In this work, we developed a novel “click”-ready pH-cleavable phosphoramidate linker for controlled-release of monomethyl auristantin E (MMAE) in antibody- and small molecule-drug conjugates application. This water-soluble linker was found to have tremendous stability at physiological pHs while rapidly releasing its payload at acidic pH. The linker can also be tailored to release payloads of diverse functional groups, broadening its applications.

中文翻译：

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一种点击就绪的 pH 触发的基于氨基磷酸酯的连接体，用于单甲基 auristatin E 的控制释放

在这项工作中，我们开发了一种新型“点击”就绪 pH 可裂解的氨基磷酸酯接头，用于在抗体和小分子药物缀合物应用中控制单甲基阿里斯坦汀 E (MMAE) 的释放。人们发现这种水溶性连接体在生理 pH 值下具有极大的稳定性，同时在酸性 pH 值下快速释放其有效负载。连接器还可以定制以释放不同功能组的有效负载，从而扩大其应用范围。