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Neuropeptide S Family Related Drug Discovery Products

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Neuropeptide S (NPS), the endogenous ligand of the orphan Gq- and Gs-protein coupled receptor GPR154 (NPSR1), was initially discovered. With the exception of fish, all tetrapodes contain the gene that codes for the NPS precursor peptide, and mammalian species share this gene's highly conserved sequence. The brain, thyroid, salivary, and mammary glands are the organs that express the NPS/NPSR1 system at the highest level. Only the pons in humans has been studied for Nps mRNA expression, which was discovered in the extension of the medial and lateral parabrachial nuclei, in the Kölliker-Fuse nucleus, and all around the nearby lateral lemniscus and pontine central gray matter.

Overview of the impact of the administration of NPS in various brain areas in rodents. Fig.1. Overview of the impact of the administration of NPS in various brain areas in rodents. (Tobinski & Rappeneau, 2021)

Creative Biolabs can offer in vitro assays and related products to meet the needs of neuropeptide S family drug discovery:

Overview of Neuropeptide S Family

  • NPSR1

These two primary transcripts of NPSR1 have nine exons and alternative 30 exons. NPSR1-A and NPSR1-B both encode proteins with 371 and 377 amino acids, respectively. All terrestrial animals share the Genetic sequences that code for NPS peptide precursor, whereas fish do not. Studies on the distribution of NPSR1 expression in human tissues have revealed that it is widely distributed. Northern blotting demonstrated that peripheral leukocytes and all eight organs examined—including the spleen, thymus, prostate, testis, uterus, small intestine, colon, and lung—express NPSR1. According to immunohistochemistry, isoform B is primarily found in the apical epithelial cells of the bronchus, stomach, and skin, while isoform A is primarily present in smooth muscle cells.

Two-dimensional illustration of human NPSR1-A and NPSR1-B. Fig.2. Two-dimensional illustration of human NPSR1-A and NPSR1-B. (Zhang & Tao, 2019)

Neuropeptide S Family Drug Discovery

GPCRs are the largest family of membrane proteins in human. GPCRs have traditionally been significant targets for drug development since they regulate practically all physiological activities. One of the most prevalent chronic diseases is asthma, and NPSR1, a member of the family A GPCRs, exhibits a strong correlation with the disease. It is crucial to research NPSR1 mutations and find ligands in order to create novel asthma medications. Our understanding of the connection between NPSR1 and asthma is currently limited, despite various investigations on the SNPs and functions of NPSR1. To investigate NPSR1's future therapeutic potential for asthma, more research on this gene is required.

References

  1. Tobinski, A.M.; Rappeneau, V. Role of the neuropeptide S system in emotionality, stress responsiveness and addiction-like behaviours in rodents: relevance to stress-related disorders. Pharmaceuticals. 2021, 14(8): 780.
  2. Zhang, Z.R.; Tao, Y.X. Physiology, pharmacology, and pathophysiology of neuropeptide S receptor. Progress in Molecular Biology and Translational Science. 2019, 161: 125-148.

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