Ontology highlight
ABSTRACT:
SUBMITTER: Patterson JT
PROVIDER: S-EPMC4140540 | biostudies-other | 2014 Aug
REPOSITORIES: biostudies-other
Patterson James T JT Asano Shigehiro S Li Xiuling X Rader Christoph C Barbas Carlos F CF
Bioconjugate chemistry 20140806 8
Current routes for synthesizing antibody-drug conjugates commonly rely on maleimide linkers to react with cysteine thiols. However, thioether exchange with metabolites and serum proteins can compromise conjugate stability and diminish in vivo efficacy. We report the application of a phenyloxadiazole sulfone linker for the preparation of trastuzumab conjugates. This sulfone linker site-specifically labeled engineered cysteine residues in THIOMABs and improved antibody conjugate stability in human ...[more]