Department of Chemistry, Indian Institute of Science Education and Research Bhopal, Bhauri, Bhopal, MP 462 066, India.
Chem Commun (Camb). 2018 Jun 28;54(53):7302-7305. doi: 10.1039/c8cc03311k.
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.
我们报道了一种化学选择性和位点选择性的方法，可以区分一个赖氨酸与其多个拷贝、N 端和其他竞争物。膦酰-Mannich 方案适用于多种蛋白质，并在不引起结构和功能干扰的情况下安装探针。它提供了一种抗体药物偶联物，对表达 HER2 的 SKBR3 乳腺癌细胞具有选择性的抗增殖活性。
