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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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Publication details

The article was received on 11 Jul 2013, accepted on 02 Aug 2013 and first published on 05 Aug 2013


Article type: Communication
DOI: 10.1039/C3CC45220D
Citation: Chem. Commun., 2013,49, 8187-8189
  • Open access: Creative Commons BY license
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    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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