We report a chemoselective and site-selective approach that distinguishes one Lys from its multiple copies, N-terminus, and other competitors. The phospha-Mannich protocol works with multiple proteins and installs probes without structural and functional perturbations. It delivers an antibody–drug conjugate with selective anti-proliferative activity towards HER2 expressing SKBR3 breast cancer cells.

中文翻译：

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通过无金属多组分方法对蛋白质中的赖氨酸进行单点标记†

我们报告了一种化学选择性和位点选择性的方法，该方法可将一个Lys与它的多个副本，N末端和其他竞争者区分开。phospha-Mannich协议可与多种蛋白质一起使用，并且安装探针时不会受到结构和功能的干扰。它为表达HER2的SKBR3乳腺癌细胞提供了具有选择性抗增殖活性的抗体-药物结合物。