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Development of peptide-based PET probe targeting integrin alpha5beta1

Research Project

Project/Area Number 24591827
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Radiation science
Research InstitutionNational Institute of Radiological Sciences

Principal Investigator

JIN Zhao-Hui  独立行政法人放射線医学総合研究所, 分子イメージング研究センター, 主任研究員 (70324150)

Co-Investigator(Kenkyū-buntansha) ZHANG Ming-Rong  独立行政法人放射線医学総合研究所, 分子イメージング研究センター, プログラムリーダー (80443076)
Co-Investigator(Renkei-kenkyūsha) FURUKAWA Takako  独立行政法人放射線医学総合研究所, 分子イメージング研究センター, チームリーダー (00221557)
Project Period (FY) 2012-04-01 – 2015-03-31
Project Status Completed (Fiscal Year 2014)
Budget Amount *help
¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2014: ¥520,000 (Direct Cost: ¥400,000、Indirect Cost: ¥120,000)
Fiscal Year 2013: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2012: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywordsalpha5beta1 integrin / Fluorine-18 / PET imaging / Fibronectin / Radioprobe / 18F
Outline of Final Research Achievements

This study was aimed to develop a novel PET imaging probe targeting the transmembrane glycoprotein receptor, α5β1integrin, by use of the fibronectin-mimetic peptide sequence KSSPHSRNSGSGSGSGSGRGDSP (called PR_b). PR_b was modified and conjugated with the chelating agent p-SCN-Bn-NOTA, and radiolabeled with 18F based on the chelation of 18F-aluminum fluoride. 18F-PR_b was produced with a radiochemical purity of >95%; it exhibited α5β1-binding activity and specificity in cultured cells and in tumor-bearing mice, and had a rapid blood clearance and a predominant renal excretion pathway. In vivo α5β1-positive tumors could be clearly visualized by 18F-PR_b PET imaging. 18F-PR_b was developed as a promising PET imaging agent targeting the α5β1 integrin.

Report

(4 results)
  • 2014 Annual Research Report   Final Research Report ( PDF )
  • 2013 Research-status Report
  • 2012 Research-status Report
  • Research Products

    (17 results)

All 2015 2014 2013 2012 Other

All Journal Article (7 results) (of which Peer Reviewed: 7 results,  Open Access: 2 results,  Acknowledgement Compliant: 1 results) Presentation (8 results) Book (1 results) Remarks (1 results)

  • [Journal Article] Comparison of intratumoral FDG and Cu-ATSM distributions in cancer tissue originated spheroid (CTOS xenografts, a tumor model retaining the original tumor properties.2014

    • Author(s)
      Furukawa T, Yuan Q, Jin ZH, Aung W, Yoshii Y, Hasegawa S, Endo H, Inoue M, Zhang MR, Fujibayashi Y, Saga T.
    • Journal Title

      Nuclear Medicine and Biology

      Volume: 41 Issue: 8 Pages: 653-659

    • DOI

      10.1016/j.nucmedbio.2014.05.139

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Journal Article] Molecular imaging of ectopic metabotropic glutamate 1 receptor in melanoma with a positron emission tomography radioprobe 18 F-FITM.2014

    • Author(s)
      Xie L, Yui J, Fujinaga M, Hatori A, Yamasaki T, Kumata K, Wakizaka H, Furutsuka K, Takei M, Jin ZH, Furukawa T, Kawamura K, Zhang MR.
    • Journal Title

      International Journal of Cancer

      Volume: in press Issue: 8 Pages: 1852-1859

    • DOI

      10.1002/ijc.28842

    • Related Report
      2014 Annual Research Report 2013 Research-status Report
    • Peer Reviewed / Open Access
  • [Journal Article] PET imaging and biodistribution analysis of the effects of succinylated gelatin combined with l-lysine on renal uptake and retention of 64Cu-cyclam-RAFT-c(-RGDfK-)4 in vivo.2014

