用于单载物抗体药物偶联物的二硫键重桥连试剂。
Disulfide re-bridging reagents for single-payload antibody-drug conjugates.
机构信息
Yusuf Hamied Department of Chemistry, University of Cambridge, Cambridge, CB2 1EW, UK.
Department of Organic Chemistry, Faculty of Science, Palacky University, Tr. 17. Listopadu 12, Olomouc, 77900, Czech Republic.
出版信息
Chem Commun (Camb). 2023 Aug 10;59(65):9868-9871. doi: 10.1039/d3cc02980h.
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.
存在许多抗体药物偶联物 (ADC) 连接子技术，可用于合成药物抗体比 (DAR) 为偶数整数（通常为 2、4 或 8）的 ADC。然而，奇数整数 DAR 的 ADC 更难合成。在这里，我们报告了使用 TetraDVP 接头合成负载单个弹头的 ADC 的方法，该接头可同时重新桥接 IgG1 抗体的所有四个链间二硫键。
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