Development of a Novel 18 F-Labeled Probe for PET Imaging of Estrogen Receptor β

Estrogen receptor beta (ERβ) is an important ER subtype that plays crucial roles in many physiological and pathological disorders. Herein, we developed the probe [ F]PVBO for ERβ targeted PET imaging and obtained promising results. The nonradioactive PVBO showed a 12.5-fold stronger binding affinity...

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Published in:Journal of medicinal chemistry 2023-01, Vol.66 (2), p.1210-1220
Main Authors: Zhou, Yujing, Lei, Peng, Han, Jiaxin, Wang, Zhiming, Ji, Aiyan, Wu, Yuyang, Zheng, Lingling, Zhang, Xiaoqing, Qu, Chunrong, Min, Jian, Zhu, Weiliang, Xu, Zhijian, Liu, Xingdang, Chen, Hao, Cheng, Zhen
Format: Article
Language:English
Subjects:
Animals
Cell Line, Tumor
Estradiol
Estrogen Receptor alpha - metabolism
Estrogen Receptor beta - metabolism
Humans
Positron-Emission Tomography - methods
Receptors, Estrogen - metabolism
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Summary:Estrogen receptor beta (ERβ) is an important ER subtype that plays crucial roles in many physiological and pathological disorders. Herein, we developed the probe [ F]PVBO for ERβ targeted PET imaging and obtained promising results. The nonradioactive PVBO showed a 12.5-fold stronger binding affinity to ERβ than to ERα . assays revealed the specific uptake of [ F]PVBO by DU145 cells. The uptake of [ F]PVBO by DU145 xenografts increased during the 120 min dynamic scanning, with a maximum uptake of 2.80 ± 0.30% ID/g. Based on time activity curves (TACs), the injection of [ F]PVBO with unlabeled PVBO or ERB-041 resulted in a significant signal reduction with the tumor/muscle (T/M) ratio
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.2c00761