Estrogen receptor β (ERβ) has recently been identified as a pharmaceutical target in hormone replacement therapy for breast cancers. However, the biological function of ERβ in disease progression remains unclear. A highly ERβ-selective fluorescent probe (FPNM) was discovered exhibiting nanomolar affinity for ERβ with an ERβ/ERα selectivity as high as 80, which allowed specific labeling of intracellular ERβ. Moreover, distinct ERβ dynamics in various cellular bio-settings such as prostate cancer (DU-145) or triple-negative breast cancer (MDA-MB-231) cells were directly observed for the first time viaFPNM staining.

中文翻译：

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用于活细胞中雌激素受体β成像的高亲和力亚型选择性荧光探针†

雌激素受体β（ERβ）最近已被确定为乳腺癌荷尔蒙替代疗法的药物靶标。然而，ERβ在疾病进展中的生物学功能仍不清楚。发现具有高ERβ选择性的荧光探针（FPNM）对ERβ表现出纳摩尔摩尔亲和力，其ERβ/ERα选择性高达80，可以对细胞内ERβ进行特异性标记。此外，首次通过FPNM染色直接观察到各种细胞生物环境（例如前列腺癌（DU-145）或三阴性乳腺癌（MDA-MB-231））中不同的ERβ动态。