Other

All Presentation (4 results) (of which Invited: 1 results) Remarks (2 results)

  • [Presentation] 脳βセクレターゼの酵素活性の核医学イメージングを目的とした新規SPECT用プローブの開発2016

    • Author(s)
      川崎 梓, 渡邊裕之, 小野正博, 佐治英郎
    • Organizer
      第56回日本核医学会
    • Place of Presentation
      名古屋
    • Year and Date
      2016-11-03
    • Related Report
      2016 Annual Research Report
  • [Presentation] βセクレターゼの酵素活性を標的とした新規放射性ヨウ素標識プローブの開発2016

    • Author(s)
      渡邊裕之、川崎 梓、小野正博、佐治英郎
    • Organizer
      第11回日本分子イメージング学会学術集会
    • Place of Presentation
      神戸市
    • Year and Date
      2016-05-28
    • Related Report
      2015 Research-status Report
  • [Presentation] アルツハイマー病の早期診断および治療薬開発のための分子イメージングプローブの開発2016

    • Author(s)
      渡邊 裕之
    • Organizer
      第136年会日本薬学会
    • Place of Presentation
      横浜市
    • Year and Date
      2016-03-27
    • Related Report
      2015 Research-status Report
  • [Presentation] アルツハイマー病の診断・治療のための核医学分子イメージングプローブの開発2015

    • Author(s)
      渡邊 裕之
    • Organizer
      第28回バイオメディカル分析化学シンポジウム
    • Place of Presentation
      長崎市
    • Year and Date
      2015-08-21
    • Related Report
      2015 Research-status Report
    • Invited
  • [Remarks] 京都大学大学院薬学研究科・病態機能分析学分野

    • URL

      http://www.pharm.kyoto-u.ac.jp/byotai/

    • Related Report
      2016 Annual Research Report
  • [Remarks] 京都大学大学院薬学研究科 病態機能分析学分野

    • URL

      http://www.pharm.kyoto-u.ac.jp/byotai/

    • Related Report
      2015 Research-status Report

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Published: 2015-04-16   Modified: 2018-03-22  

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