一种用于活细胞受体靶向荧光成像的BODIPY标记三价糖簇。
A BODIPY-tagged trivalent glycocluster for receptor-targeting fluorescence imaging of live cells.
作者信息
Guo Chen, Si Fang-Yu, Wang Chen-Han, Wang Ning, Hu Xi-Le, James Tony D, Li Jia, Wang Chengyun, He Xiao-Peng
机构信息
Key Laboratory for Advanced Materials and Joint International Research Laboratory of Precision Chemistry and Molecular Engineering, Feringa Nobel Prize Scientist Joint, Research Center, School of Chemistry and Molecular Engineering, East China University of Science and Technology 130 Meilong Rd Shanghai 200237 China
National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences Shanghai 201203 China
出版信息
Chem Sci. 2025 May 27. doi: 10.1039/d4sc08472a.
Multivalent glycoclusters have been extensively used as a targeting agent for drug delivery. However, tools capable of investigating their dynamic interactions with a target receptor remain elusive. Here, we synthesized fluorescently-tagged galactoclusters for the fluorescence imaging of cells that overly express the asialoglycoprotein receptor (ASGPr). A trivalent galactoside was synthesized, to which a boron dipyrromethene (BODIPY) dye was conjugated. The resulting fluorescent glycocluster was used for the targeted fluorescence imaging of liver cancer cells with a high ASGPr expression level. The trivalent probe was also demonstrated to be applicable for super-resolution imaging of ASGPr-mediated ligand endocytosis and the dynamic intracellular translocation to the lysosomes. As such, this study provides a suitable chemical tool for the study of receptor dynamics using fluorescently tagged glycoclusters.
多价糖簇已被广泛用作药物递送的靶向剂。然而，能够研究其与靶受体动态相互作用的工具仍然难以捉摸。在此，我们合成了荧光标记的半乳糖簇，用于对过度表达去唾液酸糖蛋白受体（ASGPr）的细胞进行荧光成像。合成了一种三价半乳糖苷，并将硼二吡咯亚甲基（BODIPY）染料与之共轭。所得的荧光糖簇用于对具有高ASGPr表达水平的肝癌细胞进行靶向荧光成像。还证明了三价探针适用于ASGPr介导的配体内吞作用的超分辨率成像以及向溶酶体的动态细胞内转运。因此，本研究提供了一种合适的化学工具，用于使用荧光标记的糖簇研究受体动力学。
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