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Synthesis and applications of theranostic oligonucleotides carrying multiple fluorine atoms
Valeriy G Metelev1,2, Alexei A Bogdanov1,3,4
1Laboratory of Molecular Imaging Probes, Department of Radiology, University of Massachusetts Medical School, Worcester MA, USA.
Abstract:
The use of various oligonucleotide (ON) syntheses and post-synthetic strategies for targeted chemical modification enables improving their efficacy as potent modulators of gene expression levels in eukaryotic cells. However, the search still continues for new approaches designed for increasing internalization, lysosomal escape, and tissue specific delivery of ON. In this review we emphasized all aspects related to the synthesis and properties of ON derivatives carrying multifluorinated (MF) groups. These MF groups have unique physico-chemical properties because of their simultaneous hydrophobicity and lipophobicity. Such unusual combination of properties results in the overall modification of ON mode of interaction with the cells and making multi-fluorination highly relevant to the goal of improving potency of ON as components of new therapies. The accumulated evidence so far is pointing to high potential of ON probes, RNAi components and ON imaging beacons carrying single or multiple MF groups for improving the stability, specificity of interaction with biological targets and delivery of ONs in vitro and potentially in vivo.
Insights
Multifluorinated (MF) groups enhance oligonucleotide (ON) properties for gene therapy. These modifications improve cellular uptake, stability, and delivery, showing potential for novel ON-based therapies.
Area of Science:
- Oligonucleotide chemistry
- Medicinal chemistry
- Molecular biology
Background:
- Oligonucleotides (ONs) are crucial for modulating gene expression but face challenges in cellular delivery and stability.
- Current strategies aim to improve ON efficacy through chemical modifications and advanced delivery systems.
- Developing novel ON derivatives is essential for enhancing their therapeutic potential.
Purpose of the Study:
- To review the synthesis and properties of oligonucleotide derivatives incorporating multifluorinated (MF) groups.
- To explore the impact of MF groups on ON physicochemical characteristics and cellular interactions.
- To assess the potential of MF-modified ONs for improving therapeutic applications.
Main Methods:
- Review of literature on oligonucleotide synthesis and chemical modification strategies.
- Analysis of the properties of multifluorinated groups, including hydrophobicity and lipophobicity.
- Evaluation of evidence regarding the performance of MF-modified ONs in vitro and in vivo.
Main Results:
- Multifluorinated (MF) groups impart unique hydrophobicity and lipophobicity to oligonucleotides (ONs).
- These properties modify the interaction of ONs with cells, enhancing cellular uptake and lysosomal escape.
- MF-modified ONs demonstrate improved stability, target specificity, and delivery efficiency.
Conclusions:
- Multifluorinated ONs show significant promise for improving the potency and delivery of ON-based therapeutics.
- MF groups offer a valuable strategy for overcoming key challenges in oligonucleotide drug development.
- Further research into MF-modified ONs could lead to advanced therapies for various diseases.
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