| Project/Area Number |
15K15462
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Radiation science
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| Research Institution | Kobe Pharmaceutical University |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
Hagimori Masayori 長崎大学, 薬学部, 准教授 (40446125)
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| Project Period (FY) |
2015-04-01 – 2017-03-31
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| Project Status |
Completed (Fiscal Year 2016)
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| Budget Amount *help |
¥3,510,000 (Direct Cost: ¥2,700,000、Indirect Cost: ¥810,000)
Fiscal Year 2016: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2015: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
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| Keywords | 薬学 / 放射線 / 癌 / がん / 放射性薬剤 / ヘパラナーゼ |
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| Outline of Final Research Achievements |
Heparanase is an enzyme which plays an essential role for cancer metastasis. In this study, we designed and synthesized novel heparanase-targeted radioiodine-labeled probes, [I-125]1 and [I-125]2, based on a chemical structure of selective heparanase inhibitor, OGT2115, for quantitative diagnosis of cancer with single photon emission computed tomography. In a heparanase inhibition assay, non-radioactive 1 and 2 exhibited high heparanase inhibitory potencies similar to heparanase inhibitors previously reported. In addition, [I-125]1 showed a high stability in injection solution, cellular accumulation in cancer cells dependent on expression level of heparanase, and good in vivo biodistribution in normal mice. These results suggest that [I-123]1 targeting heparanase could be a candidate for qualitative diagnosis of cancers.
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