Identification of Two Novel α1-AR Agonists Using a High-Throughput Screening Model

Molecules

Fang Xu¹  Hong Chen¹  Xuelan He²  Jingyi Xu²  Bingbing Xu²  Biyun Huang²  Xue Liang² 

[1] id="af1-molecules-19-12699">Research Center, Guangzhou Medical University, 195# Dongfengxi Road, Guangzhou 510182, Chi

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

DOI  :  10.3390/molecules190812699

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.