2011 Fiscal Year Final Research Report
Development of cationic histone deacetylase inhibitors as enhancer of gene transfection and expression
| Project/Area Number |
21590131
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Kansai University |
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Principal Investigator |
NAGAOKA Yasuo 関西大学, 化学生命工学部, 教授 (90243039)
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| Co-Investigator(Kenkyū-buntansha) |
HATTORI Yoshiyuki 星薬科大学, 薬学部, 准教授 (90350222)
UESATO Shinichi 関西大学, 化学生命工学部, 教授 (50111969)
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| Project Period (FY) |
2009 – 2011
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| Keywords | リポフェクション / ヒストン脱アセチル化酵素阻害剤 / 非ウイルスベクター / 遺伝子発現 / HDAC |
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| Research Abstract |
Lipofection is the most versatile transfection methods to transfect genes into mammalian cells, because of its safety and its handiness. However, the expression efficiency of the transfected genes with this method is much lower than that with viral vector. We therefore attempted to develop highly efficient enhancer for lipofection. According to this objective, we accomplished the development of lipofection enhancers which enhance the expression of genes up to 23 times more than that of control. Structure of the enhancer is based on histone deacetylase(HDAC) inhibitors, which increase acetylation level of histone in nucleus resulting in the enhancement of transcription efficiencies. HDAC inhibitors also inhibit a cytosolic isozyme of HDAC_s, HDAC6, to facilitate transportation of transfected genes to the nucleus. This may also contribute to the enhancement of the transfected gene expression.
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[Journal Article] Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl) benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain2012
Author(s)
Y. Hirata, M. Hirata, Y. Kawaratani, M. Shibano, M. Taniguchi, M. Yasuda, Y. Ohmomo, Y. Nagaoka, K. Baba, S. Uesato
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Journal Title
Bioorg. Med. Chem. Lett
Volume: 22(5)
Pages: 1926-1930
Peer Reviewed
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