Acid-cleavable thiomaleamic acid linker for homogeneous antibody–drug conjugation† †Electronic supplementary information (ESI) available: 1H and 13C spectra for all novel compounds, and ES-MS spectra for all reactions with proteins described herein. See DOI: 10.1039/c3cc45220dClick here for additional data file.
نویسندگان
چکیده
In this communication we describe a novel acid-cleavable linker strategy for antibody-drug conjugation. Functional disulfide bridging of the single interchain disulfide bond of a trastuzumab Fab fragment yields a homogeneous antibody-drug conjugate bearing a thiomaleamic acid linker. This linker is stable at physiological pH and temperature, but quantitatively cleaves at lysosomal pH to release the drug payload.
منابع مشابه
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