NPSR1 Membrane Protein Introduction

Introduction of NPSR1

Neuropeptide S receptor (NPSR1), also known as G protein-coupled receptor for asthma susceptibility or GPR154, is a 7-transmembrane G protein-coupled receptor (GPCR) which can induce intracellular signalling via mobilization of calcium, promote in cyclic adenosine monophospate (cAMP) levels, and the mitogen-activated protein kinase (MAPK) pathway. In humans, NPSR1 polymorphism is related to asthma, inflammatory bowel disease, panic disorders, rheumatoid arthritis, as well as intermediate phenotypes of functional gastrointestinal disorders.

Function of NPSR1 Membrane Protein

Numerous studies indicated that NPSR1 is widely distributed in the brain. Mutations in this gene have also been associated with many diseases. It has been shown that activation of NPSR by NPS affects both gastrointestinal motility and mucosal permeability simultaneously. In the CNS, activation of the NPSR by NPS promotes arousal and anxiolytic-like effects. So the anxiolytic and arousal-promoting effects of NPS make the NPS–NPSR1 system become an interesting potential drug target in mood-related disorders. In addition, mutations in NPSR have also been linked to a susceptibility to asthma. So activation of NPSR in the airway epithelium has a number of effects including upregulation of matrix metalloproteinases which are involved in the pathogenesis of asthma.

Fig.1 Molecular model of NPSR1. (Anedda, 2010)

Application of NPSR1 Membrane Protein in Literature

1. Streit F., et al. Sex-specific association between functional neuropeptide S receptor gene (NPSR1) variants and cortisol and central stress responses. Psychoneuroendocrinology. 2017, 76: 49-56. PubMed ID: 27883964.
   
   

   This article showed NPSR1 is highly expressed in the limbic system, exogenous NPS exerts pronounced anxiolytic and fear-attenuating effects in rodents and extensive close crosstalk between the NPS system and the hypothalamic-pituitary-adrenal (HPA) axis has been demonstrated.

2. Acevedo N., et al. Neuropeptide S (NPS) variants modify the signaling and risk effects of NPS Receptor 1 (NPSR1) variants in asthma. PloS one. 2017, 12(5): e0176568. PubMed ID: 28463995.
   
   

   The authors of this group examined the effects of different combinations of these NPS and NPSR1 variants on downstream signaling and genetic risk of asthma. In conclusion, they found NPS variants modify asthma risk and should be considered in genetic association studies of NPSR1 with asthma and other complex diseases.

3. Liao Y., et al. Human Neuropeptide S Receptor Is Activated via a Galphaq Protein-biased Signaling Cascade by a Human Neuropeptide S Analog Lacking the C-terminal 10 Residues. The Journal of biological chemistry. 2016, 291(14): 7505-16. PubMed ID: 26865629.
   
   

   This article studied on rat brain have demonstrated that NPS expression tends to be highly localized in the distinct brain stem clusters located around the locus coeruleus. They proved human NPS was identified as a biased agonist, preferentially activating a G_αq-dependent signaling cascade through NPSR.

4. Adori C., et al. Neuropeptide S- and Neuropeptide S receptor-expressing neuron populations in the human pons. Frontiers in neuroanatomy. 2015, 9: 126. PubMed ID: 26441556.
   
   

   This article showed NPSR1 expressed in a few pontine cell clusters, but widely distributed in the brain. They thought anxiolytic and arousal-promoting effects of NPS make the NPS–NPSR1 system an interesting potential drug target in mood-related disorders.

5. Pulkkinen V., et al. Neuropeptide S receptor 1 (NPSR1) activates cancer-related pathways and is widely expressed in neuroendocrine tumors. Virchows Archiv: an international journal of pathology. 2014, 465(2): 173-83. PubMed ID: 24915894.
   
   

   The authors studied whether NPS/NPSR1 could be used as a biomarker for neuroendocrine neoplasms and to identify the gene pathways affected by NPS/NPSR1. Their results showed that NETs are a source of NPS and NPSR1 and that NPS affects cancer-related pathways.

NPSR1 Preparation Options

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Reference

1. Anedda F, et al. (2011). Multiple polymorphisms affect expression and function of the neuropeptide S receptor (NPSR1). PloS one. 6(12), e29523.

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