    • Author(s)
      Jin ZH, Furukawa T, Sogawa C, Claron M, Aung W, Tsuji AB, Wakizaka H, Zhang MR, Boturyn D, Dumy P, Fujibayashi Y, Saga T.
    • Journal Title

      European Journal of Pharmaceutics and Biopharmaceutics

      Volume: 86(3) Issue: 3 Pages: 478-486

    • DOI

      10.1016/j.ejpb.2013.11.006

    • Related Report
      2014 Annual Research Report 2013 Research-status Report
    • Peer Reviewed
  • [Journal Article] Micro-positron emission tomography/contrast-enhanced computed tomography imaging of orthotopic pancreatic tumor-bearing mice using the αvβ3 integrin tracer 64Cu-labeled cyclam-RAFT-c(-RGDfK-)42013

    • Author(s)
      Aung W, Jin ZH, Furukawa T, Claron M, Boturyn D, Sogawa C, Tsuji AB, Wakizaka H, Fukumura T, Fujibayashi Y, Dumy P, Saga T.
    • Journal Title

      Molecular Imaging

      Volume: 12(6) Pages: 376-387

    • Related Report
      2013 Research-status Report
    • Peer Reviewed
  • [Journal Article] C-Type Natriuretic Peptide Specifically Acts on the Pylorus and Large Intestine in Mouse Gastrointestinal Tract2013

    • Author(s)
      Sogawa C, Wakizaka H, Aung W, Jin ZH, Tsuji AB, Furukawa T, Kunieda T, Saga T.
    • Journal Title

      Am J Pathol.

      Volume: 182 Issue: 1 Pages: 172-179

    • DOI

      10.1016/j.ajpath.2012.09.015

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Positron emission tomography imaging of tumor angiogenesis and monitoring of antiangiogenic efficacy using the novel tetrameric peptide probe 64Cu-cyclam-RAFT-c(-RGDfK-)4.2012

    • Author(s)
      Jin ZH, Furukawa T, Claron M, Boturyn D, Coll JL, Fukumura T, Fujibayashi Y, Dumy P, Saga T.
    • Journal Title

      Angiogenesis

      Volume: 15 Issue: 4 Pages: 569-580

    • DOI

      10.1007/s10456-012-9281-1

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Basic studies on radioimmunotargeting of CD133-positive HCT116 cancer stem cells.2012

    • Author(s)
      Jin ZH, Sogawa C, Furukawa T, Saito Y, Aung W, Fujibayashi Y, Saga T.
    • Journal Title

      Molecular Imaging

      Volume: 11 Pages: 445-450

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Presentation] Comparison of tumor uptake of the radiotracers targeting cancer metabolism2015

    • Author(s)
      Takako Furukawa, Qinghua Yuan , Zhao-Hui Jin, Winn Aung, Tsuneo Saga
    • Organizer
      2015 World Molecular Imaging Congress
    • Place of Presentation
      Honolulu, Hawaii
    • Year and Date
      2015-09-02 – 2015-09-05
    • Related Report
      2014 Annual Research Report
  • [Presentation] Labeling and stability studies for a tetrameric cyclic RGD peptide based radiopharmaceutical 64/67Cu-cyclam-RAFT-c(-RGDfK-)42015

    • Author(s)
      Zhao-Hui Jin, Takako Furukawa, Mélissa Degardin, Didier Boturyn, Ming-Rong Zhang, Yasuhisa Fujibayashi, Pascal Dumy, Tsuneo Saga
    • Organizer
      2015 World Molecular Imaging Congress
    • Place of Presentation
      Honolulu, Hawaii
    • Year and Date
      2015-09-02 – 2015-09-05
    • Related Report
      2014 Annual Research Report
  • [Presentation] Development of 18F-labeled fibronectin-mimetic peptide for positron emission tomography imaging of a5b1 integrin expression2014

