Introduction of GPR18
GPR18 is encoded by the GPR18 gene. GPR18 belongs to the class A G-protein-coupled receptor family which has been implicated in the tumorigenesis and metastasis of human cancers and is considered amongst the most desirable targets for drug development. GPR18 is comprised of 338 amino acid in human and it’ s gene located at 3q26.2-q27. It is expressed in midpiece of spermatozoon (at protein level), most abundant in testis and spleen, highly expressed in CD4 and CD8-positive T-cells as well as CD19-positive B-cells.
|Basic Information of GPR18|
|Protein Name||N-arachidonyl glycine receptor|
|Aliases||G-protein coupled receptor 18, NAGly receptor|
|Organism||Homo sapiens (Human)|
Function of GPR18 Membrane Protein
GPR18 is amply expressed in lymphocytes, with particularly high expression in CD8αα γδT intraepithelial lymphocytes (IELs), and it functions in establishing an IEL compartment of normal size. At the same time, small molecule agonists of GPR18 might augment the size of the KLRG1+ effector CD8 T cell compartment, which might be useful, for example, during viral responses or in the context of tumor immunotherapy. Moreover, it has revealed that GPR18 is also associated with apoptosis and cell cycle arrest of prostate cancer cells. GPR18 transcription levels in the prostate cancer tissue samples and cell lines, such as PC-3, LNCaP, DU145, and 22Rv1 cells, were obviously higher than that seen in normal prostate tissue and cells, and scientists have proved that the expression level of endogenous GPR18 is associated with the pathogenesis of prostate cancer. Beyond that, knockdown of GPR18 in prostate cancer cells increased the expression of caspase 1 and IL6, induced cell cycle arrest and apoptosis.
Fig.1 Homology model of GPR18 receptor structure (Kothandan, 2013).
Application of GPR18 Membrane Protein in Literature
This review explores the current scientific knowledge on GPR18 including its localization, signaling pathways, and pharmacology. Importantly, the involvement of nutritional factors and potential dietary regulation of GPR18 and its (patho)physiological roles are described.
This article reveals that amauromine shows antagonistic activity at the cannabinoid-like orphan receptor GPR18. The diketopiperazine 1 may thus serve as a lead structure for the development of more potent and selective GPR18 antagonists, which are required to study the orphan receptor's potential as a new drug target.
This article reveals that the most potent GPR18 antagonist was (Z)-2-(3-(4-chlorobenzyloxy)benzylidene)-6,7-dihydro-2H-imidazo[2,1b][1,3]thiazin-3(5H)-one representing the ﬁrst selective GPR18 antagonist.
This article identifies 27-O-methylasporyzin C as the first selective GPR18 antagonist with an indole structure. The new natural indole derivatives may serve as lead structures for the development of GPR18- and CB receptor-blocking drugs.
GPR18 Preparation Options
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