NMUR1 Membrane Protein Introduction

Introduction of NMUR1

Neuromedin-U receptor 1 (NMUR1) is a protein which is encoded by the NMUR1 gene in humans. The gene is localized on chromosome 2q34-q37. It has been reported that NMUR1 consists of 403 amino acids with a predicted molecular mass of 44,979 Da. The expression of NMUR1 can be detected predominantly in the periphery, especially in the gastrointestinal tract. The mRNA for NMUR1 has been detected in various tissues and the expression levels are highest in peripheral tissues, such as the stomach and small intestines.

Function of NMUR1 Membrane Protein

Neuromedin U is a structurally highly conserved neuropeptide, which is involved in a series of functions that include smooth-muscle contraction, controlling the ion transport and blood flow in the intestine, and regulation of adrenocortical functions. From the functional screening assays, the NMUR1 enables the mediation of intracellular Ca²⁺ signaling with potency in the nanomolar range. It has been also reported that the NMUR1 can be associated with phosphoinositide hydrolysis. The activation of NMUR1 is able to stimulate the release of arachidonic via a Ca²⁺-dependent activation of phospholipase A2. Just same as many GPCRs, the activation of NMUR1 or NMUR2 enables the activation of the mitogen-activated protein kinase signaling pathway. In addition, the development of homology models of neuromedin U would be a potential tool in drugs discovery for the neuromedin U receptor 1 related diseases.

Fig.1 Structure of human NMUR1. (Brighton, 2004)

Application of NMUR1 Membrane Protein in Literature

1. Nagarajan S.K., et al. Binding Interaction Analysis of Neuromedin U Receptor 1 with the Native Protein Neuromedin U. 2017, 10(1):14-19.
   
   

   Neuromedin is a neuropeptide which is involved in different functions. This article performs a protein-protein docking analysis for the complex of neuromedin U and neuromedin U receptor 1. The development of homology models of neuromedin U would be a potential tool in drugs discovery for the neuromedin U receptor 1 related diseases.

2. Nagai H., et al. Differential effects of selective agonists of neuromedin U1 and 2 receptors in obese and diabetic mice. British Journal of Pharmacology. 2017, 175(2): 359. PubMed ID: 29057457
   
   

   This article reports that NMUR1 selective agonist can be a benefit for the treatment of obesity and diabetes, while the NMUR2 selective agonist can be served as the well-balanced drug for the treatment of obesity.

3. Takayama K., et al. Discovery of a Human Neuromedin U Receptor 1-Selective Hexapeptide Agonist with Enhanced Serum Stability. Journal of Medicinal Chemistry. 2017, 60(12): 5228. PubMed ID: 28548497
   
   

   This article reveals that neuromedin U is a useful antiobesity drug lead, which enables the activation of NMUR1 and NMUR2. Based on the research of structure-activity relationship of serum stability and pharmacokinetic properties, they have developed a novel human neuromedin U receptor 1-selective hexapeptide agonist with enhanced serum stability.

4. Klose C., et al. The neuropeptide neuromedin U stimulates innate lymphoid cells and type 2 inflammation. Nature. 2017, 549(7671): 282-286. PubMed ID: 28869965
   
   

   This article reveals that the NMUR1 neuronal signaling circuit offers a selective mechanism which can be used to promote rapid type 2 cytokine responses by the innate immune system and enteric nervous system.

5. Takayama K., et al. Discovery of potent hexapeptide agonists to human neuromedin u receptor 1 and identification of their serum metabolites. Acs Medicinal Chemistry Letters. 2015, 6(3): 302-7. PubMed ID: 4360155
   
   

   This article developed hexapeptide agonists 2 and 3, which are highly selective to human NMUR1 and NMUR2. Their serum metabolites have also been identified. In addition, they also tested the stability of synthesized agonists in rat and two major biodegradation sites: Phe2-Arg5-Asn6 have also been identified.

6. De A.P., et al. Development of potent and proteolytically stable human neuromedin U receptor agonists. European Journal of Medicinal Chemistry. 2018, 144: 887-897. PubMed ID: 29329072
   
   

   NMU is the highly conserved endogenous peptide which is involved in various physiological processes. According to the introduction of unnatural amino acids into the native sequence, the author has developed a novel NMU-analogs based on NMU-8.

NMUR1 Preparation Options

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