2016 Fiscal Year Final Research Report
Development of novel probes for in vivo imaging of b-secretase activity in the brain
| Project/Area Number |
15K19785
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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
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| Research Institution | Kyoto University |
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Principal Investigator |
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| Project Period (FY) |
2015-04-01 – 2017-03-31
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| Keywords | βセクレターゼ / アルツハイマー / イメージング / SPECT |
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| Outline of Final Research Achievements |
The deposition of amyloid β (Aβ) aggregates is the key neurodegenerative event of Alzheimer’s disease (AD). The cleavage of amyloid precursor protein (APP) by β-secretase is the first step of Aβ formation. Therefore, in vivo imaging of β-secretase activity would be useful for the diagnosis of AD. The aim of this study is to develop novel probes for in vivo imaging of β-secretase activity in the brain. We designed and synthesized [125I]PSCP based on the strategy of metabolic trapping. In vitro cleavage assay, [125I]PSCP was cleaved by β-secretase in a time dependent manner. In order to evaluate brain uptake of [125I]PSCP, in vivo biodistribution study using normal mice was performed. [125I]PSCP showed higher brain uptake compared with [125I]SCP, which has no cell penetrating peptide. These results suggest that [125I]PSCP has a potential as a probe for imaging β-secretase activity in the brain.
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| Free Research Field |
分子イメージンング
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