UTS2R Membrane Protein Introduction

Introduction of UTS2R

UTS2R, a rhodopsin family G protein coupled-receptor, is encoded by UTS2R gene. It can be expressed in many tissues, such as brain, peripheral tissues, and blood vessels. Many studies conducted on UTS2R show that it has two endogenous agonists, one is urotensin II, and the other is urotensin II-related peptide. It can active the hypothalamic paraventricular neurons (PVN) which leads to increased plasma levels of adrenocorticotropic hormones. Meanwhile, researches during the past few decades suggest it is associated with various diseases, which provides possibilities for therapeutic applications.

Function of UTS2R Membrane Protein

Urotensin II and Urotensin-II receptors are important molecular factors that regulate vasoconstriction and all the diseases that are linked to the abnormalities in blood pressure regulation (i.e., hypertension, kidney diseases, cirrhosis). Recently, Urotensin II and its receptor have also been involved in metabolic syndrome, diabetes, and schizophrenia. Recent strong findings suggest that Urotensin II and its receptor are involved in the onset and development of different epithelial cancers. Indeed, it is reported that cell growth, motility, and invasion in human breast, bladder, prostate, colorectal and glioblastoma cancer cells are regulated by Urotensin II and Urotensin-II receptor axis, which also regulates focal adhesion kinase and small Guanosine-5'-triphosphate binding proteins that likely have a role in motility and invasion mediated by Urotensin-II receptor.

Fig.1 Schematic representation of the structure of human UT. (Hélène, 2017)

Application of UTS2R Membrane Protein in Literature

1. Yigit M., et al. Oxidative/antioxidative status, lymphocyte DNA damage, and urotensin-2 receptor level in patients with migraine attacks. Neuropsychiatr Dis Treat. 2018, 14, 367-374. PubMed ID: 29416338
   
   

   This article conducts a study in patients with migraine attacks, trying to analyze the level of oxidative/antioxidative status, lymphocyte DNA damage, and urotensin-2 receptor. These results show that the higher level is found in patients with a migraine compared to controls.

2. Bandholtz S., et al. Urolinin: The first linear peptidic urotensin-II receptor agonist. J Med Chem. 2018, 59(22), 10100-10112. PubMed ID: 27791374
   
   

   This article reveals that individual U-II amino acid positions and side chain characteristics play an important role in U-IIR activation, which helps to identify the first peptidic Urotensin-II Receptor Agonist.

3. Federico A., et al. Urotensin-II receptor: A double identity receptor involved in vasoconstriction and in the development of digestive tract cancers and other tumors. Cancer Drug Targets. 2017, 17(2), 109-121. PubMed ID: 27338741
   
   

   Authors in this group analyze the expression level and pathway of Urotensin II and its receptor in different kinds of cancers. These results indicate that its expression on tumor tissues is strongly associated with clinical therapy and disease diagnosis.

4. Lim C.J., et al. Benzo[b]thiophene-2-carboxamide derivatives as potent urotensin-II receptor antagonists. Bioorg Med Chem Lett. 2016, 26(19), 4684-4686. PubMed ID: 27597245
   
   

   Authors in this article synthesize and evaluate a series of benzo[b]thiophene-2-carboxamide derivatives, and trying to find whether they can be potent urotensin-II receptor antagonists.

5. Cadirci E., et al. Blocking of urotensin receptors as new target for treatment of carrageenan induced inflammation in rats. Peptides. 2016, 82, 35-43. PubMed ID: 27208703
   
   

   This article conducts a study in rats which have acute inflammation induced by carrageenan, to identify whether blocking of urotensin receptors can be used to treat this disease in rats. This study shows the role of urotensin II receptors in the physiopathogenesis of acute inflammatory response that underlying many diseases accompanied by inflammation.

UTS2R Preparation Options

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Reference

1. Hélène Castel, et al. (2017) The G protein-coupled receptor UT of the neuropeptide urotensin II displays structural and functional chemokine features. Front Endocrinol (Lausanne). 8, 76.

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