Castañeda, L; Maruani, A; Schumacher, FF; Miranda, E; Chudasama, V; Chester, KA; Baker, JR; ... Caddick, S; + view all Castañeda, L; Maruani, A; Schumacher, FF; Miranda, E; Chudasama, V; Chester, KA; Baker, JR; Smith, ME; Caddick, S; - view fewer (2013) Acid-cleavable thiomaleamic acid linker for homogeneous antibody-drug conjugation. Chemical Communications , 49 pp. 8187-8189. 10.1039/c3cc45220d.

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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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