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Stabilized peptide targeting programmed death-ligand 1 for Positron Emission Tomography imaging and cancer immunotherapy

Research Project

Project/Area Number 18H06217
Research Category

Grant-in-Aid for Research Activity Start-up

Allocation TypeSingle-year Grants
Review Section 0902:General internal medicine and related fields
Research InstitutionNational Institutes for Quantum and Radiological Science and Technology

Principal Investigator

胡 寛  国立研究開発法人量子科学技術研究開発機構, 放射線医学総合研究所 標識薬剤開発部, 博士研究員(任常) (00827678)

Project Period (FY) 2018-08-24 – 2020-03-31
Project Status Completed (Fiscal Year 2018)
Budget Amount *help
¥2,990,000 (Direct Cost: ¥2,300,000、Indirect Cost: ¥690,000)
Fiscal Year 2018: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Keywordsstabilized peptide / PD-L1 / PET imaging
Outline of Annual Research Achievements

I developed a native peptide-based PET tracer for imaging tumor PD-L1 for the first time. I labeled the peptide with 18F and 64Cu. Moreover, the peptide was pegylated to form PEG-peptide conjugates via an optimum ‘one-pot’ strategy. The as-made radiotracers were evaluated for stability and specificity in vitro and imaged in normal mice and in a tumor model. As consequence, the 64Cu labeled compounds showed preferable imaging potential in vivo. Furthermore, the pegylation was demonstrated to change the pharmacokinetics and biodistribution of the tracers. Our studies suggested that native peptide-based tracers are capable of PD-L1 imaging, further improvement of the performance via rational design and exactly under current investigation.These results were published in Chem Commun.

Research Progress Status

平成30年度が最終年度であるため、記入しない。

Strategy for Future Research Activity

平成30年度が最終年度であるため、記入しない。

Report

(1 results)
  • 2018 Annual Research Report
  • Research Products

    (5 results)

All 2019 2018

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

  • [Journal Article] Developing native peptide-based radiotracers for PD-L1 PET imaging and improving imaging contrast by pegylation2019

    • Author(s)
      Kuan Hu、Masayuki Hanyu、Xie Lin、Zhang Yiding、Kotaro Nagatsu、Hisashi Suzuki、Zhang Ming-Rong
    • Journal Title

      Chemical Communications

      Volume: 55 Issue: 29 Pages: 4162-4165

    • DOI

      10.1039/c9cc00445a

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Synthesis and Preliminary Evaluation of 11C‐Labeled VU0467485/AZ13713945 and Its Analogues for Imaging Muscarinic Acetylcholine Receptor Subtype2019

    • Author(s)
      Xiaoyun Deng Akiko Hatori Zhen Chen Katsushi Kumata Tuo Shao Xiaofei Zhang Tomoteru Yamasaki Kuan Hu Qingzhen Yu Longle Ma Gangqiang Wang Lu Wang Yihan Shao Lee Josephson Shaofa Sun Ming‐Rong Zhang Steven Liang
    • Journal Title

      ChemMedChem

      Volume: 14 Issue: 3 Pages: 303-309

    • DOI

      10.1002/cmdc.201800710

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a “Tail Switching” Strategy on a Piperazinyl Azetidine Skeleton2019

    • Author(s)
      Chen Zhen、Mori Wakana、Deng Xiaoyun、Cheng Ran、Ogasawara Daisuke、Zhang Genwei、Schafroth Michael A.、Dahl Kenneth、Fu Hualong、Hatori Akiko、Shao Tuo、Zhang Yiding、Yamasaki Tomoteru、Zhang Xiaofei、Rong Jian、Yu Qingzhen、Hu Kuan、Fujinaga Masayuki、Xie Lin、Kumata Katsushi、Gou Yuancheng、Chen Jingjin、Gu Shuyin
    • Journal Title

      Journal of Medicinal Chemistry

      Volume: 62 Issue: 7 Pages: 3336-3353

    • DOI

      10.1021/acs.jmedchem.8b01778

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Presentation] Develop a peptide-based PET radiotracer for imaging PD-L1 expression in cancer2018

    • Author(s)
      胡寛
    • Organizer
      The 10th China-Japan-Korea Symposium on Radiopharmaceutical Sciences(CJKSRS 2018)
    • Related Report
      2018 Annual Research Report
    • Int'l Joint Research
  • [Presentation] Radiolabeled Peptide for Anti-PD-L1 Imaging and Therapy2018

    • Author(s)
      Hu Kuan , 謝 琳 , 破入 正行 , 張 明栄
    • Organizer
      第2回日本核医学会分科会 放射性薬品科学研究会 第18回放射性医薬品・画像診断薬研究会
    • Related Report
      2018 Annual Research Report

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Published: 2018-08-27   Modified: 2019-12-27  

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