Article
Discovery of novel antagonists on β2-adrenoceptor from natural products using a label-free cell phenotypic assay.
Naunyn-Schmiedeberg's archives of pharmacology - 1 Dec 2018
Zhang Pengyu, Wang Jixia, Zhao Ying, Zhang Xiuli, Qu Lala, Wang Chaoran, Feng Jiatao, Wang Anhui, Zhou Weijia, Liu Yanfang, Hou Tao, Zhou Han, Wang Zhiwei, Liang Xinmiao
Abstract excerpt
Label-free cell phenotypic assays were performed to establish a β2-adrenoceptor (β2-AR) target model in A431 cells and a β1-AR target model in transfected HEK293-β1 cells, using known β2-AR and β1-AR agonists and antagonists. A list of natural compounds was screened on the target models, among which seven new compounds were found to be antagonistically active against β2-AR. After receptor specificity evaluations...
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