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Development of practical synthetic method of radiobromine-labeled peptides for PET imaging

Research Project

Project/Area Number 15K09946
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Radiation science
Research InstitutionGunma University

Principal Investigator

Yamada Keiichi  群馬大学, 大学院理工学府, 准教授 (70323334)

Research Collaborator Watanabe Shigeki  
Hanaoka Hirofumi  
Project Period (FY) 2015-04-01 – 2019-03-31
Project Status Completed (Fiscal Year 2018)
Budget Amount *help
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2017: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2016: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2015: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
KeywordsPET薬剤 / 生物活性ペプチド / 放射性臭素 / 標識合成 / PETイメージング / 環状ペプチド / 腫瘍標的化ペプチド / PET診断薬
Outline of Final Research Achievements

We developed facile synthetic method of radiobromine-labeled bioactive peptides via electrophilic desilylation. In this study, we synthesized bromine-77 labeled cyclic RGD peptide in good radiochemical yield.

Academic Significance and Societal Importance of the Research Achievements

本研究で開発した標識合成法は核医学的診断に資する新規放射性ペプチド薬剤の合成に適用できるため、腫瘍をはじめとする様々な疾病の非侵襲的診断やRI内用療法に基づく放射線治療への応用が期待される。また、放射性臭素は現在実用化されている放射性フッ素よりも半減期が長いため、遠隔地への標識化合物の輸送が実現できれば、RI製造設備を持たない医療機関でのPET検査などに利用できる可能性がある。

Report

(5 results)
  • 2018 Annual Research Report   Final Research Report ( PDF )
  • 2017 Research-status Report
  • 2016 Research-status Report
  • 2015 Research-status Report
  • Research Products

    (16 results)

All 2019 2018 2017 2016 2015 Other

All Journal Article (5 results) (of which Int'l Joint Research: 1 results,  Peer Reviewed: 4 results,  Acknowledgement Compliant: 1 results) Presentation (10 results) (of which Int'l Joint Research: 3 results) Remarks (1 results)

  • [Journal Article] A convenient and reproducible method for the synthesis of astatinated 4-[211At]astato-l-phenylalanine via electrophilic desilylation2019

    • Author(s)
      Watanabe Shigeki、Azim Mohammad Anwar-Ul、Nishinaka Ichiro、Sasaki Ichiro、Ohshima Yasuhiro、Yamada Keiichi、Ishioka Noriko S.
    • Journal Title

      Organic & Biomolecular Chemistry

      Volume: 17 Issue: 1 Pages: 165-171

    • DOI

      10.1039/c8ob02394h

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] 放射性ペプチド薬剤の標識合成と診断・治療への展開:現状と課題2019

    • Author(s)
      山田圭一
    • Journal Title

      Bio Industry

      Volume: 36 Pages: 75-81

    • Related Report
      2018 Annual Research Report
  • [Journal Article] Synthesis and Characterization of Radiobromine-labeled Bioactive Peptides for Molecular Imaging2018

    • Author(s)
      Keiichi Yamada, Shigeki Watanabe, Ichiro Sasaki, Hirofumi Hanaoka, and Noriko S. Ishioka
    • Journal Title

      Peptide Science 2017

      Volume: -

    • Related Report
      2017 Research-status Report
    • Peer Reviewed
  • [Journal Article] PET薬剤を指向した放射性ハロゲン標識化合物の開発:現状と課題2017

    • Author(s)
      山田圭一
    • Journal Title

      Bio Clinica

      Volume: 32 Pages: 66-71

    • Related Report
      2017 Research-status Report
    • Peer Reviewed
  • [Journal Article] Synthesis and properties of silylated phenylalanine derivatives2016

    • Author(s)
      K. Yamada, S. Watanabe, S. Watanabe, T. Takahashi, T. Moriguchi, H. Oku, N. S. Ishioka, and K. Shinozuka
    • Journal Title

      Peptide Science 2015

      Volume: 52 Pages: 93-94

    • Related Report
      2015 Research-status Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Presentation] ケイ素―ハロゲン交換反応を用いた放射性臭素標識化合物合成に関する基礎的検討2018

