| Literature DB >> 33687404 |
Jonathan D Bargh1, Stephen J Walsh, Nicola Ashman, Albert Isidro-Llobet, Jason S Carroll, David R Spring.
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.Entities:
Year: 2021 PMID： 33687404 DOI： 10.1039/d1cc00957e
Source DB: PubMed Journal: Chem Commun (Camb) ISSN： 1359-7345 Impact factor: 6.222