2015 Fiscal Year Final Research Report
Design and synthesis of chiral peptide nucleic acid for antigene therapeutics
| Project/Area Number |
24590135
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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 | Teikyo University (2015)
The University of Tokyo (2012-2014) |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
KITTAKA ATSUSHI 帝京大学, 薬学部, 教授 (00214833)
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| Project Period (FY) |
2012-04-01 – 2016-03-31
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| Keywords | 核酸 / ゲノム / 遺伝子 / 癌 / 有機化学 |
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| Outline of Final Research Achievements |
The synthesis of new β-Lys PNA monomers and their incorporation into a 10-residue PNA sequence have been achieved. PNA containing β-Lys PNA units formed a stable hybrid duplex with DNA. However, incorporation of β-Lys PNA units caused destabilization of PNA-DNA duplexes to some extent. Electrostatic attractions between β-PNA and DNA could reduce this destabilization effect. Subsequently, bipyridine-conjugated β-Lys PNA was prepared and exhibited sequence selective cleavage of DNA. Based on the structures of the cleavage products and molecular modeling, we reasoned that bipyridine moiety locates within the minor groove of the PNA-DNA duplexes. The lysine side chain of β-PNA is a versatile handle for attaching various functional molecules.
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| Free Research Field |
医歯薬学
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