Phenotypic assessment and ligand screening of ETA/ETB receptors with label-free dynamic mass redistribution assay

	Phenotypic assessment and ligand screening of ETA/ETB receptors with label-free dynamic mass redistribution assay
	Qu, Lala; Zhang, Xiuli; Wang, Jixia; Zhou, Han; Hou, Tao; Wei, Lai; Xu, Fangfang; Liang, Xinmiao
刊名	NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
	2019
卷号	393 期号:6
关键词	Dynamic mass redistribution assay Endothelin receptor type A Endothelin receptor type B High-throughput screening Ligand binding
英文摘要	Endothelin receptors, consisting of two subtypes, ETA and ETB, are expressed in various tissues and widely regulate cardiovascular systems. The two receptors show distinct biological characteristics and are involved in different downstream pathways. Hence, to evaluate the ETA and ETB receptors on the same platform is helpful to display their pharmacological features. In this study, we developed a label-free dynamic mass redistribution (DMR) assay to investigate the phenotypic features of the ETA and ETB receptors in native cell lines. Meanwhile, specific agonists and antagonists were investigated for their pharmacological parameters. Results indicated that the DMR response of endothelin 1 (ET-1, an endogenous ETA/ETB agonist) was cell line dependent on ETA receptors and this ligand generated a biphasic dose-response curve in SH-SY5Y as well as PC3 cell lines. ET-1 and IRL 1620 (an ETB agonist) showed different DMR responses in U251 cells. IC50 values of antagonists were consistent with the K-i values previously reported. Furthermore, a list of compounds was screened on the ETA and ETB receptor models established by the high-throughput DMR assays. This study demonstrated that the DMR assay had great potential in the phenotypic-based investigation and ligand screening of GPCRs.
内容类型	期刊论文
源URL	[http://210.75.249.4/handle/363003/60489]
专题	西北高原生物研究所_中国科学院西北高原生物研究所
推荐引用方式 GB/T 7714	Qu, Lala,Zhang, Xiuli,Wang, Jixia,et al. Phenotypic assessment and ligand screening of ETA/ETB receptors with label-free dynamic mass redistribution assay[J]. NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY,2019,393(6).
APA	Qu, Lala.,Zhang, Xiuli.,Wang, Jixia.,Zhou, Han.,Hou, Tao.,...&Liang, Xinmiao.(2019).Phenotypic assessment and ligand screening of ETA/ETB receptors with label-free dynamic mass redistribution assay.NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY,393(6).
MLA	Qu, Lala,et al."Phenotypic assessment and ligand screening of ETA/ETB receptors with label-free dynamic mass redistribution assay".NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY 393.6(2019).