Advances in Site-specific Conjugation Technologies Applied to the Synthesis of Antibody-Drug Conjugates
10.13748/j.cnki.issn1007-7693.20232887
- VernacularTitle:抗体偶联药物合成过程中定点偶联技术的前沿进展
- Author:
Yujia CHEN
1
;
Ziyi YOU
2
;
Chanyuan XIONG
1
;
Li LIN
1
;
Liqiang PAN
1
,
3
Author Information
1. College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China
2. College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, ChinaCollege of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China
3. The First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310058, China
- Publication Type:Journal Article
- Keywords:
antibody-drug conjugates;
site-specific conjugation;
biological activity;
targeted therapy
- From:
Chinese Journal of Modern Applied Pharmacy
2024;41(2):261-276
- CountryChina
- Language:Chinese
-
Abstract:
Antibody-drug conjugates(ADCs), as an emerging therapy for cancer treatment, have made significant progress in the past few decades. However, due to the heterogeneity of ADCs, they still face various issues and challenges in clinical therapy. Therefore, site-specific conjugation techniques have become a crucial area of research in ADCs, and in recent years, this field has witnessed numerous breakthrough advancements, empowering ADCs with enhanced performance. The review provides a comprehensive overview of the frontiers in site-specific conjugation technologies for ADCs. Categorized into seven major classes including lysine-based, cysteine-based, low-abundance amino acid-based and glycosylation site-based conjugation techniques, ribosomal incorporation of unnatural and noncanonical amino acids and enzyme-mediated conjugation techniques, it meticulously describes 21 classical and emerging techniques such as the THIOMAB technology and linchpin-directed modification, in order to offer valuable insights for the development of next-generation ADCs.