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Development of GLP-1 based imaging probes focused on extrapancreatic action of glucagon-like peptide receptor agonist

Research Project

Project/Area Number 16K19880
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeMulti-year Fund
Research Field Radiation science
Research InstitutionOsaka University of Pharmaceutical Sciences (2017-2018)
National Cardiovascular Center Research Institute (2016)

Principal Investigator

Naoya Kondo  大阪薬科大学, 薬学部, 助教 (80756172)

Project Period (FY) 2016-04-01 – 2019-03-31
Project Status Completed (Fiscal Year 2018)
Budget Amount *help
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2018: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2017: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2016: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Keywords放射性医薬品 / GLP-1 / 核医学イメージング / 前立腺がん
Outline of Final Research Achievements

In this study, we focused on the extrapancreatic action of glucagon-like peptide receptor agonist (GLP-1RA) and developed a novel imaging probe that enables quantification of GLP-1R expression in vivo. In addition, we developed novel probes targeting MMPs, representative markers of inflammatory diseases which are therapeutic targets for GLP-1 RA. The novel GLP-1R imaging probe achieves high specific activity, convenient labeling, and high accumulation in pancreas, which is a GLP-1R high expression tissue. And co-localization of the radioactive accumulation region and the GLP-1R expression region were observed. As a result, it was shown to be effective as a GLP-1R imaging probe. On the other hand, the accumulation in prostate cancer tissues that have been reported to have therapeutic effects by GLP-1RA is low. Therefore, the correlation between the therapeutic effects and the amount of GLP-1R expression needs to be examined in detail in the future.

Academic Significance and Societal Importance of the Research Achievements

GLP-1Rはインスリン放出に関わるターゲットとして着目されており、GLP-1Rアゴニストが糖尿病治療薬として上市されている。近年の研究では、GLP-1Rアゴニストは、がん、動脈硬化、アルツハイマー病など多様な疾患への治療効果を有することが示され、GLP-1Rの各疾患での機能、GLP-1Rアゴニストの生体内挙動の解明が求められている。本研究ではGLP-1Rイメージングプローブの開発やGLP-1Rの治療標的となる炎症性疾患のマーカーを標的としたイメージングプローブの開発に成功した。本研究成果はGLP-1R作動薬と治療に関連する今後の診断・治療領域の医療に有益な情報をもたらすと考えられる。

Report

(4 results)
  • 2018 Annual Research Report   Final Research Report ( PDF )
  • 2017 Research-status Report
  • 2016 Research-status Report
  • Research Products

    (8 results)

All 2019 2018 2017

All Journal Article (2 results) (of which Int'l Joint Research: 2 results,  Peer Reviewed: 2 results,  Open Access: 1 results) Presentation (6 results) (of which Int'l Joint Research: 1 results)

  • [Journal Article] Development of matrix metalloproteinase-targeted probes for lung inflammation detection with positron emission tomography2018

    • Author(s)
      Kondo N, Temma T, Aita K, Shimochi S, Koshino K, Senda M, Iida H.
    • Journal Title

      Sci Rep

      Volume: 8 Issue: 1 Pages: 1347-1347

    • DOI

      10.1038/s41598-018-19890-1

    • Related Report
      2018 Annual Research Report 2017 Research-status Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Journal Article] Development of matrix metalloproteinase-targeted probes for PET imaging of COPD.2017

    • Author(s)
      Kondo Naoya、Temma Takashi、Aita Kazuki、Shimochi Saeka、Koshino Kazuhiro、Senda Michio、Iida Hidehiro
    • Journal Title

      Journal of Nuclear Medicine

      Volume: 58 (no. supplement 1) Pages: 474-474

    • Related Report
      2017 Research-status Report
    • Peer Reviewed / Int'l Joint Research
  • [Presentation] 糖尿病薬リキシセナチドを母体としたGLP-1受容体標的イメージングプローブの開発2019

    • Author(s)
      池田 有快、近藤 直哉、大石 綾香、平田 雅彦、天滿 敬
    • Organizer
      日本薬学会第139年会
    • Related Report
      2018 Annual Research Report
  • [Presentation] CD147/EMMPRIN結合ペプチドAP9を母体とする放射性ヨウ素標識ペプチドプローブの開発2019

    • Author(s)
      中林 真理、近藤 直哉、土屋 友亮、平田 雅彦、天滿 敬
    • Organizer
      日本薬学会第139年会
    • Related Report
      2018 Annual Research Report
  • [Presentation] 動脈硬化の質的診断を目的とした酸化LDL結合性核医学イメージングプローブの開発2018

    • Author(s)
      近藤 直哉、天滿 敬、依田敬子、西郡寛太郎、尾江悟、塩見雅志、小野正博、佐治英郎
    • Organizer
      第5回日本ウサギバイオサイエンス研究会学術集会
    • Related Report
      2018 Annual Research Report
  • [Presentation] 疾患におけるマトリックスメタロプロテアーゼ発現のインビボ定量法構築を目的とした核医学イメージングプローブの開発2018

    • Author(s)
      近藤 直哉、天滿 敬、相田 一樹、下地 佐恵香、千田 道雄、飯田 秀博
    • Organizer
      第68回 日本薬学会近畿支部総会・大会
    • Related Report
      2018 Annual Research Report
  • [Presentation] Development of matrix metalloproteinase-targeted probes for PET imaging of COPD.2017

    • Author(s)
      Kondo Naoya、Temma Takashi、Aita Kazuki、Shimochi Saeka、Koshino Kazuhiro、Senda Michio、Iida Hidehiro
    • Organizer
      Society of Nuclear Medicine and Molecular Imaging 64th Annual Meeting
    • Related Report
      2017 Research-status Report
    • Int'l Joint Research
  • [Presentation] 前立腺がんに発現するGLP-1受容体を標的とした新規放射性ヨウ素標識プローブの開発2017

    • Author(s)
      近藤 直哉、天滿 敬、下地 佐恵香、飯田 秀博
    • Organizer
      日本薬学会 第137年会
    • Place of Presentation
      仙台
    • Related Report
      2016 Research-status Report

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Published: 2016-04-21   Modified: 2020-03-30  

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