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Issue 31, 2018
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A high-affinity subtype-selective fluorescent probe for estrogen receptor β imaging in living cells

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Abstract

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.

Graphical abstract: A high-affinity subtype-selective fluorescent probe for estrogen receptor β imaging in living cells

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Supplementary files

Article information


Submitted
20 Jan 2018
Accepted
22 Mar 2018
First published
23 Mar 2018

Chem. Commun., 2018,54, 3887-3890
Article type
Communication

A high-affinity subtype-selective fluorescent probe for estrogen receptor β imaging in living cells

Z. Hu, L. Yang, W. Ning, C. Tang, Q. Meng, J. Zheng, C. Dong and H. Zhou, Chem. Commun., 2018, 54, 3887
DOI: 10.1039/C8CC00483H

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