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Study on radiolabeling using nucleic acid RNAi medicine

Research Project

Project/Area Number 15K15460
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeMulti-year Fund
Research Field Radiation science
Research InstitutionGihu University of Medical Science

Principal Investigator

Nagai Makoto  岐阜医療科学大学, 保健科学部, 准教授 (30460497)

Co-Investigator(Kenkyū-buntansha) 片渕 哲朗  岐阜医療科学大学, 保健科学部, 教授 (00393231)
Project Period (FY) 2015-04-01 – 2018-03-31
Project Status Completed (Fiscal Year 2017)
Budget Amount *help
¥3,510,000 (Direct Cost: ¥2,700,000、Indirect Cost: ¥810,000)
Fiscal Year 2017: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000)
Fiscal Year 2016: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2015: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywords放射性医薬品 / 核酸医薬品 / 放射性 / RNAi / 放射性核酸医薬品 / ケモインフォマティクス / シミュレーション / 分子軌道法 / 薬学 / 放射線 / 遺伝子 / 核酸
Outline of Final Research Achievements

Radiopharmaceuticals of RNA medicine have not been found. In this research, we aimed to prepare radioactive nucleic acid drugs that withstand metallic labels and bound to target genes. Molecular design of RNAi drugs that specifically accumulate in human cancer cells even after radiolabeling was designed by molecular orbital method. As a result, substitution at the 5-position hydrogen atom of uracil resulted in not impairing the hybrid ability of the base even when labeling was carried out. Synthetic addition of nonradioactive iodine from BNA or LNA as a raw material was prepared, added to human leukemia cultured cells, and cell growth rate after culturing was measured. The transcription inhibition rate of the synthesized and added RNAi medicine was a result which was not different from usual.

Academic Significance and Societal Importance of the Research Achievements

本研究が目指す成果は、点在するがん細胞等の検査や治療薬として使用できる核酸医薬品の開発である。本研究成果は分子量の大きい放射性物質を核酸断片に結合させることで、核酸断片が金属との凝集の防止と自由度の確保をする分子設計法および分子モデルとして結果が得られた。
放射性物質を用いた核酸分子設計に関する合成法の報告は数少なく学術的にも意義があった。また、今後、細胞内への導入確認および検査・治療等への応用ができれば、点在するがん治療への対応が可能となり社会的意義はあると思われる。

Report

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

    (7 results)

All 2018 2017 2016

All Journal Article (6 results) (of which Peer Reviewed: 4 results,  Open Access: 4 results) Presentation (1 results)

  • [Journal Article] Effect of St John’s Wort on the pharmacokinetics and expression of cytochrome P450 CYP3A4 and CYP3A5 in healthy volunteers2018

    • Author(s)
      Makoto Nagai, Kazuhiro Inagaki
    • Journal Title

      Journal Medical Nursing Environment Science

      Volume: 2 Pages: 18-25

    • Related Report
      2017 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] Interaction of lime and hassaku orange components with rat and human P450 CYP3A.2018

    • Author(s)
      Makoto Nagai, Kazuhiro Inagaki
    • Journal Title

      Journal Medical Nursing Environment Science

      Volume: 2 Pages: 31-36

    • Related Report
      2017 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] Effect of the rind portion in Hassaku extracts on the pharmacokinetics of primidone2018

    • Author(s)
      Makoto Nagai, Kazuhiro Inagaki
    • Journal Title

      Journal Medical Nursing Environment Science

      Volume: 2 Pages: 26-30

    • Related Report
      2017 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] The Cytochrome P450(CYP)3A4, CYP3A5 Genotype and Phenotype Frequencies and that Novel Single Polymorphisms affected Phenotype from Japanese Individual2017

    • Author(s)
      Makoto Nagai, Kazuhiro Inagaki
    • Journal Title

      Journal Medical Nursing Environment Science

      Volume: 1 Pages: 11-17

    • Related Report
      2017 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] MD法によるInsulinと変異InsulinA鎖とのタンパク質相互作用に関する研究2017

    • Author(s)
      永井慎
    • Journal Title

      岐阜医療科学大学紀要

      Volume: 11 Pages: 21-23

    • Related Report
      2016 Research-status Report
  • [Journal Article] ゲノム編集技術2016

    • Author(s)
      永井慎
    • Journal Title

      バイオテクニシャン

      Volume: 2 Pages: 3-6

    • Related Report
      2016 Research-status Report
  • [Presentation] 放射性標識をした核酸医薬品の設計モデリングと機能性評価2018

    • Author(s)
      永井 慎,片渕哲朗
    • Organizer
      第138回 日本薬学会
    • Related Report
      2017 Annual Research Report

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Published: 2015-04-16   Modified: 2022-11-04  

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