Furanose Sugar Modification

The chemical modification of the furanose sugar moiety has been extensively studied to enhance binding affinity, reduce susceptibility toward nuclease cleavage, and modulate activity^[1]. It can be said that the small structural changes of the furanose sugar moiety have a profound effect on the properties of oligonucleotides. Alfa Chemistry has a dedicated chemical modification technology platform to provide furanose sugar modification services and technical advice. You can trust our capabilities and contact us.

Common Furanose Sugar Modification

2'-O-methyl (2'-O-Me), 2'-O-methoxyethyl (2'-MOE) and 2'-fluoro (2'-F) are the most commonly used 2' substituents of furanose sugar. These modifications increase the nuclease resistance of oligonucleotides by replacing the nucleophilic 2'-hydroxyl group of unmodified oligonucleotides, leading to improved stability in plasma, increased tissue half-lives and, consequently, prolonged oligonucleotide therapeutic effects[2]. In addition, these modifications also enhance the binding affinity of oligonucleotides to complementary RNA by promoting the 3'-endo pucker conformation (RNA-like) of ribose.

2'-O-Me modification

2'-O-Me is a naturally occurring modification that helps improve the properties of oligonucleotides. This modification can reduce off-target effects and is widely used to improve the nuclease stability of small interfering RNA (siRNA) drugs. In addition, 2'-O-Me modification can abrogate the immune responses that are induced by siRNA and ASO drugs.

2'-MOE modification

2'-MOE modification is widely used in oligonucleotides to improve their resistance to nucleases. Several ASO drugs using 2'-MOE have entered clinical development in the past decade and one ASO drug, Kynamro, was recently approved by The United States Food and Drug Administration for the treatment of familial hypercholesterolemia.

2'-F modification

2'-F modification refers to the substitution of the 2'-OH group on the furanose sugar ring by a fluorine atom, which is roughly the same size as a hydrogen atom, but is highly electronegative. 2'-F modification increases the binding affinity of oligonucleotides to target mRNA sequences. At present, this modification has been extensively investigated in the context of oligonucleotide therapeutics and appears to have a privileged role in enhancing the drug-like properties of siRNA.

What We Offer?

As the world's leading explorer of oligonucleotide therapeutics, Alfa Chemistry provides our customers with furanose sugar modification services for therapeutic oligonucleotides. You can also contact us to customize any furanose sugar-modified oligonucleotide you need.

Why Choose Us?

• Experienced experts
• Extensive chemical modification technologies
• Advanced analytical equipment
• Professional technical advice
• Competitive price
• Fast delivery

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

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