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一种用于实时可视化活细胞中γ-谷氨酰转肽酶活性的水溶性荧光探针。

A water-soluble fluorescent probe for real-time visualization of γ-glutamyl transpeptidase activity in living cells.

机构信息

Key Laboratory for Advanced Materials and Feringa Nobel Prize Scientist Joint Research Center, Institute of Fine Chemicals, School of Chemistry and Molecular Engineering, Frontiers Science Center for Materiobiology and Dynamic Chemistry, East China University of Science and Technology, Shanghai, 200237, PR China.

Key Laboratory for Advanced Materials and Feringa Nobel Prize Scientist Joint Research Center, Institute of Fine Chemicals, School of Chemistry and Molecular Engineering, Frontiers Science Center for Materiobiology and Dynamic Chemistry, East China University of Science and Technology, Shanghai, 200237, PR China.

出版信息

Bioorg Med Chem Lett. 2022 Jul 15;68:128762. doi: 10.1016/j.bmcl.2022.128762. Epub 2022 Apr 28.

Abstract

γ-glutamyl transpeptidase (GGT) is a kind of cell-surface enzyme that is overexpressed in many cancer cells. It is of great significance to develop an ideal tool for the diagnosis of GGT-rich cancer cells. Here, we reported a simple-structured but effective imaging probe for the detection of GGT activity. In the presence of GGT, the γ-glutamyl linkage could be cleaved specifically to produce amino-substituted product, resulting in significant fluorescence enhancement at 578 nm. Moreover, we successfully employed the probe to monitor GGT activity in HepG2 cells. We envisaged that such a simple but effective imaging tool could improve the practical applications for bioimaging.

摘要

γ-谷氨酰转肽酶(GGT)是一种在许多癌细胞中过度表达的细胞表面酶。开发一种用于诊断富含 GGT 的癌细胞的理想工具具有重要意义。在这里,我们报道了一种结构简单但有效的成像探针,用于检测 GGT 活性。在 GGT 的存在下,γ-谷氨酰键可以被特异性切割,产生氨基取代产物,导致在 578nm 处产生显著的荧光增强。此外,我们成功地利用该探针监测了 HepG2 细胞中的 GGT 活性。我们设想,这种简单但有效的成像工具可以提高生物成像的实际应用。

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