Applications of sugar modifications in oligo synthesis

The baseclick technology, based on the principles of click chemistry, represents a revolution in the field of nucleic acid synthesis. By enabling highly specific, sugar-targeted modifications, this technology opens new doors for therapeutic applications in areas such as gene editing, diagnostics and RNA-based treatments. In particular, the ability to strategically incorporate sugars into oligonucleotides improves the specificity, stability and cellular uptake of these molecules.

How does this technology work?

One of the most important applications of click chemistry is the post-synthetic modification of oligonucleotides, which enables the precise and efficient attachment of functional groups to oligonucleotides. For example, nucleoside triphosphates have been modified using click chemistry to introduce labels or functional probes into DNA or RNA strands. This technique has proved particularly useful in the development of oligonucleotide conjugates, e.g. those containing fluorescent dyes, for diagnostic applications to detect specific biomolecules or for bioimaging. (1)

The precision and versatility of baseclick technology plays a central role in the advancement of nucleic acid-based therapies, including antisense oligonucleotides (ASOs), small interfering RNAs (siRNAs) and mRNA therapies.

Applications of sugar modifications in oligosynthesis

Recent studies have demonstrated the utility of baseclick technology in the incorporation of mannose and other sugar moieties into oligonucleotides. These modifications enhance cell-specific targeting, especially in macrophages and other immune cells, offering promising applications for inflammatory diseases and conditions such as acute lung injury. The ability of this technology to target specific cells via sugar receptors, such as mannose receptors, is one of the secrets to developing more effective treatments and opens new avenues in personalized medicine and targeted drug delivery. (2)

1.?????? Tiwari, V.K., Jaiswal, M.K., Rajkhowa, S., Singh, S.K. (2024). Click Chemistry in Nucleic Acids. In: Click Chemistry. Materials Horizons: From Nature to Nanomaterials. Springer, Singapore. https://doi.org/10.1007/978-981-97-4596-8_14

2.????? Trimannose-coupled antimiR-21 for macrophage-targeted inhalation treatment of acute inflammatory lung damage, C. Beck et al., 2023, Nature Communications, Vol. 14, 4564. https://doi.org/10.1038/s41467-023-40185-1