Disulfide re-bridging reagents for single-payload antibody-drug conjugates.
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ABSTRACT:
SUBMITTER: King TA
PROVIDER: S-EPMC10414422 | biostudies-literature | 2023 Aug
REPOSITORIES: biostudies-literature
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Disulfide re-bridging reagents for single-payload antibody-drug conjugates.
King Thomas A TA Walsh Stephen J SJ Kapun Mia M Wharton Thomas T Krajcovicova Sona S Glossop Melanie S MS Spring David R DR
Chemical communications (Cambridge, England) 20230810 65
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. ...[more]
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