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Design and synthesis of novel amino acid PET tracer

Research Project

Project/Area Number 16K10304
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Radiation science
Research InstitutionNational Center of Neurology and Psychiatry

Principal Investigator

KATO KOICHI  国立研究開発法人国立精神・神経医療研究センター, 脳病態統合イメージングセンター, 室長 (50382198)

Research Collaborator TSUJI Atsushi  
KUMAMOTO Takuya  
Project Period (FY) 2016-04-01 – 2019-03-31
Project Status Completed (Fiscal Year 2018)
Budget Amount *help
¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2018: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2017: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2016: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Keywordsアミノ酸 / PET / トランスポーター / モノカルボン酸 / デュアルイメージング / 放射性医薬品 / PET
Outline of Final Research Achievements

In this study, 11C-labeled S-methyl-α-methylcysteine (LMMCY) and S-methyl-cysteine (LMCY) were synthesized and their PET studies were carried out using small lung cell SY-tumor bearing mice. Both tracers were accumulated highly in the tumor and the uptake ratios into pancreas and liver were significantly different. The uptake of LMMCY was high in the pancreas and that of LMCY was high both in the pancreas and liver. The mechanism of different uptake of these tracers remains to be studied.
The comparison study of uptake of 11C-AIB and its analog 11C-MeAIB into tumor was performed using eight lung cancer cells. Both tracers were transported into all cells mainly through system A. In addition 11C-AIB was transported partially via system L and ASC. Therefore higher uptake of 11C-AIB was observed in all cells than 11C-MeAIB and in three cells statistically significant difference.

Academic Significance and Societal Importance of the Research Achievements

アミノ酸はペプチドやタンパク質の構成要素であり、代謝を介してクエン酸回路の中間体、あるいは神経伝達物質を供給する。疾患によってペプチドやタンパク質の合成、ATP産出やシナプス化学伝達が亢進・抑制することから、アミノ酸の代謝や細胞への取り込みの変化をPETで捉えた画像は様々な疾患診断の指標になると考えられる。
本研究で検討を行った11C標識メチル-α-メチルシステインは既存のメチルシステインと比較して小細胞がんに細胞により高く集積し、膵臓/肝臓の取込み比が大きいことが明らかになった。取込み過程の違いが明らかになれば、それぞれの臓器を対象とした診断、治療への道が開けるのではないかと考えられる。

Report

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

    (4 results)

All 2018 2017

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

  • [Journal Article] Direct comparison of 2?amino[3?11C]isobutyric acid and 2?amino[11C]methyl?isobutyric acid uptake in eight lung cancer xenograft models2018

    • Author(s)
      Sudo Hitomi、Tsuji Atsushi、Sugyo Aya、Okada Maki、Kato Koichi、Zhang Ming?Rong、Saga Tsuneo、Higashi Tatsuya
    • Journal Title

      International Journal of Oncology

      Volume: 53 Pages: 2737-2744

    • DOI

      10.3892/ijo.2018.4596

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Synthesis and evaluation pf 11C-labeled coumarin analog as an imaging probe for detecting monocarboxylate transporters expression2017

    • Author(s)
      Tateishi, H.; Tsuji, A. B.; Kato, K.; Sudo, H.; Sugyo, A.; Hanakawa, T.; Zhang, M. R.; Saga, T.; Arano, Y.; Higashi. T.
    • Journal Title

      Bioorganic & Medicinal Chemistry Letters

      Volume: 27 Issue: 21 Pages: 4893-4897

    • DOI

      10.1016/j.bmcl.2017.09.033

    • Related Report
      2017 Research-status Report
    • Peer Reviewed / Open Access
  • [Presentation] Evaluation of 11C-labeled S-methyl8R)-a-methylcyctein as a novel PET tracer for tumor imaging2018

    • Author(s)
      Kato, K.; Tateishi, H.; Sudo, H.; Sugyo, A.; Tsuji, A. B.; Higashi, T.
    • Organizer
      12th Congress of the World Federation of Nuclear Medicine and Biology
    • Related Report
      2018 Annual Research Report
    • Int'l Joint Research
  • [Presentation] Development of a 11C-labeled coumarin analog for the dual mode imaging of monocarboxylate transporter2017

    • Author(s)
      Tateishi, H,; Tsuji, A, B,; Zhang, M. R.; Arano Y.; Kato, K.
    • Organizer
      International Symposium of Radiopharmaceutical Sciences
    • Related Report
      2017 Research-status Report
    • Int'l Joint Research

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

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