Synthesis and evaluation of 2',4'-bridged nucleic acid with a phenoxazine base
Project/Area Number |
15K08024
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Research Category |
Grant-in-Aid for Scientific Research (C)
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Allocation Type | Multi-year Fund |
Section | 一般 |
Research Field |
Drug development chemistry
|
Research Institution | Osaka University |
Principal Investigator |
Nakagawa Osamu 大阪大学, 薬学研究科, 招へい教員 (90380691)
|
Project Period (FY) |
2015-04-01 – 2018-03-31
|
Project Status |
Completed (Fiscal Year 2017)
|
Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2017: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2016: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2015: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
|
Keywords | 核酸化学 / 核酸医薬 / 人工核酸 / 糖部架橋型核酸 |
Outline of Final Research Achievements |
We designed and synthesized a novel artificial 2’,4’-methylene bridged nucleic acid with a phenoxazine nucleobase (named BNAP). Oligonucleotide containing BNAP showed higher binding affinities toward complementary DNA and RNA. Thus, BNAP is a promising candidate for oligonucleotide therapeutics, especially for those requiring high duplex-forming ability. On the other hand, we developed a novel artificial nucleic acid containing a 9-azaphenoxazine nucleobase (9-TAP), which behaves as a cytosine (C) analog as well as a thymine (T) analog. Oligonucleotides containing 9-TAP could form stable duplexes via metal-mediated base pairs with C and T, via AgI and HgII, respectively. Duplexes bearing the mismatched base pair 9-TAP-C were effectively stabilized in the presence of CuII. Thus, 9-TAP is expected to have applications in DNA nanotechnology via the formation of various nanostructures triggered by different metal ions.
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Report
(4 results)
Research Products
(14 results)