偶联化学应用于抗体-寡核苷酸偶联物的研究进展

Background: With the development of antibody genetic engineering technology and the popularization of oligonucleotide solid-phase synthesis, antibody-oligonucleotide conjugates (AOCs) have gradually attracted the attention of academia and pharmaceutical companies. Linker is one of the key components of AOC, which conjugates antibody to oligonucleotide through bioorthogonal chemical reactions. Research Status: Educated by ADC linker coupling chemistry, AOC linker coupling chemistry has also flourished recently, using natural amino acid or non-canonical amino acid anchors at the antibody. Linkage was made through amide bond, thioether bond, disulfide bond, triazole, etc. Meanwhile, several site-specific conjugation platforms, such as THIOMAB-siRNA, have been applied based on random conjugation. Research Applications: This paper aim to analyze advantages and disadvantages related to coupling chemistry in preparing AOC, expected to improve AOCs design.