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Development of Radio-Theranostics molecular probes for prostate cancer

Research Project

Project/Area Number 18K15566
Research Category

Grant-in-Aid for Early-Career Scientists

Allocation TypeMulti-year Fund
Review Section Basic Section 52040:Radiological sciences-related
Research InstitutionKyoto College of Medical Science (2020-2021)
Kyoto Pharmaceutical University (2018-2019)

Principal Investigator

Yagi Yusuke  京都医療科学大学, 医療科学部, 助教 (90802207)

Project Period (FY) 2018-04-01 – 2022-03-31
Project Status Completed (Fiscal Year 2021)
Budget Amount *help
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2020: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2019: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2018: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywords前立腺特異的膜抗原 / PSMA / PET / SPECT / マイクロ波合成 / 標識合成 / 迅速合成 / ラジオセラノスティクス / 前立腺がん / ウレア誘導体 / ユニットカップリング型プローブ / マイクロ波 / 放射線科学 / 分子イメージング / がん治療 / 放射性医薬品
Outline of Final Research Achievements

Prostate cancer is a disease that causes an increasing number of deaths each year. Since early detection of prostate cancer is expected to cure the disease, nuclear medicine molecular probes have been developed. In this study, we developed molecular probes targeting Prostate-specific membrane antigen (PSMA) for the purpose of radio-theranostics (the integration of diagnosis and treatment using radioisotopes).
As a result, we found a novel microwave labeling method for the radionuclide Ga-68 and a candidate compound that shows accumulation against prostate cancer.

Academic Significance and Societal Importance of the Research Achievements

本研究では、ユニットカップリング型分子プローブ(UCMP)創製法を導入した前立腺がんRadio-Theranosticsプローブ開発を行い、画像診断と治療を融合させた新しい前立腺がん治療の個別化、効率化を目指した。これまで本方法論で前立腺がん用分子プローブの開発は今までにない。また本方法論は様々な分子プローブの開発に応用可能である。今回、本研究で見出したマイクロ波を用いたGa-68標識法は短半減期放射性核種に非常に有用であり、他の放射性核種標識に貢献できると考えられる。

Report

(5 results)
  • 2021 Annual Research Report   Final Research Report ( PDF )
  • 2020 Research-status Report
  • 2019 Research-status Report
  • 2018 Research-status Report
  • Research Products

    (11 results)

All 2021 2020 2019 2018 Other

All Journal Article (6 results) (of which Int'l Joint Research: 2 results,  Peer Reviewed: 6 results,  Open Access: 2 results) Presentation (3 results) (of which Int'l Joint Research: 1 results) Book (1 results) Remarks (1 results)

  • [Journal Article] A Putative Single-Photon Emission CT Imaging Tracer for Erythropoietin-Producing Hepatocellular A2 Receptor2021

    • Author(s)
      Furukawa Takenori、Kimura Hiroyuki、Torimoto Hanae、Yagi Yusuke、Kawashima Hidekazu、Arimitsu Kenji、Yasui Hiroyuki
    • Journal Title

      ACS Medicinal Chemistry Letters

      Volume: 12 Issue: 8 Pages: 1238-1244

    • DOI

      10.1021/acsmedchemlett.1c00030

    • Related Report
      2021 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] Copper-mediated radioiodination reaction through aryl boronic acid or ester precursor and its application to direct radiolabeling of a cyclic peptide2021

    • Author(s)
      Yuto Kondo, Hiroyuki Kimura, Chiaki Fukumoto, Yusuke Yagi, Yasunao Hattori, Hidekazu Kawashima, Hiroyuki Yasui
    • Journal Title

      Journal of Labelled Compounds and Radiopharmaceuticals

      Volume: - Issue: 8 Pages: 336-345

    • DOI

      10.1002/jlcr.3925

    • Related Report
      2021 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Synthesis of 18F-labeled streptozotocin derivatives and an in-vivo kinetics study using positron emission tomography2020

    • Author(s)
      Arimitsu Kenji、Yagi Yusuke、Koshino Kazuhiro、Nishito Yukina、Higuchi Takahiro、Yasui Hiroyuki、Kimura Hiroyuki
    • Journal Title

