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What are common conjugation chemistries for antibody-ASO conjugates?

There are several chemistries allowing conjugating antibodies to ASOs:

Click chemistry utilizes azide-alkyne cycloaddition reactions to synthesize Ab-ASO conjugates with high specificity and bioorthogonality. These conjugation methods enable site-specific conjugation.

Disulfide linker chemistries utilize cleavable linker molecules in reducing environments, enabling the controlled release of ASO in the intracellular space.

Hydrazone or oxime ligation utilizes aldehyde-modified oligonucleotides with hydrazine-functionalized antibodies.

Thiol-maleimide chemistries introduce thiol groups on either the ASO or antibody. Thiols react with a maleimide-modified partner molecule. Thiol-maleimide-based conjugation methods are efficient and widely used.

 

Please review: Bioconjugate Chemistry for Molecular Engineering