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


ABSTRACT: Site-specific conjugation technologies enable the production of homogeneous antibody-drug 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.

SUBMITTER: Li X 

PROVIDER: S-EPMC4839195 | biostudies-literature | 2015 Nov

REPOSITORIES: biostudies-literature

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

Li Xiuling X   Patterson James T JT   Sarkar Mohosin M   Pedzisa Lee L   Kodadek Thomas T   Roush William R WR   Rader Christoph C  

Bioconjugate chemistry 20150724 11


Site-specific conjugation technologies enable the production of homogeneous antibody-drug 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  ...[more]

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