Development of radioiolabeled uracil derivatives as radionuclide therapeutic agents for thymidine phosphorylase expressing tumors
| Project/Area Number |
23591826
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Radiation science
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| Research Institution | Health Sciences University of Hokkaido |
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Principal Investigator |
OHKURA Kazue 北海道医療大学, 薬学部, 教授 (60094827)
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| Co-Investigator(Kenkyū-buntansha) |
KUGE Yuji 北海道大学, アイソトープ総合センター, 教授 (70321958)
AKIZAWA Hiromichi 昭和薬科大学, 薬学部, 教授 (90311795)
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| Co-Investigator(Renkei-kenkyūsha) |
TAMAKI Nagara 北海道大学, 大学院・医学研究科, 教授 (30171888)
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| Project Period (FY) |
2011 – 2013
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| Project Status |
Completed (Fiscal Year 2013)
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| Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2013: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2012: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2011: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
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| Keywords | 放射線 / 核医学 / がん治療 / 内用放射線治療 / チミジンホスホリラーゼ |
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| Research Abstract |
Radionuclide therapy is a propitious method for treating and prolonging the lives of patients with cancer. The expression of thymidine phosphorylase (TP) is closely associated with angiogenesis and tumor invasiveness. To develop radiopharmaceuticals for in vivo TP-targeting radiotherapy, several radioiodinated TP inhibitors were synthesized. Although the radioiodinated 5-iodo-6-(oxoimidazolidinyl)methyluracil derivative showed successful results following in vitro evaluations, the results of in vivo evaluations were inadequate for radionuclide therapy. To solve the problem of high radioactivity in the liver due to indicative physiological TP expression, a prodrug was designed to undergo conversion into a strong TP inhibitor by an enzyme overexpressed in the tumor. Although substantial investigations are required, the approach obtained from this study will pave the way for the development of in vivo TP-targeted radiotherapy.
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Report
(4 results)
Research Products
(13 results)
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[Presentation] Preparation and evaluation of IIMU for SPECT imaging thymidine phosphorylase expression in tumors2013
Author(s)
Nishijima K, Zhao S, Zhao Y, Feng F, Shimizu Y, Abo N, Akizawa H, Ohkura K, Tamaki N, Kuge Y
Organizer
20^<th> International Synposium on Radiopharmaceutical Sciences
Place of Presentation
Jeju, Korea
Related Report
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[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
Jeju, Korea
Related Report
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