PD-ECGF-targeted tumor imaging with new F-18 radiolabeled uracil derivatives

• Project/Area Number: 23591811
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Radiation science
• Research Institution: Hokkaido University
• Principal Investigator: Nishijima Ken-ichi 北海道大学, 医学(系)研究科(研究院), 特任講師 (60364254)
• Co-Investigator(Kenkyū-buntansha): 大倉 一枝 北海道医療大学, 薬学部, 教授 (60094827)
• Project Period (FY): 2011 – 2013
• Project Status: Completed (Fiscal Year 2013)
• Budget Amount: ¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000); Fiscal Year 2013: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000); Fiscal Year 2012: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000); Fiscal Year 2011: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
• Keywords: 放射性薬剤 / 癌 / チミジンホスホリラーゼ / Thymidine Phosphorylase / 血小板由来血管内皮細胞増殖因子 / 腫瘍イメージング / F-18標識合成

Outline of Final Research Achievements

The angiogenic factor PD-ECGF/ thymidine phosphorylase (TP) is expressed at high levels in a variety of solid tumors compared with normal tissue. In this study, we aimed at the development of F-18 radiopharmaceuticals for imaging of angiogenesis.
5-fluoro analog of IIMU and BOMU, a potent inhibitor of TP studied the synthesis was performed. We have succeeded in creating new compounds for TP. However F-labeled TP inhibitor was not given. The results of this study gave an important knowledge on to creating the F-18 labeled compounds.

Research Products

• [Journal Article] 特集１ 核医学検査の新しい展開 治療戦略に役立つ放射性薬剤の開発 (2011)
  • Author(s): 久下裕司、西嶋剣一、趙 松吉
  • Journal Title: 映像情報メディカル Volume: 43（11） Pages: 842-849
• [Journal Article] Radiolabeled uracil derivative as a novel SPECT probe for thymidine phosphorylase : suppressed accumulation into tumor cells by target gene knockdown (2011)
  • Author(s): Li H, Zhao S, Jin Y, Nishijima K, Akizawa H, Ohkura K, Tamaki N, Kuge Y
  • Journal Title: Nucl Med Commun Volume: 32 Issue: 12 Pages: 1211-1215
  • DOI: 10.1097/mnm.0b013e32834b7ea7
  • NAID: 120004979488
  • Peer Reviewed
• [Presentation] Preparation and evaluation of [123I]IIMU for SPECT imaging of thymidine phosphorylase expression in tumors. (2013)
  • Author(s): Nishijima K, Zhao S, Zhao Y, Feng F, Shimizu Y, Abo N, Akizawa H, Ohkura K, Tamaki N, and Kuge Y
  • Organizer: 20th International Symposium on Radiopharmaceutical Sciences
  • Place of Presentation: ICC Jeju (Korea)
• [Presentation] チミジンホスホリラーゼイメージング剤の開発～北海道臨床開発機構とのコラボレーション～ (2012)
  • Author(s): 西嶋剣一、永井榮一
  • Organizer: 第52回日本核医学会学術総会
  • Place of Presentation: ロイトン札幌（札幌市）
  • Invited
• [Presentation] チミジンホスホリラーゼイメージング剤[123I]5-iodo-6-[(2-iminoimidazolidinyl)methyl]uracilの開発：タンパク結合測定と画像化の検討 (2012)
  • Author(s): 西嶋剣一、越田早織、趙松吉、秋澤宏行、大倉一枝、松本博樹、志賀 哲、玉木長良、久下裕司
  • Organizer: 日本薬学会 第132年会
  • Place of Presentation: 北海道大学（札幌）
• [Presentation] チミジンホスホリラーゼイメージング剤[123I]5-iodo-6-[(2-iminoimidazolidinyl)methyl]uracilの開発：血漿タンパク結合とI-123標識合成検討 (2011)
  • Author(s): 西嶋剣一、越田早織、趙松吉、秋澤宏行、大倉一枝、松本博樹、久下裕司
  • Organizer: 第11回放射性医薬品・画像診断薬研究会
  • Place of Presentation: 京都テルサ（京都）