GPR151 Membrane Protein Introduction

Introduction of GPR151

GPR151, also known as PGR7, GALR4, GPCR-2037, and GALRL, belongs to the A type of G protein-coupled receptor (GPCR) for which the endogenous ligand remains unknown and it shows the highest homology to the galanin receptors 2 and 3 but responds only very weakly to the neuropeptide galanin. It is encoded by the GPR151 gene which is located at 5q32, and the mass of it is 46,637 Da in human. At the same time, GPR151 is highly conserved from lower vertebrates to mammals, including humans

Function of GPR151 Membrane Protein

The activity of GPR151 is mediated by G proteins, its expression is enriched in specific diencephalic structures, where the highest levels are observed in the habenular area, in the nervous system of vertebrates. Sequence-structure phylogenetic analysis of the rhodopsin-like family placed GPR151 within ‘cluster 14’, together with galanin receptor 1 (GalR1), GalR2, GalR3 and the kisspeptin receptor (Kiss1R/Gpr54). Besides, GPR151 belongs to the highly druggable Class A of GPCRs, makes it a potential target for novel treatment modalities for common and devastating psychiatric maladies such as mood disorders and drug dependence. What’ s more, GPR151 has recently been shown to be significantly up-regulated in the dorsal root ganglia following neuronal injury models of neuropathic pain, however, the GPR151 orphan receptor does not appear to be involved in the modulation of pain-related behaviors. It is worth mentioning that through modulation of cholinergic, serotonergic and peptidergic neuronal circuits in the brainstem, 151 may coordinate functions related to addiction, reinforcement learning, decision-making, pain processing, and depression.

Fig.1 GPCRs initially interact with their signaling partners before they leave the biosynthetic machinery (Dupré, 2009).

Application of GPR151 Membrane Protein in Literature

1. Holmes F.E., et al. Targeted disruption of the orphan receptor Gpr151 does not alter pain-related behaviour despite a strong induction in dorsal root ganglion expression in a model of neuropathic pain. Molecular & Cellular Neurosciences. 2016, 78:35-40. PubMed ID: 27913310
   
   

   This article indicates that despite the very large upregulation in the DRG after a nerve injury model of neuropathic pain, the Gpr151 orphan receptor does not appear to be involved in the modulation of pain-related behaviors. Further, galanin is unlikely to be an endogenous ligand for Gpr151.

2. Broms J., et al. Monosynaptic retrograde tracing of neurons expressing the G-protein coupled receptor Gpr151 in the mouse brain. Journal of Comparative Neurology. 2017, 525(15). PubMed ID: 28657115
   
   

   This article presents a map of the afferent connectivity of a diencephalic neuronal population defined by Gpr151 expression, neuronal population will facilitate the design of investigations regarding the function of GPR151 as well as the interpretation of the effects of pharmacological modulators of this system.

3. Broms J., et al. Conserved expression of the GPR151 receptor in habenular axonal projections of vertebrates. Journal of Comparative Neurology. 2015, 523(3), 359-380. PubMed ID: 25116430
   
   

   The data of this article demonstrates that GPR151 is highly conserved, specific for a subdivision of the habenular neurocircuitry, and constitutes a promising novel target for psychiatric drug development.

4. Emdin C.A., et al. Analysis of predicted loss-of-function variants in UK Biobank identifies variants protective for disease. Nature Communications. 2018, 9:1613. PubMed ID: 29691411
   
   

   This article identifies 18 new low-frequency or rare (allele frequency < 5%) predicted loss-of-function (pLOF) variant-phenotype associations, one of them is GPR151, and then it revealed that pLOF variants in the gene GPR151 protect against obesity and type 2 diabetes.

5. Wagner F., et al. Microarray analysis of transcripts with elevated expressions in the rat medial or lateral habenula suggest fast GABAergic excitation in the medial habenula and habenular involvement in the regulation of feeding and energy balance. Brain Structure & Function. 2016, 221(9):4663-4689. PubMed ID: 26888156
   
   

   This article reveals that several G-protein related receptors, including GPR151, and many neuropeptides related to feeding are differentially expressed in the habenular region, indicating that its involvement in the regulation of food consumption and energy expenditure may have been underestimated so far.

GPR151 Preparation Options

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Reference

1. Dupré D J, et al. (2009). The role of G_βγ subunits in the organization, assembly, and function of gpcr signaling complexes. Annu Rev Pharmacol Toxicol. 49(49), 31-56.

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