GPR160 Membrane Protein Introduction

Introduction of GPR160

GPR160 is encoded by the GPR160 gene. It belongs to the G-protein-coupled receptor (GPCR) family which have been implicated in the tumorigenesis and metastasis of human cancers and are considered amongst the most desirable targets for drug development. GPR160 is an orphan class A GPCR previously annotated as GPCR1 or GPCR150. The human GPR160 protein is comprised of 338 amino acids and encoded by 7 exons located at 3q26.2-q27. Orthologues of GPR160 have been identified in the Rhesus monkey, dog, cow, rat, mouse, chicken, zebrafish, and frog.

Function of GPR160 Membrane Protein

G protein-coupled receptors (GPCRs) are cell membrane proteins which transduce extracellular signals into intracellular effector pathways through the activation of heterotrimeric G proteins. It has been reported that GPR160 is associated with apoptosis and cell cycle arrest of prostate cancer cells. The transcription levels of GPR160 in the prostate cancer tissue samples and cell lines, such as DU145, PC-3, and 22Rv1 cells, were evidently higher than that seen in normal prostate tissue and cells, and scientists have proved that the expression level of endogenous GPR160 is associated with the pathogenesis of prostate cancer. Beyond that, knockdown of GPR160 in prostate cancer cells increased the expression of caspase 1 and IL6, induced cell cycle arrest and apoptosis. What’s more, it has been found that GPR160 expression was significantly upregulated in the dorsal horn of the spinal cord in two models of neuropathic pain in rats. It also reveals that GPR160 may be a potential therapeutic target to mitigate chronic neuropathic pain conditions.

Fig.1 Representative structures of G protein-coupled receptors from Class A, B, and C. (Mace, 2015)

Application of GPR160 Membrane Protein in Literature

1. Zhou C., et al. G Protein-Coupled Receptor GPR160 Is Associated with Apoptosis and Cell Cycle Arrest of Prostate Cancer Cells. Oncotarget. 2016, 7(11), 12823-12839. PubMed ID: 26871479
   
   

   This article investigates the potential function of GPR160 in the pathogenesis of prostate cancer. Knockdown of GPR160 by ShGPR160 made prostate cancer cell apoptosis and growth arrest both in vitro and in athymic mice. It suggests that the expression level of endogenous GPR160 is associated with the pathogenesis of prostate cancer.

2. Harada C., et al. (187) Identification of spinal GPR160 as a novel protein promoting chronic neuropathic pain states. The Journal of Pain. 2017, 18 (4), S23.
   
   

   This article reveals a previously unrecognized role for GPR160 in the induction and maintenance of neuropathic pain states. Knockdown of spinal GPR160 expression prevented and reversed neuropathic pain functionally linking GPR160 to the neuropathic pain phenotype. It shows that GPR160 is a potential therapeutic target to mitigate chronic neuropathic pain conditions.

3. Yang H., et al. G protein-coupled receptor160 regulates mycobacteria entry into macrophages by activating ERK. Cellular Signalling. 2016, 28(9), 1145. PubMed ID: 27259691
   
   

   This article shows an important role of GPR160 in regulating the entry of BCG into macrophages by targeting the ERK signaling pathway. As GPCRs have proven to be successful drug targets in the pharmaceutical industry, it's tempting to speculate that compounds targeting GPR160, a G protein-coupled receptor, could intervene in Mtb infection.

4. Lee J. E., et al. MicroRNA signatures associated with immortalization of EBV-transformed lymphoblastoid cell lines and their clinical traits. Cell Proliferation. 2011, 44(1), 59-66. PubMed ID: 21199010
   
   

   This study identifies miRNAs associated with terminal immortalization of Epstein-Barr virus (EBV)-transformed lymphoblastoid cell line (LCL) and associated clinical traits. It has been found that miR-125b is the putative negative regulator of GPR160, which is found to be differentially expressed in LCLs during long-term culture.

GPR160 Preparation Options

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Reference

1. Mace O. J., et al. (2015). Pharmacology and physiology of gastrointestinal enteroendocrine cells. Pharmacology Research & Perspectives. 3(4), e00155.

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