Development of radiogallium-labeled agents for PET imaging without cyclotron

• Project/Area Number: 21390347
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Single-year Grants
• Section: 一般
• Research Field: Radiation science
• Research Institution: Kobe Pharmaceutical University (2011); Kyushu University (2009-2010)
• Principal Investigator: MUKAI Takahiro 神戸薬科大学, 薬学部, 教授 (30284706)
• Co-Investigator(Kenkyū-buntansha): MAGATA Yasuhiro 浜松医科大学, 光量子医学研究センター, 教授 (20209399)
• Project Period (FY): 2009 – 2011
• Project Status: Completed (Fiscal Year 2011)
• Budget Amount: ¥17,160,000 (Direct Cost: ¥13,200,000、Indirect Cost: ¥3,960,000); Fiscal Year 2011: ¥3,380,000 (Direct Cost: ¥2,600,000、Indirect Cost: ¥780,000); Fiscal Year 2010: ¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000); Fiscal Year 2009: ¥8,580,000 (Direct Cost: ¥6,600,000、Indirect Cost: ¥1,980,000)
• Keywords: 放射性医薬品 / 造影剤 / 放射線 / 癌 / 薬学

Research Abstract

In this study, we designed DOTA-MN2 and DOTA-TZ2, employing metronidazole moiety as a recognition site of hypoxic tumors and Ac-TZ14011 peptide as a CXCR4 ligand, respectively. Radiogallium-DOTA-MN2 exhibited the high stability and significant accumulation in the hypoxic tumors. Ga-DOTA-TZ2 showed the high affinity to CXCR4 in vitro. These results provide useful information about the chemical design of radiogallium-labeled radiopharmaceuticals for PET studies.

Research Products

• [Journal Article] Design of Ga-DOTA-based bifunctional radiopharmaceuticals : Two functional moieties can be conjugated to radiogallium-DOTA without reducing the complex stability (2009)
  • Author(s): Takahiro Mukai, Jun Suwada, Kohei Sano, Mayumi Okada, Fumihiko Yamamoto, and Minoru Maeda
  • Journal Title: Bioorganic & Medicinal Chemistry Volume: Vol.17, No.13 Issue: 13 Pages: 4285-4289
  • DOI: 10.1016/j.bmc.2009.05.041
  • Peer Reviewed
• [Journal Article] Design of Ga-DOTA-based bifunctional radiopharmaceuticals : Two functional moieties can be conjugated to radiogallium-DOTA without reducing the complex stability (2009)
  • Author(s): T.Mukai, et al
  • Journal Title: Bioorganic & Medicinal Chemistry 17 Pages: 4285-4289
  • Peer Reviewed
• [Presentation] A radiogallium-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for imaging tumors (2011)
  • Author(s): Kohei Sano, Ryo Masuda, Shinya Oishi, Hayato Hisada, Kenta Shimokawa, Nobutaka Fujii, Hideo Saji, Takahiro Mukai
  • Organizer: The Society of Nuclear Medicine 58th Annual Meeting
  • Place of Presentation: San Antonio
  • Year and Date: 2011-06-06
• [Presentation] Evaluation of a radiogallium-labeled bifunctional chelate, Ga-DOTA-MN2, for hypoxic tumor imaging (2010)
  • Author(s): Takahiro Mukai, Kohei Sano, Mayumi Okada, Minoru Maeda
  • Organizer: The 23rd Annual Congress of the European Association of Nuclear Medicine
  • Place of Presentation: Vienna
  • Year and Date: 2010-10-10
• [Presentation] Evaluation of a radiogallium-labeled bifunctional chelate, Ga-DOTA-MN2, for hypoxic tumor imaging (2010)
  • Author(s): Takahiro Mukai, et al.
  • Organizer: The 23rd Annual Congress of the European Association of Nuclear Medicine
  • Place of Presentation: Vienna, Austria
  • Year and Date: 2010-10-10
• [Presentation] 放射性ガリウム標識二官能性キレート、Ga-DOTA-MN2のがん低酸素領域イメージング剤としての評価 (2010)
  • Author(s): 佐野紘平、岡田真由美、前田稔、向高弘
  • Organizer: 第5回日本分子イメージング学会学術集会
  • Place of Presentation: 大津
  • Year and Date: 2010-05-23
• [Presentation] 放射性ガリウム標識二官能性キレート、Ga-DOTA-MN2のがん低酸素領域イメージング剤としての評価 (2010)
  • Author(s): 佐野紘平, 岡田真由美, 前田稔, 向高弘
  • Organizer: 第5回日本分子イメージング学会学術集会
  • Place of Presentation: 滋賀県立県民交流センター(大津市)
  • Year and Date: 2010-05-23
• [Presentation] がん低酸素領域の核医学イメージングを目的とした放射性ガリウム標識二官能性キレートの開発 (2009)
  • Author(s): 岡田真由美、諏訪田純、向高弘、佐野紘平、前田稔
  • Organizer: 第9回放射性医薬品・画像診断薬研究会
  • Place of Presentation: 京都
  • Year and Date: 2009-11-14
• [Presentation] がん低酸素領域の核医学イメージングを目的とした放射性ガリウム標識二官能性レートの開発 (2009)
  • Author(s): 岡田真由美、諏訪田純、向高弘, ら
  • Organizer: 第9回放射性医薬品・画像診断薬研究会
  • Place of Presentation: 京都大学(京都市)
  • Year and Date: 2009-11-14
• [Presentation] A radio-gallium-labeled bifunctional chelate for hypoxic tumor imaging (2009)
  • Author(s): Takahiro Mukai, Jun Suwada, Fumihiko Yamamoto, and Minoru Maeda
  • Organizer: 18th International Symposium on Radiopharmaceutical Sciences
  • Place of Presentation: Edmonton
  • Year and Date: 2009-07-14
• [Presentation] A radiogallium-labeled bifunctional chelate for hypoxic tumor imaging (2009)
  • Author(s): T.Mukai, et al
  • Organizer: 18th International Symposium on Radiopharmaceutical Sciences
  • Place of Presentation: Edmonton, Canada
  • Year and Date: 2009-07-14