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Issue 74, 2013
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Acid-cleavable thiomaleamic acid linker for homogeneous antibody–drug conjugation

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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.

Graphical abstract: Acid-cleavable thiomaleamic acid linker for homogeneous antibody–drug conjugation

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Supplementary files

Article information


Submitted
11 Jul 2013
Accepted
02 Aug 2013
First published
05 Aug 2013

This article is Open Access

Chem. Commun., 2013,49, 8187-8189
Article type
Communication

Acid-cleavable thiomaleamic acid linker for homogeneous antibody–drug conjugation

L. Castañeda, A. Maruani, F. F. Schumacher, E. Miranda, V. Chudasama, K. A. Chester, J. R. Baker, M. E. B. Smith and S. Caddick, Chem. Commun., 2013, 49, 8187
DOI: 10.1039/C3CC45220D

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