Journal
CHEMICAL COMMUNICATIONS
Volume 49, Issue 74, Pages 8187-8189Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3cc45220d
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Funding
- EPSRC
- BBSRC
- Wellcome Trust
- UCLB
- BBSRC [BB/J010448/1] Funding Source: UKRI
- Biotechnology and Biological Sciences Research Council [BB/J010448/1] Funding Source: researchfish
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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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