Synthesis of radiobromine-labeled antitumor peptides and application for theranostic probes
| Project/Area Number |
24591748
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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 | Gunma University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
YAMAGUCHI Aiko 群馬大学, 大学院医学系研究科, 寄付講座等教員 (80609032)
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| Co-Investigator(Renkei-kenkyūsha) |
WATANABE Shigeki 独立行政法人日本原子力研究開発機構, 量子ビーム応用研究部門, 研究員 (10450305)
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| Project Period (FY) |
2012-04-01 – 2015-03-31
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| Project Status |
Completed (Fiscal Year 2014)
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| Budget Amount *help |
¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
Fiscal Year 2014: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2013: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2012: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Keywords | 抗腫瘍活性ペプチド / 放射性臭素 / 標識合成 / 治療的診断 / 抗腫瘍ペプチド / PET / 環状ペプチド / トリプルネガティブ乳がん / 細胞毒性 / イメージング / 薬物動態 |
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| Outline of Final Research Achievements |
Triple negative breast cancer (TNBC) refers to any breast cancer that does not express the genes for hormone receptor and HER2/neu receptor. Unfortunately, TNBC cannot be treated with either hormone therapy and anti-HER2 antibody. Therefore, new targeted therapies are therefore an urgent unmet medical need for TNBC patients. We recently found that halogenated cyclic pentapeptides based on natural cyclic peptide sansalvamide A, namely SA-Br and SA-I, exhibit potent cytotoxicity to MDA-MB-231, one of the TNBC cell line. In this study, we tried to develop a theranostics probe based on radiobromine-labeled SA-Br and analogues. Initially, we developed a new method for preparing radiobromine-labeled peptides via silicon-halogen exchange reaction. Next, a series of cyclic peptides analogous to SA-I were synthesized via on-resin cyclization using oxime resin. Unfortunately, cytotoxicity of these peptides against MDA-MB-231 was much weaker than that of the parent peptide.
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Report
(4 results)
Research Products
(13 results)
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[Presentation] Synthesis and biological evaluation of N-methylated cyclic pentapeptides against malignant breast cancer cell lines,2014
Author(s)
K. Yamada, C. Takano, K. Matsumoto, H. Ueno, S. Watanabe, T. Moriguchi, H. Oku, S. Torii, K. Shinozuka
Organizer
1st International Symposium of Gunma University Medical Innovation & 6th International Conference on Advanced Micro-Devise Engineering
Place of Presentation
Kiryu City Hall (Kiryu, Gunma)
Year and Date
2014-12-05
Related Report
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