Aptamers are oligonucleotide molecules that are easily degraded by nuclease, which greatly hinders aptamer applications in medical research. Aptamers modified with 2' fluoro have been shown to resist nuclease degradation. Creative Biolabs is an excellent server provider who is skilled in offering the most professional aptamer modification services including 2' fluoro modification. We are committed to helping customers around the world discover functional and stable aptamers to advance their scientific research.
2' Fluoro Modifications
Aptamers are intolerant to nuclease due to their inherent oligonucleotide characteristics. The half-life of the unmodified aptamers is generally about 5min in the serum and less than 1h in the cell. A study showed that the half-life of the unmodified anti-thrombin DNA aptamer is as short as 108 s in vivo. A number of technologies have been established to protect aptamers from nuclease degradation. Among these, incorporation of 2' fluoro into aptamers is a common approach and has been widely used in clinical studies. Aptamers modified with 2' fluoro have been shown to considerably increase nuclease resistance. For example, Macugen, a targeted anti-VEGF aptamer, is modified by 2' fluoro, which has been approved to treat ocular vascular disease. The half-life of the drug is up to 18h in human plasma. Besides, aptamers modified with 2' fluoro have been also shown to improve their binding affinity for their ligands compared to the corresponding unmodified aptamers.
Fig.1 2' fluoro modification. (Yu, 2016)
Featured Services
Creative Biolabs has focused on aptamer development research for years and has accumulated rich experience. We offer a series of aptamer development services including library construction, aptamer selection, sequencing, synthesis, modification, and binding affinity test. Especially, our in-home scientists are very specialized in aptamer modifications and support a range of customized aptamer modification solutions according to different purposes of projects. To improve the resistance of aptamer to nuclease, we support a variety of oligonucleotide modification strategies such as 2' fluoro, 2' NH2, and 2' O-methyl. By leveraging a chemical modification technology, we support the introduction of 2' fluoro modification into aptamers during single-stranded oligonucleotide library preparation and at amplification steps in the selection process as well as during the process of aptamer synthesis.
Advantages
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Excellent experts providing a variety of flexible solutions for incorporating 2' fluoro into aptamers
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End-to-end services from consultation to stable aptamers delivery
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Ensured high quality, consistent reproducibility, and satisfying quantity
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Rapid turn-around time to accelerate your project success
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Best after-sales service
If you are interested in our services, please don’t hesitate to contact us for more details. We will be the most reliable partner for you in aptamer development.
Reference
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Yu, Y.; et al. Molecular selection, modification and development of therapeutic oligonucleotide aptamers. Int. J. Mol. Sci. 2016, 17:358.
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Questions & Answer
A: 2' Fluoro bases have a fluorine modified ribose which increases binding affinity (Tm) and also confers some relative nuclease resistance when compared to native RNA. 2'-fluoro is the most common 2'-substitution modification on the ribose unit. Typically, it is used to increase nuclease resistance and optimize aptamer affinity.
A: Some scientists have investigated 2' fluoro-modified aptamers that bind to vascular endothelial growth factor (VEGF) for the treatment of AMD. And others have developed 2' fluoro-modified RNA aptamers that can target prostate-specific membrane antigen (PSMA) for potential therapeutic use in human prostate cancer cells.
A: On the one hand, the generated 2' fluoro-modified aptamers can be highly stable in human serum, showing a moderate affinity. On the other hand, these 2' fluoro-modified aptamers can be easily conjugated to different nanocarriers, which in general show high specificity as well as improved targeting toxicity.
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