The Site-specific Conjugation Strategy of HER2-targeted Antibody-drug Conjugates and its Application in Tumor Treatment

This paper focuses on the site-specific conjugation strategies of HER2-targeted antibody-drug conjugates (ADCs) and their applications in tumor therapy. First, it elaborates on the biological characteristics of HER2-positive tumors, the current treatment status, the rise of antibody-drug conjugates, and the necessity of site-specific conjugation strategies. Then, it introduces various site-specific conjugation strategies for HER2-targeted ADCs, such as engineered cysteines and non-natural amino acid insertion, conducts technical comparisons and optimizations, and lists representative drugs. Next, it explores the applications of site-specific conjugated ADCs in tumor therapy, including clinical efficacy, mechanisms to overcome drug resistance, and safety optimization. Finally, it analyzes the challenges in technology and clinical practice and presents prospects for future research directions. This study contributes to promoting the further development of HER2-targeted ADCs in tumor therapy.