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Identification of a Novel Small-Molecule Agonist for Human G Protein-Coupled Receptor 3

Identification of a Novel Small-Molecule Agonist for Human G Protein-Coupled Receptor 3

Chenli Ye, Zhenghong Zhang, Zhilong Wang, Qiuhong Hua, Ru Zhang, Xin Xie

J Pharmacol Exp Ther. 2014 Jun;349(3):437-43.

PMID: 24633425

Abstract:

G protein-coupled receptor 3 (GPR3) is an orphan G protein-coupled receptor (GPCR) predominantly expressed in mammalian brain and oocytes. GPR3 plays important roles in these two organs and is known as a Gαs-coupled receptor-activated constitutively in cells. However, the signal transduction pathway and pharmacological function of GPR3 remain unclear because of the lack of a specific ligand. By use of a human embryonic kidney 293 cell line stably expressing FLAG-GPR3-green fluorescent protein, a chemical screening for GPR3 ligands was performed using homogeneous time-resolved fluorescence cAMP assay. Diphenyleneiodonium chloride (DPI) was identified as a novel agonist of GPR3 with weak or no cross-reactivity with other GPCRs. DPI was further characterized to activate several GPR3-mediated signal transduction pathways, including Ca(2+) mobilization, cAMP accumulation, membrane recruitment of β-arrestin2, and receptor desensitization. Parallel studies revealed that the activity of DPI is much more pronounced than sphingosine 1-phosphate, a previously reported GPR3 agonist. Our study identified a novel and specific agonist of GPR3, which provides a useful tool for further study of this orphan GPCR.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP4673261-B	Diphenyleneiodonium Chloride - CAS 4673-26-1		4673-26-1	Price

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