Chemical Modification

Oligonucleotides targeting mRNA have broad application prospects in the treatment of human diseases. However, naked or unmodified oligonucleotides not only are highly susceptible to degradation by nucleases and have low membrane permeability due to their high molecular weight and negative charges, but also can trigger different degrees of their off-target effects and/or immunogenicity^[1]. Based on a large number of experimental results and long-term experience, it was recognized that chemical modification such as backbone modification, furanose sugar modification, and nucleobase modification, or their innovative combinations can greatly improve the availability of oligonucleotide therapeutics.

Alfa Chemistry has a dedicated technology platform for chemical modification of therapeutic oligonucleotide, providing customers with chemical modification services and technical advice to support the development of oligonucleotide therapeutics and address unmet medical needs.

Backbone Modification

Backbone modification refers to the replacement of a non-bridging oxygen atom on the phosphodiester linkage with sulfur, carbon, nitrogen, boron, etc.

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Furanose Sugar Modification

2ʹ-O-methyl (2ʹ-O-Me), 2ʹ-O-methoxyethyl (2ʹ-MOE) and 2′-fluoro (2ʹ-F) are the most commonly used 2ʹ substituents of furanose sugar.

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Nucleobase Modification

Generally speaking, nucleobase modification includes adenine methylation and deamination, cytosine methylation, hydroxymethylation and carboxy substitution, guanine oxidation, etc.

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Our products and services are for research use only and cannot be used for any clinical purposes.

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