GPR75 Membrane Protein Introduction

Introduction of GPR75

Probable G-protein coupled receptor 75 (GPR75) is a protein that in humans is encoded by the GPR75 gene. GPR75 belongs to the G protein-coupled receptor family, which is a type of cell surface receptors that activate guanine-nucleotide binding proteins upon the binding of a ligand. G protein-coupled receptor can be activated by the chemokine Chemokine (C-C motif) ligand 5 (RANTES). GPRs stimulate inositol trisphosphate production and calcium mobilization upon activation by coupled to heterotrimeric G_q proteins. GPR75 activates the downstream signaling pathway involving the PI3, Akt and MAP kinases and plays a role in neuron survival. GPR75 may also be activated to regulate the insulin secretion by pancreatic islet cells.

Function of GPR75 Membrane Protein

A study conducted by Dr. Schwartzman's lab at the New York Medical College found that 20-hydroxyeicosatetraenoic acid (20-HETE), a bioactive eicosanoid formed by ω-hydroxylation of arachidonic acid, mediated its hypertension effects on the vascular system by activating GPR75 (G_q) signaling. GPR75 is also associated with diseases such as Doyne cellular retinal dystrophy. Among the related pathways of it are Peptide ligand-binding receptors. Gene ontology (GO) annotations associated with this gene include G protein-coupled receptor activity and C-C chemokine receptor activity.

Fig.1 Hypothetical incorporation of the GPR75 signaling pathways in attempt to explain the established vascular and renal tubular effects of 20-hydroxyeicosatetraenoic acid (20-HETE). (Fan, 2017)

Application of GPR75 Membrane Protein in Literature

1. Dedoni S., et al. The Orphan G Protein-coupled Receptor 75 Signaling is Activated by the Chemokine CCL5. J Neurochem. 2018. PubMed ID: 29772059
   
   

   Authors in this group investigate whether CCL5 could activate a G_q signaling through GPR75. The results show that GPR75 signaling is activated by the chemokine CCL5 and the findings may help to develop small molecule GPR75 agonists that mimic CCL5.

2. Garcia V., et al. 20-HETE Signals Through G-Protein-Coupled Receptor GPR75 (Gq) to Affect Vascular Function and Trigger Hypertension. Circ Res. 2017, 120(11): 1776-1788. PubMed ID: 28325781
   
   

   The article reports that 20-HETE signals through GPR75 (G_q) to affect vascular function and trigger hypertension. They first identify a GPCR target for an eicosanoid of this class and may provide the molecular basis for the signaling and pathophysiological functions mediated by 20-HETE in hypertension and cardiovascular diseases.

3. Fan F., et al. GPR75 Identified as the First 20-HETE Receptor: A Chemokine Receptor Adopted by a New Family. Circ Res. 2017, 120(11): 1696-1698. PubMed ID: 28546348
   
   

   The article reports that 20-HETE acts via the G-protein-coupled receptor GPR75. Activation of this receptor can protect hippocampus from β-amyloid toxicity and stimulate insulin secretion in pancreatic islet cells.

4. Liu B., et al. The novel chemokine receptor, G-protein-coupled receptor 75, is expressed by islets and is coupled to stimulation of insulin secretion and improved glucose homeostasis. Diabetologia. 2013, 56(11): 2467-76. PubMed ID: 23979485
   
   

   Authors in this group measure islet CCL5 receptor mRNA expression and detected GPR75 in islets. It shows that although CCL5 is implicated in the pathogenesis of diabetes through activation of CCRs, it has beneficial effects on beta cells through GPR75 activation.

5. Liu B., et al. The novel chemokine receptor, G-protein-coupled receptor 75, is expressed by islets and is coupled to stimulation of insulin secretion and improved glucose homeostasis. Diabetologia. 2013, 56(11): 2467-76. PubMed ID: 23979485
   
   

   This article reveals that CCL5 is implicated in the pathogenesis of diabetes through activation of CCRs. CCL5 has beneficial effects on beta cells through GPR75 activation.

GPR75 Preparation Options

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Reference

1. Fan F, et al. (2017). GPR75 Identified as the First 20-HETE Receptor: A Chemokine Receptor Adopted by a New Family. Circ Res. 120(11): 1696-1698.

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