2018 Fiscal Year Final Research Report
Development of Aib-containing delivery tool of siRNA into cancer cells with ability of spatio-temporal control of siRNA actions
| Project/Area Number |
16K08331
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Osaka University of Pharmaceutical Sciences |
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Principal Investigator |
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| Project Period (FY) |
2016-04-01 – 2019-03-31
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| Keywords | 核酸医薬 / siRNA / 膜透過性ペプチド / 両親媒性ヘリックスペプチド / α-aminoisobutyric acid / Aib / RGD配列 |
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| Outline of Final Research Achievements |
Recently, drugs based on RNA molecules, such as small interfering RNA (siRNA) and microRNA (miR), have been actively developed for the treatment of intractable diseases. siRNA regulates gene expression by inhibiting specific messenger RNA (mRNA) translation. The α-aminoisobutyric acid (Aib)-containing peptidic delivery tools of these RNA molecules into cells, which have the abilities of cancer cell specificity and control of the duration of the actions, have been developed. Although the creation of the delivery tool enabling the control of the duration of the action have been tried unsuccessfully, we have shown an Aib-containing delivery tool the abilities of cancer cell specificity. Furthermore, in consequence of structure-activity relationship studies, we can show the suitable structure for delivery of RNA into cells.
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| Free Research Field |
薬学
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| Academic Significance and Societal Importance of the Research Achievements |
難治性疾患に対して種々の医薬品が開発されてきている．その中の１つである核酸医薬は，臨床の場に提供されている医薬品は少ない．その薬剤の本体である核酸分子は生体内で不安定で分解されやすく，細胞膜透過性が悪いという欠点がある．この薬剤の欠点を補うためにペプチド性デバイスの創製を行い，核酸医薬とペプチド性デバイスの複合体ががん細胞に入りやすいこと及びこのペプチド性デバイスの必要な化学構造を示すことができた．
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