Site-Specific Dual Antibody Conjugation via Engineered Cysteine and Selenocysteine Residues

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• 作者：Xiuling Li ; James T. Patterson ; Mohosin Sarkar ; Lee Pedzisa ; Thomas Kodadek ; William R. Roush ; Christoph Rader
• 刊名：Bioconjugate Chemistry
• 出版年：2015
• 出版时间：November 18, 2015
• 年：2015
• 卷：26
• 期：11
• 页码：2243-2248
• 全文大小：449K
• ISSN：1520-4812

文摘

Site-specific conjugation technologies enable the production of homogeneous antibody鈥揹rug conjugates (ADCs) with improved therapeutic indices compared to conventional ADCs. However, current site-specific conjugation methods can only attach one type of drug to a single antibody. Given the emergence of acquired resistance to current ADCs, arming single antibodies with different drugs may provide an attractive option in the development of next-generation ADCs. Here, we describe a site-specific dual conjugation strategy as a platform for dual warhead ADCs.