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. 2021 Apr 11;57(28):3457-3460.
doi: 10.1039/d1cc00957e. Epub 2021 Mar 9.

A dual-enzyme cleavable linker for antibody-drug conjugates

Jonathan D Bargh  1 , Stephen J Walsh, Nicola Ashman, Albert Isidro-Llobet, Jason S Carroll, David R Spring
Affiliations

A dual-enzyme cleavable linker for antibody-drug conjugates

Jonathan D Bargh et al. Chem Commun (Camb). .

Abstract

A novel enzyme cleavable linker for antibody-drug conjugates is reported. The 3-O-sulfo-β-galactose linker is cleaved sequentially by two lysosomal enzymes - arylsulfatase A and β-galactosidase - to release the payload in targeted cells. An α-HER2 antibody-drug conjugate synthesised using this highly hydrophilic dual-cleavable linker exhibited excellent cytotoxicity and selectivity.

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