| Project/Area Number |
16K21603
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Radiation science
Tumor therapeutics
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| Research Institution | National Institutes for Quantum and Radiological Science and Technology |
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Principal Investigator |
Ohshima Yasuhiro 国立研究開発法人量子科学技術研究開発機構, 高崎量子応用研究所 放射線生物応用研究部, 主任研究員(定常) (00588676)
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| Research Collaborator |
WATANABE Satoshi
SUZUKI Hiroyuki
SAKASHITA Tetsuya
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| Project Period (FY) |
2016-04-01 – 2018-03-31
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| Project Status |
Completed (Fiscal Year 2017)
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| Budget Amount *help |
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2017: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2016: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
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| Keywords | α線放出核種 / 211At / 2-AAMP / L型アミノ酸トランスポーター1（LAT1) / がん / L型アミノ酸トランスポーター1（LAT1） / 薬学 / 放射線 / 癌 |
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| Outline of Final Research Achievements |
In this study, we synthesized 2-[211At]astato-α-methyl-L-phenylalanine (2-AAMP) and evaluated its usefulness as a novel radiopharmaceutical targeting L-type amino acid transporter 1 (LAT1). 2-AAMP was successfully synthesized with high yield and purity by labelling the precursor with 211At in the presence of oxidant. 2-AAMP was taken up to tumor cells via LAT1, and induced DNA double strand break, growth inhibition and cell death. 2-AAMP was stable in vivo, and further accumulated and retained in tumor. On the other hand, 2-AAMP was rapidly cleared from normal organs in mice. These results suggest that 2-AAMP might be useful as a novel α-emitting radiopharmaceutical.
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