2016 Fiscal Year Final Research Report
Development of a radioiodine-labeled heparanase-targeted probe
| Project/Area Number |
15K15462
|
|---|
| Research Category |
Grant-in-Aid for Challenging Exploratory Research
|
| Allocation Type | Multi-year Fund |
|---|
| Research Field |
Radiation science
|
|---|
| Research Institution | Kobe Pharmaceutical University |
|---|
Principal Investigator |
|
|---|
| Co-Investigator(Renkei-kenkyūsha) |
Hagimori Masayori 長崎大学, 薬学部, 准教授 (40446125)
|
|---|
| Project Period (FY) |
2015-04-01 – 2017-03-31
|
| Keywords | 薬学 / 放射線 / 癌 |
|---|
| 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.
|
| Free Research Field |
放射線科学
|