    • Author(s)
      渡辺茂樹,山田圭一,佐々木一郎,石岡典子
    • Organizer
      第2回日本核医学会分科会放射薬品科学研究会/第18回放射性医薬品・画像診断薬研究会
    • Related Report
      2018 Annual Research Report
  • [Presentation] ケイ素ーアスタチン交換反応を用いたアスタチン標識アミノ酸誘導体の合成2018

    • Author(s)
      渡辺茂樹,Mohammad Anwar-UlAzim,西中一朗,佐々木一郎,大島康宏,山田圭一,石岡典子
    • Organizer
      第62回放射化学討論会
    • Related Report
      2018 Annual Research Report
  • [Presentation] 有機ケイ素前駆体を用いたアスタチン標識アミノ酸の合成2018

    • Author(s)
      渡辺茂樹,Mohammad Anwar-UlAzim,西中一朗,佐々木一郎,大島康宏,山田圭一,石岡典子
    • Organizer
      第58回日本核医学会学術総会
    • Related Report
      2018 Annual Research Report
  • [Presentation] ケイ素-ハロゲン交換反応を利用した放射性臭素標識ペプチドの合成研究2017

    • Author(s)
      山田圭一, 渡辺茂樹, 佐々木一郎, 花岡宏史, 石岡典子
    • Organizer
      第17回放射性医薬品画像診断薬研究会
    • Related Report
      2017 Research-status Report
  • [Presentation] 有機ケイ素前駆体を用いた放射性臭素標識アミノ酸誘導体の合成2017

    • Author(s)
      渡辺茂樹, 佐々木一郎, 山田圭一, 石岡典子
    • Organizer
      第57回日本核医学会学術総会
    • Related Report
      2017 Research-status Report
  • [Presentation] ynthesis and Characterization of Radiobromine-labeled Bioactive Peptides for Molecular Imaging2017

    • Author(s)
      K. Yamada, S. Watanabe, I. Sasaki, H. Hanaoka, and N. S. Ishioka
    • Organizer
      第54回ペプチド討論会
    • Related Report
      2017 Research-status Report
  • [Presentation] Synthesis and Biological Evaluation of N-Methylated Cyclic Pentapeptides against Malignant Breast Cancer Cell Lines2016

    • Author(s)
      K. Yamada, S. Rokudai, R. Kawabata, M. Nishiyama K. Shinozuka
    • Organizer
      3rd International Symposium of Gunma University Medical Innovation
    • Place of Presentation
      Kiryu, Gunma
    • Related Report
      2016 Research-status Report
    • Int'l Joint Research
  • [Presentation] Synthesis and properties of silylated phenylalanine derivatives and its application to bioactive cyclic peptides2015

    • Author(s)
      K. Yamada, S. Watanabe, S. Watanabe, S. Torii, N. S. Ishioka, and K. Shinozuka
    • Organizer
      2nd International Symposium of Gunma University Medical Innovation
    • Place of Presentation
      Gunma University, Maebashi, Japan
    • Year and Date
      2015-12-08
    • Related Report
      2015 Research-status Report
    • Int'l Joint Research
  • [Presentation] Synthesis and properties of silylated phenylalanine derivatives2015

    • Author(s)
      K. Yamada, S. Watanabe, S. Watanabe, T. Takahashi, T. Moriguchi, H. Oku, N. S. Ishioka, and K. Shinozuka
    • Organizer
      52nd Japanese Peptide Symposium
    • Place of Presentation
      Hiratsuka City Hall, Hiratsuka, Japan
    • Year and Date
      2015-11-15
    • Related Report
      2015 Research-status Report
  • [Presentation] Synthesis of a Radiobrominated Amino Acid Derivatives via Silicon-Bromine Exchange Reaction2015

    • Author(s)
      S. Watanabe, K. Yamada, S. Watanabe, H. Oku, T. Moriguchi, K. Shinozuka, N. S. Ishioka
    • Organizer
      21st International symposium on Radiopharmaceutical Sciences
    • Place of Presentation
      Missouri, USA
    • Year and Date
      2015-05-26
    • Related Report
      2015 Research-status Report
    • Int'l Joint Research
  • [Remarks] Dr. Yamada Homepage

    • URL

      http://peptide-chem.chem-bio.st.gunma-u.ac.jp/yamada/yamada-index.html

    • Related Report
      2015 Research-status Report

URL: 

Published: 2015-04-16   Modified: 2020-03-30  

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