In recent years, several antibody drug conjugates (ADC) have been accepted by the FDA as therapeutics against cancer. It is well-known that control of drug-to-antibody ratio (DAR) is vital for the success of an ADC, which inspires the advancement of better and simpler methods for tight control of DAR. We present the development of an antibody DNA wireframe cube conjugate for precise control of DAR. The DNA wireframe cube consists of four single strands, which when folded present eight single stranded domains. One domain is bound to a monofunctionalized antibody DNA conjugate, and the seven others are attached to DNA functionalized with the potent tubulin inhibitor MMAE, thereby preparing an ADC with a DAR of precisely seven. The formation of the ADC is investigated by gel electrophoresis and atomic force microscopy. Lastly, the developed MMAE loaded ADC was used for targeted drug delivery in vitro.

中文翻译：

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线框 DNA 立方体：用于靶向递送多拷贝单甲基 Auristatin E 的抗体偶联物

近年来，几种抗体药物偶联物 (ADC) 已被 FDA 接受为抗癌药物。众所周知，药物抗体比 (DAR) 的控制对于 ADC 的成功至关重要，这激发了更好、更简单的方法来严格控制 DAR。我们介绍了用于精确控制 DAR 的抗体 DNA 线框立方体偶联物的开发。DNA 线框立方体由四个单链组成，折叠时呈现八个单链结构域。一个结构域与单功能化抗体 DNA 偶联物结合，另外七个结构域连接到用强效微管蛋白抑制剂 MMAE 功能化的 DNA 上，从而制备出 DAR 恰好为 7 的 ADC。通过凝胶电泳和原子力显微镜研究 ADC 的形成。最后，