Theranostics 2020; 10(3):1391-1414. doi:10.7150/thno.37936 This issue


Synthesis and applications of theranostic oligonucleotides carrying multiple fluorine atoms

Valeriy G. Metelev1,2, Alexei A. Bogdanov Jr.1,3,4✉

1. Laboratory of Molecular Imaging Probes, Department of Radiology, University of Massachusetts Medical School, Worcester MA, USA.
2. Department of Chemistry, Moscow State University, Moscow, Russian Federation.
3. Laboratory of Molecular Imaging, A.N. Bakh Institute of Biochemistry, Federal Research Center "Fundamentals of Biotechnology" of the Russian Academy of Sciences, Moscow.
4. Department of Bioengineering and Bioinformatics, Moscow State University, Moscow.

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Metelev VG, Bogdanov AA Jr.. Synthesis and applications of theranostic oligonucleotides carrying multiple fluorine atoms. Theranostics 2020; 10(3):1391-1414. doi:10.7150/thno.37936. Available from

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Graphic 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.

Keywords: oligonucleotide, perfluorinated, drug delivery, sensor, fluorescence, magnetic resonance spectroscopy