Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 17, Issue 19, Pages 4835-4842Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c9ob00668k
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Funding
- Ministry of Education, Culture, Sports, Science and Technology, Japan [17H04886]
- Health Sciences Research Grants for Research on Psychiatric and Neurological Diseases and Mental Health from the Ministry of Health, Labour and Welfare of Japan
- Grants-in-Aid for Scientific Research [17H04886] Funding Source: KAKEN
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For the improvement of nuclease resistance, four kinds of new modifications through a carbamoylethyl linker were designed. Among them, the 2'-O-[2-N-{2-(benzimidazol-1-yl) ethyl} carbamoylethyl] modification showed 20-fold longer half-life when treated with a 3' to 5' exonuclease compared to the 2'-O-methoxyethyl (MOE) modification, which is used in approved drugs. In addition, this large modification did not disturb the binding affinity or RNase H-dependent antisense activity. From these findings, it could be concluded that an adequate linker, such as carbamoylethyl in this study, could extend the utility of 2'-O-modification without loss of the properties of nucleic acids. This strategy would be useful for the development of nucleic acid therapeutics.
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