Development of 211At-labeled amino acid derivative targeting LAT1 as a novel alpha-emitting radiopharmaceutical
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 |
Research Field |
Radiation science
Tumor therapeutics
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Research Institution | National Institutes for Quantum and Radiological Science and Technology |
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 |
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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Report
(3 results)
Research Products
(1 results)
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[Journal Article] Efficacy of system l amino acid transporter 1 inhibition as a therapeutic target in esophageal squamous cell carcinoma.2016
Author(s)
Ohshima Y, Kaira K, Yamaguchi A, Oriuchi N, Tominaga H, Nagamori S, Kanai Y, Yokobori T, Miyazaki T, Asao T, Tsushima Y, Kuwano H, Ishioka NS.
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Journal Title
Cancer Sci.
Volume: 107
Issue: 10
Pages: 1499-1505
DOI
Related Report
Peer Reviewed / Open Access