1. A novel photostable near-infrared fluorescent selective estrogen receptor modulator (SERM) for live-cell 3D imaging of breast cancer.
- Author
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Yang, Chunmei, He, Pei, Meng, Qiuyu, Dong, Chune, Zhou, Hai-Bing, and Yang, Lu
- Subjects
- *
SELECTIVE estrogen receptor modulators , *THREE-dimensional imaging , *BREAST cancer , *BREAST imaging , *ESTROGEN receptors , *INFRARED imaging - Abstract
Estrogen receptor (ER) is a major transcriptional regulator that plays an important role in the treatment of breast cancer. Herein, we rationally designed and synthesized a novel small-molecule near-infrared (NIR) fluorescent probe, 2-(4-(2-(2,5-bis(2-fluoro-4-hydroxyphenyl)thiophen-3-yl)vinyl)− 3-cyano-5,5-dimethylfuran-2(5 H)ylidene)malononitrile (TCFT) , which could enable prolonged live-cell imaging by three-dimensional (3D) confocal microscopy. Moreover, this bifunctional probe also exhibited photostability, selective estrogen receptor modulator activity, and potent antiproliferative activity for targeted breast cancer therapy, which would be a prominent NIR fluorescent probe for breast cancer study. [Display omitted] • A novel photostable NIR fluorescent probe TCFT was developed for estrogen receptor. • TCFT was successfully applied in prolong live-cell imaging of estrogen receptor by 3D confocal microscopy. • TCFT exhibited selective estrogen receptor modulator activity and potent antiproliferative activity for breast cancer therapy. • TCFT possessed the potential as a theranostic probe for estrogen receptor (+) breast cancer study. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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