2015 Fiscal Year Final Research Report
Development of chemical drug delivery system using pepducin for boron carriers of BNCT
| Project/Area Number |
26670059
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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 |
Drug development chemistry
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| Research Institution | Gifu Pharmaceutical University |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
Masunaga Shin-ichiro 京都大学, 原子炉実験所, 教授 (80238914)
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| Project Period (FY) |
2014-04-01 – 2016-03-31
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| Keywords | ホウ素中性子捕捉療法 / ホウ素キャリア / 化学的分子送達システム / がん |
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| Outline of Final Research Achievements |
Selective delivery of sufficient quantity of 10B to tumor cells is essential for the success of boron neutron capture therapy (BNCT). Although sodium borocaptate (BSH) has been used clinically as a boron carrier for BNCT, it is impermeable to plasma membrane due to its anionic charges. Recently, we found that pepducins, which are artificial lipopeptides derived from an inner loop domain of G protein-coupled receptors (GPCRs), enabled anionic molecule such as fluorescein to penetrate membrane directly.
In this study, we designed and synthesized novel pepducin-boron cluster hybrid compounds as membrane permeable boron carriers for BNCT and evaluated their intracellular penetration ability. The pepducin comprising 13pep and palmitoyl tail showed the highest uptake quantity of boron atom into cells. We are further trying to modify the structure of boron carriers for tumor targeting delivery.
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| Free Research Field |
創薬化学
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