Kanagawa Institute of Industrial Science and Technology (KISTEC), Kanagawa 243-0435, Japan.
Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Tokyo 101-0062, Japan.
ACS Appl Bio Mater. 2021 Sep 20;4(9):6647-6651. doi: 10.1021/acsabm.1c00383. Epub 2021 May 7.
Eradication of cancer stem cells (CSCs) is an ultimate goal in cancer chemotherapy. Although a ligand-assisted targeting approach seems rational, the existence of subpopulations of CSCs and their discrimination from those present on healthy sites makes it a severe challenge. Some boronic acid (BA) derivatives are known for the ability to bind with glycan-terminal sialic acid (SA), in a manner dependent on the acidification found in hypoxic tumoral microenvironment. Taking advantage of this feature, here we show that the BA-ligand fluorescence conjugate can effectively target multiple CSC subpopulations in parallel, which otherwise must be independently aimed when using antibody--ligands.
根除癌症干细胞（CSC）是癌症化疗的终极目标。尽管配体辅助靶向方法似乎合理，但 CSC 的亚群的存在及其与健康部位存在的 CSC 的区分，使得这成为一个严峻的挑战。一些硼酸（BA）衍生物以能够与糖末端唾液酸（SA）结合的能力而闻名，其方式取决于缺氧肿瘤微环境中发现的酸化。利用这一特性，我们在这里表明，BA-配体荧光缀合物可以有效地同时靶向多个 CSC 亚群，而当使用抗体-配体时，这些亚群必须独立靶向。
