GPR87 Membrane Protein Introduction

Introduction of GPR87

Probable G-protein coupled receptor 87 (GPR87) is a protein that in humans is encoded by the GPR87 gene. This gene encodes a G protein-coupled receptor and is located in a cluster of G protein-coupled receptor genes on chromosome 3. The encoded protein has been shown to be overexpressed in lung squamous cell carcinoma and regulated by p53. G protein-coupled receptors play a role in cell communication. They are characterized by an extracellular N terminus, 7 transmembrane regions, and an intracellular C.

Basic Information of GPR87
Protein Name	G-protein coupled receptor 87
Gene Name	GPR87
Aliases	G-protein coupled receptor 95, GPR95, FKSG78
Organism	Homo sapiens (Human)
UniProt ID	Q9BY21
Transmembrane Times	7
Length (aa)	358
Sequence	MGFNLTLAKLPNNELHGQESHNSGNRSDGPGKNTTLHNEFDTIVLPVLYLIIFVASILLNGLAVWIFFHIRNKTSFIFYLKNIVVADLIMTLTFPFRIVHDAGFGPWYFKFILCRYTSVLFYANMYTSIVFLGLISIDRYLKVVKPFGDSRMYSITFTKVLSVCVWVIMAVLSLPNIILTNGQPTEDNIHDCSKLKSPLGVKWHTAVTYVNSCLFVAVLVILIGCYIAISRYIHKSSRQFISQSSRKRKHNQSIRVVVAVFFTCFLPYHLCRIPFTFSHLDRLLDESAQKILYYCKEITLFLSACNVCLDPIIYFFMCRSFSRRLFKKSNIRTRSESIRSLQSVRRSEVRIYYDYTDV

Function of GPR87 Membrane Protein

GPR87 is a cell surface GPCR which is overexpressed in various cancers. It plays a vital role in tumor cell survival. A previous study identified GPR87 as one of five GPCRs significantly overexpressed in squamous cell carcinoma. Overexpression of GPR87 in non-small cell lung carcinoma (NSCLC) is significantly correlated with poorer differentiation. Higher expression of GPR87 is significantly associated with poorer survival for patients with NSCLC. Moreover, GPR87 is essential for p53-dependent cell survival of RKO and MCF7 cell lines in response to DNA damage induced by doxorubicin or camptothecin and may serve as a novel therapeutic target for cancer treatment and prevention. GPR87 is also overexpressed in bladder cancer and promotes cell proliferation in bladder cancer cells.

Fig.1 Signal transduction by GPR87 and its role in cell clustering and transformation. (Niss, 2017)

Application of GPR87 Membrane Protein in Literature

Wang L., et al. Overexpression of G protein-coupled receptor GPR87 promotes pancreatic cancer aggressiveness and activates NF-κB signaling pathway. Mol Cancer. 2017, 16(1): 61. PubMed ID: 28288630

The article reports that GPR87 enhanced pancreatic cancer aggressiveness by activating NF-κB signaling pathway. GPR87 plays a critical oncogenic role in pancreatic cancer progression and may be used as a target for pancreatic cancer therapy.
Niss Arfelt K., et al. SREB2/GPR87, a schizophrenia risk factor, negatively regulates hippocampal adult neurogenesis and neurogenesis-dependent learning and memory. Cell Signal. 2017, 30: 9-18. PubMed ID: 27865873

The article indicates that the robust surface expression of GPR87 and general high druggability of GPCRs make GPR87 an attractive future anticancer target for drugs.
Zhang X., et al. G Protein-Coupled Receptor 87 (GPR87) Promotes Cell Proliferation in Human Bladder Cancer Cells. Int J Mol Sci. 2015, 16(10): 24319-31. PubMed ID: 26473854

Authors in this group find that GPR87 promotes cell proliferation in human bladder cancer cells and it appeared to be a promising target for gene therapy.
Okazoe H., et al. Expression and role of GPR87 in urothelial carcinoma of the bladder. Int J Mol Sci. 2013, 14(6):12367-79. PubMed ID: 23752273

This article focuses on the possible role of GPR87 in urothelial carcinoma of the bladder. The results suggest that progression from non-muscle-invasive to muscle-invasive tumor was more frequently observed in patients with GPR87-positive tumors.
Yan M., et al. G protein-coupled receptor 87 (GPR87) promotes the growth and metastasis of CD133⁺ cancer stem-like cells in hepatocellular carcinoma. PLoS One. 2013, 8(4): e61056. PubMed ID: 23593389

This article reports that GPR87 promotes the growth and metastasis of CD133(+) cancer stem-like cells, which may reveal new targets for prevention or therapy of hepatocellular carcinoma.

GPR87 Preparation Options

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Reference

Niss Arfelt K, et al. (2017). Signaling via G proteins mediates tumorigenic effects of GPR87. Cell Signal. 30: 9-18.

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