Disulfide re-bridging reagents for single-payload antibody-drug conjugates

Numerous antibody-drug conjugate (ADC) linker technologies exist for the synthesis of ADCs with drug-to-antibody ratios (DARs) being an even integer (typically 2, 4 or 8). However, ADCs with odd-integer DARs are significantly harder to synthesise. Here, we report the synthesis of ADCs loaded with a...

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Detalles Bibliográficos
Autores principales: King, Thomas A., Walsh, Stephen J., Kapun, Mia, Wharton, Thomas, Krajcovicova, Sona, Glossop, Melanie S., Spring, David R.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2023
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10414422/
https://www.ncbi.nlm.nih.gov/pubmed/37492000
http://dx.doi.org/10.1039/d3cc02980h
Descripción
Sumario:Numerous antibody-drug conjugate (ADC) linker technologies exist for the synthesis of ADCs with drug-to-antibody ratios (DARs) being an even integer (typically 2, 4 or 8). However, ADCs with odd-integer DARs are significantly harder to synthesise. Here, we report the synthesis of ADCs loaded with a single warhead, using TetraDVP linkers which simultaneously re-bridge all four interchain disulfides of an IgG1 antibody.

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