Research Progress on the Chemical Methods for Site-specific Coupling of Antibodies and Drugs

One of the main challenges of modern medicine is the development of efficient and safe tumor treatment methods. Antibody drug conjugates(ADC) have clinically become one of the most powerful tools for tumor treatment. Most of coupling strategy of traditional ADC drugs is using the lysine residues as the coupling sites. However, using this strategy may be highly heterogeneous, which may lead to poor drug reproducibility and low therapeutic index. Therefore, how to avoid these potential problems is the key-point of ADC drug research. In recent years, significant advances in the field of site-specific protein chemical modification methods have also partly promoted the synthesis of homogeneous ADC drugs. Therefore, this review focuses on the site-specific chemical coupling methods currently used to construct ADC, in order to provide a reference for the development of antibody-conjugated drug-conjugation chemistry.