Identification of Two Novel α1-AR Agonists Using a High-Throughput Screening ModelReport as inadecuate




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Pharmaceutical Research Center, Guangzhou Medical University, 195# Dongfengxi Road, Guangzhou 510182, China



These authors contributed equally to this work.





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Abstract α1-Adrenoceptors ARs; 1A, 1B, and 1D have been determined to perform different prominent functions in the physiological responses of the sympathetic nervous system. A high-throughput screening assay HTS was set up to detect α1-AR subtype-selective agonists by a dual-luciferase reporter assay in HEK293 cells. Using the HTS assay, two novel compounds, CHE3 and CHK3, were discovered as α1-ARs agonists in α1-ARs expressed in HEK293 cells. These compounds also showed moderate-weak anti-proliferative activities against tested cancer cell lines. The HTS assay proposed in this study represents a potential method for discovering more α1-AR subtype-selective ligands. View Full-Text

Keywords: agonist; α1-ARs; HTS model; anti-proliferative activities; subtype-selectivity agonist; α1-ARs; HTS model; anti-proliferative activities; subtype-selectivity





Author: Fang Xu †, Hong Chen †, Xuelan He, Jingyi Xu, Bingbing Xu, Biyun Huang, Xue Liang and Mu Yuan *

Source: http://mdpi.com/



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