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Identification of two novel α1-AR agonists using a high-throughput screening model.

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.

SUBMITTER: Xu F

PROVIDER: S-EPMC6270864 | biostudies-literature | 2014 Aug

REPOSITORIES: biostudies-literature

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Identification of two novel α1-AR agonists using a high-throughput screening model.

Xu Fang F Chen Hong H He Xuelan X Xu Jingyi J Xu Bingbing B Huang Biyun B Liang Xue X Yuan Mu M

Molecules (Basel, Switzerland) 20140820 8

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-proliferat ...[more]

PMID: 25140448

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