化学
荧光
流式细胞术
小分子
分子探针
C-Met公司
荧光各向异性
癌细胞
癌症研究
分子生物学
生物化学
生物物理学
作者
Dong Liang,Yadong Chen,Xiaojun Qin,Xingye Yang,Xuhui Dong,Mingzhao Hu,Lupei Du,Minyong Li
标识
DOI:10.1016/j.ejmech.2022.114114
摘要
C-mesenchymal-epithelia transition factor (c-Met) is highly expressed in various solid tumors such as gastric cancer, liver cancer, and lung cancer, playing a pivotal role in the growth, maintenance, and development of different tumor cells. In this study, three small-molecule fluorescent probes ( 5, 11, 16 ) targeting c-Met were developed, and their design strategies were also initially explored. In general, the fluorescence properties of the probes themselves could meet the imaging requirements, and they have shown sufficient inhibitory activities against c-Met, especially probe 16 , reflecting the targeting and acceptance. Also, fluorescence polarization assays and flow cytometry analysis verified the binding between the probes and c-Met. Cell imaging confirmed that these probes could be used to label c-Met on living cells. It is of positive significance for the development of c-Met kinase inhibitors and tumor pathology research. • Fluorescent probes ( 5, 11, 16 ) targeting c-Met were developed. • Design strategies of the probes were explored. • The probes showed strong inhibitory activities against c-Met, especially probe 16. • The binding between probes and c-Met was verified. • The probes could be used to label c-Met on living cells.
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