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

TA. King, SJ. Walsh, M. Kapun, T. Wharton, S. Krajcovicova, MS. Glossop, DR. Spring

. 2023 ; 59 (65) : 9868-9871. [pub] 20230810

Jazyk angličtina Země Anglie, Velká Británie

Typ dokumentu časopisecké články

Perzistentní odkaz   https://www.medvik.cz/link/bmc23016591

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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