Introduction of GPR146
GPR146 is encoded by gene Gpr146, and it belongs to G protein-coupled receptor (GPCR) family, which is the most abundant receptor family residing in the cell surface. Participation in various physiological processes makes GPCR become the potential targets for numerous diseases, such as diabetes, Parkinson’s disease, infectious diseases, etc. GPR146 has the typical structure of GPCRs, consisted of an extracellular N terminus, seven transmembrane helices, and an intracellular C terminus. It is acknowledged that GPR146 is a possible receptor for proinsulin C-peptide.
|Basic Information of GPR146|
|Protein Name||G-protein coupled receptor 146|
|Organism||Homo sapiens (Human)|
Function of GPR146 Membrane Protein
GPR146 was demonstrated to be the receptor of proinsulin C-peptide, which has emerged as a promising target for the treatment of diabetes-associated microvascular complications. The binding of GPR146 and C-peptide can regulate the function of retinal pigment epithelium, a monolayer of cells in the retina. In diabetic macular edema, the blood-retinal barrier consisted of retinal pigment epithelium is disrupted. Knockdown of GPR146 will block C-peptide-induced cFos expression in KATOIII cells. Additionally, the binding of C-peptide and GPR146 has therapeutic potency in the treatment of retinopathies, neuropathies, and nephropathy. GPR146 is identified as an antiviral factor specific to RNA-virus infection, such as Vesicular stomatitis virus and Newcastle disease virus. So GPR146 may be a potential target for antiviral drugs development.
Fig.1 The model of viruses escape from GPR146-mediated antiviral function. (Huang, 2017)
Application of GPR146 Membrane Protein in Literature
In this review, the authors discuss GPR146, the putative receptor of proinsulin C-peptide has the therapeutic potency in the treatment of diabetes-associated complications. They describe various strategies, such as deorphanization strategy, to study the ‘deorphanize’ of this diverse family of receptors.
Using a unique Deductive Ligand-Receptor Matching Strategy, the authors first demonstrate that GPR146 is potential a part of the C-peptide signaling complex. In the C-peptide signalosome, GPR146 may be a platform for the elucidation.
This article verifies that GPR146 distributes on the erythrocytes of healthy humans and type 2 diabetes patients. And it can mediate the effects of C-peptide on ATP release from human erythrocytes, especially in the exposure of low O2 tension in humans with type 2 diabetes.
This article reveals the antiviral role of GPR146 in fighting viral infection. But GPR146-mediated protection is eliminated by IRF3/HES1-signalling, which suggests a potential therapeutic significance of both GPR146 and HES1 signaling in viral infection.
GPR146 Preparation Options
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