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Open AccessReview

Bridged Nucleic Acids Reloaded

1
Instituto de Investigaciones Biotecnológicas Dr. Rodolfo A. Ugalde, Instituto Tecnológico de Chascomús, CONICET, Universidad Nacional de San Martín, San Martín 1650, Argentina
2
Fundación Instituto Leloir, IIBBA-CONICET, Buenos Aires C1405BWE, Argentina
3
Center for Applied Biotechnology Studies, Department of Biological Science, California State University Fullerton, Fullerton, CA 92834-6850, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Josef Jampilek
Molecules 2019, 24(12), 2297; https://doi.org/10.3390/molecules24122297
Received: 31 May 2019 / Revised: 17 June 2019 / Accepted: 18 June 2019 / Published: 21 June 2019
(This article belongs to the Special Issue Heterocycles in Medicinal Chemistry)
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PDF [721 KB, uploaded 21 June 2019]
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Abstract

Oligonucleotides are key compounds widely used for research, diagnostics, and therapeutics. The rapid increase in oligonucleotide-based applications, together with the progress in nucleic acids research, has led to the design of nucleotide analogs that, when part of these oligomers, enhance their efficiency, bioavailability, or stability. One of the most useful nucleotide analogs is the first-generation bridged nucleic acids (BNA), also known as locked nucleic acids (LNA), which were used in combination with ribonucleotides, deoxyribonucleotides, or other analogs to construct oligomers with diverse applications. However, there is still room to improve their efficiency, bioavailability, stability, and, importantly, toxicity. A second-generation BNA, BNANC (2′-O,4′-aminoethylene bridged nucleic acid), has been recently made available. Oligomers containing these analogs not only showed less toxicity when compared to LNA-containing compounds but, in some cases, also exhibited higher specificity. Although there are still few applications where BNANC-containing compounds have been researched, the promising results warrant more effort in incorporating these analogs for other applications. Furthermore, newer BNA compounds will be introduced in the near future, offering great hope to oligonucleotide-based fields of research and applications. View Full-Text
Keywords: oligonucleotides; bridged nucleic acids; locked nucleic acids; antisense; antibiotic resistance; hypercholesterolemia; myotonic dystrophy; CRISPR; Cas9; hematologic malignancies oligonucleotides; bridged nucleic acids; locked nucleic acids; antisense; antibiotic resistance; hypercholesterolemia; myotonic dystrophy; CRISPR; Cas9; hematologic malignancies
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Soler-Bistué, A.; Zorreguieta, A.; Tolmasky, M.E. Bridged Nucleic Acids Reloaded. Molecules 2019, 24, 2297.

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