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Updated: Jan 7, 2026
Genetic Encoding of a Non-Canonical Amino Acid for the Generation of Antibody-Drug Conjugates Through a Fast Bioorthogonal Reaction
Published on: September 14, 2018
AbClick Pro H: Scavenger-Free, Traceless Lys248 Conjugation Via O-Acyl Hydroxamate Chemistry for Homogeneous
Jinyoung Son1,2, Jin Woo Seo1,3, Sun Hee Park1,3
1AbTis Co. Ltd., 21, Geumhwa-ro 105beon-gil, Giheung-gu, Yongin-si, Gyeonggi-do 17073, Republic of Korea.
Abstract:
A traceless O-acyl hydroxamate Fc-binding peptide linker enables rapid, scavenger-free, and site-selective conjugation at Lys248 of human IgG1. The resulting homogeneous DAR2 antibody-drug conjugates (ADCs) retain antigen binding and internalization with payload-dependent stability and cytotoxicity. The linker's intrinsic leaving-group mechanism ensures clean FcBP release and broad payload compatibility. This robust, scalable traceless Lys248 conjugation chemistry underpins investigational new drug (IND)-approved and nonclinical ADC pipelines, offering a predictable platform for next-generation ADC design.
