A high-affinity subtype-selective fluorescent probe for estrogen receptor β imaging in living cells.
A high-affinity subtype-selective fluorescent probe for estrogen receptor β imaging in living cells.
Chem Commun (Camb). 2018 Apr 03;:
Authors: Hu Z, Yang L, Ning W, Tang C, Meng Q, Zheng J, Dong C, Zhou HB
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 via FPNM staining.
PMID: 29610818 [PubMed - as supplied by publisher]
Source: Chemical Communications - Category: Chemistry Authors: Hu Z, Yang L, Ning W, Tang C, Meng Q, Zheng J, Dong C, Zhou HB Tags: Chem Commun (Camb) Source Type: research
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