We herein describe the cell-specific release of alcohol-containing payloads a sulfatase-sensitive linker in antibody-drug conjugates (ADCs). The linker shows efficient sulfatase-mediated release and high stability in human and mouse plasma. evaluation demonstrates potent antigen dependent toxicity towards breast cancer cell lines.
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Targeted delivery of alcohol-containing payloads with antibody-drug conjugates.
Chem Commun (Camb)
June 2023
Department of Chemistry, Technical University of Denmark, Lyngby DK-2800, Denmark.
We herein describe the cell-specific release of alcohol-containing payloads a sulfatase-sensitive linker in antibody-drug conjugates (ADCs). The linker shows efficient sulfatase-mediated release and high stability in human and mouse plasma. evaluation demonstrates potent antigen dependent toxicity towards breast cancer cell lines.
View Article and Find Full Text PDFThe Methylene Alkoxy Carbamate Self-Immolative Unit: Utilization for the Targeted Delivery of Alcohol-Containing Payloads with Antibody-Drug Conjugates.
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Seattle Genetics, 21823 30th Dr SE, Bothell, WA, 98021, USA.
A strategy for the conjugation of alcohol-containing payloads to antibodies has been developed and involves the methylene alkoxy carbamate (MAC) self-immolative unit. A series of MAC β-glucuronide model constructs were prepared to evaluate stability and enzymatic release, and the results demonstrated high stability at physiological pH in a substitution-dependent manner. All the MAC model compounds efficiently released alcohol drug surrogates under the action of β-glucuronidase.
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