      Bioorganic & Medicinal Chemistry Letters

      Volume: 30 Issue: 17 Pages: 127400-127400

    • DOI

      10.1016/j.bmcl.2020.127400

    • Related Report
      2020 Research-status Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Journal Article] Aicardi-Goutieres syndrome-like encephalitis in mutant mice with constitutively active MDA52020

    • Author(s)
      Onizawa Hideo、Kato Hiroki、Kimura Hiroyuki、Kudo Tomoo、Soda Nobumasa、Shimizu Shota、Funabiki Masahide、Yagi Yusuke、Nakamoto Yuji、Priller Josef、Nishikomori Ryuta、Heike Toshio、Yan Nan、Tsujimura Tohru、Mimori Tsuneyo、Fujita Takashi
    • Journal Title

      International Immunology

      Volume: 33 Issue: 4 Pages: 225-240

    • DOI

      10.1093/intimm/dxaa073

    • Related Report
      2020 Research-status Report
    • Peer Reviewed
  • [Journal Article] Efficient gallium-68 radiolabeling reaction of DOTA derivatives using a resonant-type microwave reactor2019

    • Author(s)
      Yagi Yusuke、Shimizu Yoichi、Arimitsu Kenji、Nakamoto Yuji、Higuchi Takahiro、Togashi Kaori、Kimura Hiroyuki
    • Journal Title

      Journal of Labelled Compounds and Radiopharmaceuticals

      Volume: 62 (3) Issue: 3 Pages: 132-138

    • DOI

      10.1002/jlcr.3704

    • Related Report
      2018 Research-status Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Structure?activity relationships of succinimidyl-Cys-C(O)-Glu derivatives with different near-infrared fluorophores as optical imaging probes for prostate-specific membrane antigen2018

    • Author(s)
      Matsuoka Daiko、Watanabe Hiroyuki、Shimizu Yoichi、Kimura Hiroyuki、Yagi Yusuke、Kawai Ryoko、Ono Masahiro、Saji Hideo
    • Journal Title

      Bioorganic & Medicinal Chemistry

      Volume: 26 Issue: 9 Pages: 2291-2301

    • DOI

      10.1016/j.bmc.2018.03.015

    • Related Report
      2018 Research-status Report
    • Peer Reviewed
  • [Presentation] F-18標識ボロン酸誘導体との鈴木カップリング反応を用いた新規F-18標識法の開発2021

    • Author(s)
      屋木祐亮、近藤悠斗、樋口隆弘、木村寛之
    • Organizer
      日本薬学会第142年会
    • Related Report
      2021 Annual Research Report
  • [Presentation] In vitro characterization of metabolic trapping of a novel PET tracer for fatty acid oxidation, 18F-AS3504073-002020

    • Author(s)
      Yasuhiro OHSHIMA, Yusuke YAGI, Hiroshi FUSHIKI, Christoph MAACK, Takahiro HIGUCHI
    • Organizer
      EANM'20 virtual edition
    • Related Report
      2020 Research-status Report
    • Int'l Joint Research
  • [Presentation] 共振空洞型マイクロ波反応装置を用いた68Ga錯体形成反応の基礎評価2018

    • Author(s)
      屋木祐亮, 木村寛之, 志水陽一, 有光健治, 中本裕士, 富樫かおり, 安井裕之
    • Organizer
      第138回日本薬学会年会
    • Related Report
      2018 Research-status Report
  • [Book] Handbook of in vivo chemistry in mice : from lab to living system2020

    • Author(s)
      Katsunori Tanaka (Editor), Kenward Vong (Editor)
    • Total Pages
      560
    • Publisher
      WILEY
    • ISBN
      9783527344321
    • Related Report
      2020 Research-status Report
  • [Remarks] 京都薬科大学代謝分析学分野・研究業績

    • URL

      https://dabc.jp/?page_id=591

    • Related Report
      2018 Research-status Report

URL: 

Published: 2018-04-23   Modified: 2023-01-30  

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