GPR39 Membrane Protein Introduction

Introduction of GPR39

GPR39 is a protein encoded by the human GPR39 gene. It is a G-protein-coupled receptor (GPCR) and a member of the ghrelin/neurotensin peptide receptor subfamily which was initially found in all vertebrates. During the past years, a series of studies have proved that GPR39 plays a key role in diverse cellular and physiological processes.

Function of GPR39 Membrane Protein

As an orphan GPCR receptor belonging to the G protein-coupled receptor (GPCR) family, GPR39 is widely expressed in various mammalian tissues, such as the pancreas, gastrointestinal tract, liver, kidney, and brain. Particularly, the expression level of GPR39 is very high in digestive system. In addition, the expression of GPR39 is also found in adipose tissue, spleen, lung, heart, and reproductive tissue of several species. It has been reported that GPR39 is an active player in a diverse range of physiological and cellular events, such as insulin secretion, tumorigenesis, obesity, wound healing, cell death inhibition, proliferation and differentiation of colonocytes. Furthermore, studies have shown that GPR39 could act as an important regulator of gastrointestinal motility and secretion. Recently, several studies, including receptor knockout studies, have suggested that GPR39 is a potential target for several diseases, including type 2 diabetes and depression. And growing evidence shows that GPR39 is potently stimulated by Zn²⁺ and therefore functions as a unique membrane Zn²⁺ sensing receptor.

Fig.1 Schematic representations of common Zn²⁺ sensing receptor, ZnR/GPR39, signaling in epithelial cells. (Sunuwar, 2017)

Application of GPR39 Membrane Protein in Literature

1. Shimizu Y., et.al. Rho kinase-dependent desensitization of GPR39; a unique mechanism of GPCR downregulation. Biochemical pharmacology. 2017, 140:105-14. PubMed ID: 28619258
   
   

   This article focuses on the mechanism of feedback regulation of GPR39 function. It suggests a unique desensitization mechanism regulated by the G12/13/ROCK pathway and also identifies a novel biased ligand which avoids desensitization by biased signal transduction. These findings may be helpful for understanding the mechanism of receptor desensitization and the development of better drugs targeting GPR39.

2. Romero-Nava R., et.al. Evidence of alterations in the expression of orphan receptors GPR26 and GPR39 due to the etiology of the metabolic syndrome. Journal of Receptors and Signal Transduction. 2017, 37(4):422-9. PubMed ID: 28270014
   
   

   This article aims to evaluate the expression of the GPR39 orphan receptor in two models of metabolic syndrome (diet and genetics). It reveals that the orphan receptors GPR39v1 and GPR39v2 are expressed in different tissues and their profile expression is dependent on the etiology of the metabolic syndrome.

3. Shao Y.X., et.al. Zinc Supplementation, via GPR39, Upregulates PKCζ to Protect Intestinal Barrier Integrity in Caco-2 Cells Challenged by Salmonella enterica Serovar Typhimurium. The Journal of nutrition. 2017, 147(7):1282-9. PubMed ID: 28515165
   
   

   This article focuses on the roles of G protein-coupled receptor (GPR) 39 and protein kinase Cζ (PKCζ) in the regulation by zinc of intestinal barrier function. It demonstrates that zinc upregulates PKCζ by activating GPR39 to enhance the abundance of ZO-1, thereby improving epithelial integrity in S. typhimurium-infected Caco-2 cells.

4. Kolodziejski P.A., et.al. Changes in obestatin gene and GPR39 receptor expression in peripheral tissues of rat models of obesity, type 1 and type 2 diabetes. Journal of diabetes. 2017, 9(4):353-61. PubMed ID: 27106635
   
   

   This article aims to investigate changes in obestatin and GPR39 in pathophysiological conditions like obesity, type 1 and type 2 diabetes mellitus (T1DM and T2DM, respectively). It indicates that GPR39 may contribute to metabolic abnormalities in T1DM, T2DM, and obesity.

5. Frimurer T.M., et.al. Model-based discovery of synthetic agonists for the Zn²⁺-Sensing G-protein-coupled receptor 39 (GPR39) reveals novel biological functions. Journal of medicinal chemistry. 2017, 60(3):886-98. PubMed ID: 28045522
   
   

   This article reveals that GPR39 is a novel regulator of gastric somatostatin secretion.

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Reference

1. Sunuwar, et.al. (2017). The zinc sensing receptor, ZnR/GPR39, in health and disease. Frontiers in bioscience. 22: 1469-1492.

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