Disulfide re-bridging reagents for single-payload antibody-drug conjugates
Language English Country England, Great Britain Media electronic
Document type Journal Article
PubMed
37492000
PubMed Central
PMC10414422
DOI
10.1039/d3cc02980h
Knihovny.cz E-resources
- MeSH
- Disulfides MeSH
- Immunoconjugates * MeSH
- Indicators and Reagents MeSH
- Antineoplastic Agents * MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Disulfides MeSH
- Immunoconjugates * MeSH
- Indicators and Reagents MeSH
- Antineoplastic Agents * MeSH
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.
Apollo Therapeutics Ltd 50 60 Station Road Cambridge CB1 2JH UK
Yusuf Hamied Department of Chemistry University of Cambridge Cambridge CB2 1EW UK
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