ERα-targeted fluorescent probes are important tools for ERα study. In order to develop high quality ERα-targeted probes, a sound and complete evaluation system is essential but has not been established yet. Herein, we set up a series of evaluation criteria for ERα-targeted fluorescent probes including ERα binding affinity, fluorescence quantum yield, cytotoxicity, ERα tracking capacity, ERα selectivity and ERα labeling ability. To verify the practicability of the evaluation criteria, we designed and synthesized two ERα-targeted fluorescent probes and fully characterized their properties based on the proposed evaluation criteria. It showed that the probes exhibited better performance. Moreover, we applied the probes in MCF-7 cells to study the ERα motion characteristics for the first time. We hope that our evaluation criteria could be helpful for the establishment of a complete evaluation system for ERα-targeted fluorescent probes.

中文翻译：

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建立用于开发高质量ERα靶向荧光探针的评估标准。

靶向ERα的荧光探针是研究ERα的重要工具。为了开发高质量的以ERα为靶标的探针，健全而完整的评估系统是必不可少的，但尚未建立。在这里，我们建立了针对ERα靶向荧光探针的一系列评估标准，包括ERα结合亲和力，荧光量子产率，细胞毒性，ERα跟踪能力，ERα选择性和ERα标记能力。为了验证评估标准的实用性，我们设计并合成了两种靶向ERα的荧光探针，并根据提出的评估标准充分表征了它们的特性。表明探针表现出更好的性能。此外，我们首次将探针应用于MCF-7细胞中以研究ERα的运动特征。