The availability of tools to generate homogeneous and stable antibody conjugates without recombinant DNA technology is a valuable asset in fields spanning from in vitro diagnostics to in vivo imaging and therapeutics. We present here a general approach for the conjugation to human IgG1 antibodies, by employing a straightforward two-stage protocol based on antibody deglycosylation followed by tyrosinase-mediated ortho-quinone strain-promoted click chemistry. The technology is validated by the efficient and clean generation of highly potent DAR2 and DAR4 antibody–drug conjugates (ADCs) with cytotoxic payloads MMAE or PBD dimer, and their in vitro evaluation.

中文翻译：

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基于化学酶酪氨酸点击化学的抗体缀合物的非基因生成

在体外诊断、体内成像和治疗等领域，无需重组 DNA 技术即可生成均质且稳定的抗体缀合物的工具的可用性是一项宝贵的资产。我们在此提出了一种与人 IgG1 抗体缀合的通用方法，采用基于抗体去糖基化的简单两阶段方案，然后进行酪氨酸酶介导的邻醌菌株促进的点击化学。该技术通过高效、清洁地生成具有细胞毒性有效负载 MMAE 或 PBD 二聚体的高效 DAR2 和 DAR4 抗体药物偶联物 (ADC) 及其体外评估而得到验证。