    • Author(s)
      Zhao-Hui Jin, Takako Furukawa, Katsushi Kumata, Lin Xie, Joji Yui, Hidekatsu Wakizaka, Yasuhisa Fujibayashi, Ming-Rong Zhang, Tsuneo
    • Organizer
      2014 World Molecular Imaging Congress
    • Place of Presentation
      Seoul, Korea
    • Year and Date
      2014-09-17 – 2014-09-20
    • Related Report
      2014 Annual Research Report
  • [Presentation] Zr-89 immuno-PET imaging targeting HER3 expression in mouse models2014

    • Author(s)
      Qinghua Yuan1, Takako Furukawa, Zhao-Hui Jin, Winn Aung, Yukie Yoshii, Aya Sugyo, Kotaro Nagatsu, Hiroko Endo, Masahiro Inoue, Takashi Masuko, Yasuhisa Fujibayashi. Tsuneo Saga
    • Organizer
      2014 World Molecular Imaging Congress
    • Place of Presentation
      Seoul, Korea
    • Year and Date
      2014-09-17 – 2014-09-20
    • Related Report
      2014 Annual Research Report
  • [Presentation] HER3を標的とするZr-89 標識抗体イメージングの基礎検討Zr-89 immuno-PET imaging targeting HER3 in mice2014

    • Author(s)
      元清華、古川高子、金朝暉、Winn Aung、吉井幸恵、辻厚至、永津弘太郎、遠藤洋子、井上正宏、益子高、佐賀恒夫、藤林靖久
    • Organizer
      第9回日本分子イメージング学会総会・学術集会
    • Place of Presentation
      大阪府豊中市
    • Year and Date
      2014-05-22 – 2014-05-23
    • Related Report
      2014 Annual Research Report
  • [Presentation] HER3 を標的とするZr-89 標識抗体イメージングの基礎検討2014

    • Author(s)
      元清華、古川高子、金朝暉、Winn Aung、吉井幸恵、須堯綾、永津弘太郎、 遠藤洋子、井上正宏、益子高、佐賀恒夫、藤林靖久
    • Organizer
      第9回日本分子イメージング学会総会・学術集会
    • Place of Presentation
      大阪府豊中市・千里ライフサイエンスセンター
    • Related Report
      2013 Research-status Report
  • [Presentation] PET imaging and quantification of the effects of succinylated gelatin and/or L-lysine on renal uptake and retention of the novel radiopharmaceutical 64Cu-cyclam-RAFT-c(-RGDfK-)42013

    • Author(s)
      Zhao-Hui Jin, Takako Furukawa, Chizuru Sogawa, Atsushi Tsuji, Winn Aung, Michael Claron, Jean-Luc Coll, Didier Boturyn, Pascal Dumy, Tsuneo Saga
    • Organizer
      Annual Meeting of Society of Nuclear Medicine and Molecular Imaging (2013 SNMMI)
    • Place of Presentation
      Vancouver Convention Center, Vancouver, Canada
    • Related Report
      2013 Research-status Report
  • [Presentation] 新規分子プローブ64Cu-cyclam-RAFT-c(-RGDfK-)4を用いた腫瘍血管新生のPETイメージングおよび血管新生抑制剤の治療効果のモニタリング2012

    • Author(s)
      Zhao-Hui Jin, Takako Furukawa, Michael Claron, Didier Boturyn, Jean-Luc Coll, Toshimitsu Fukumura, Yasuhisa Fujibayashi, Pascal Dumy, and Tsuneo Saga
    • Organizer
      第7回日本分子イメージング学会総会・学術集会
    • Place of Presentation
      浜松市アクトシティ浜松
    • Related Report
      2012 Research-status Report
  • [Book] Nuclear Oncology2014

    • Author(s)
      Zhao-Hui Jin, Takako Furukawa, Tsuneo Saga
    • Total Pages
      711
    • Publisher
      Lippincott Williams and Wilkins
    • Related Report
      2014 Annual Research Report
  • [Remarks] 腫瘍血管新生のPETイメージング

    • URL

      http://www.nirs.go.jp/information/event/2012/12_11.shtml

    • Related Report
      2013 Research-status Report

URL: 

Published: 2013-05-31   Modified: 2019-07-29  

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