Acid-cleavable thiomaleamic acid linker for homogeneous antibody–drug conjugation
Chemical Communications2013Vol. 49(74), pp. 8187–8187
Citations Over TimeTop 10% of 2013 papers
Lourdes Castañeda, Antoine Maruani, Felix Schumacher, Enrique Miranda, Vijay Chudasama, Kerry Chester, James R. Baker, Mark E. B. Smith, Stephen Caddick
Abstract
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.
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