Introduction of AGTR2

AGTR2, also known as AT₂, is an angiotensin II receptor and it is an integral membrane protein belonging to the G protein-coupled receptor (GPCR) family. The cDNA for AGTR2 encodes a 363-amino acid protein, with a molecular weight of 41220 Da. This receptor shares only ~34% sequence homology with the AT₁ receptor. The gene for AGTR2 resides on the X-chromosome and has 3 exons with the entire coding region on the third exon. With respect to G-protein coupling, studies have suggested that AGTR2 may be coupled to G-proteins and that the third intracellular loop may be linked with the cell signaling pathway involving G_i and extracellular signal-regulated kinases (ERK) inactivation.

Functions of AGTR2 Membrane Protein

AGTR2 functions through its binding with angiotensin II, which is a potent pressor hormone responsible for regulating the aldosterone secretion and controlling blood pressure and volume in the cardiovascular system. Mice studies have revealed that AGTR2 plays a physiologically relevant protective role in the vasculature. Generally, it functions opposing the AT1-receptor such as mediating a vasorelaxant effect, inhibiting proliferation, and promoting cell differentiation. Besides, this receptor is also distributed in brain regions, including some thalamic nuclei, the cerebellum, and the inferior olivary nucleus. AGTR2-deficient mice show reduced spontaneous movement and exploratory behavior, and there is evidence of AGTR2 involving in cognitive function and memory. Moreover, this receptor is highly expressed in fetal tissues but regresses substantially in the postnatal period. In the adult, the AGTR2 expression is upregulated in pathophysiological situations involving tissue remodeling, inflammation, and/or repair. Upregulation of this receptor is observed in a variety of tumors, including ductal and invasive breast carcinoma, gastric cancer and lymph node metastases, high-grade astrocytoma, and high-grade renal cell carcinoma.

Fig.1 Signal transduction mechanisms and physiological effects of the AT₂ receptor. (Nouet, 2000)

Applications of AGTR2 Membrane Protein in Literature

1. Ishiguro S., et al. Involvement of angiotensin II type 2 receptor (AT2R) signaling in human pancreatic ductal adenocarcinoma (PDAC): a novel AT2R agonist effectively attenuates growth of PDAC grafts in mice. Cancer Biology & Therapy. 2015, 16(2): 307-316. PMID: 25756513

This study demonstrated that AT2R had been involved in human PDAC by measuring the expression of AT2R and AT1R in human PDAC specimens. The results showed that novel AT2R agonist could serve as an effective therapy for PDAC treatment.

2. Yang Y., et al. Angiotensin II type 2 receptor inhibits expression and function of insulin receptor in rat renal proximal tubule cells. Journal of the American Society of Hypertension. 2017, 12(2): 135-145. PMID: 29289466

This study found that activation of AT2R inhibited insulin receptor expression in a concentration and time-dependent manner in RPT cells from Wistar-Kyoto (WKY) rats.

3. Xiao Y., et al. Role of angiotensin II type 2 receptor during electrophysiological remodeling of left ventricular hypertrophic myocardium in spontaneously hypertensive rats. Journal of the American Society of Hypertension : JASH. 2017, 12(1): 58-65. PMID: 29100861

This study investigated the role of angiotensin II type 2 receptor during electrophysiological remodeling of the left ventricular hypertrophic myocardium (LVHM) in spontaneously hypertensive rats (SHRs). The results showed that stimulating this receptor improved the electrophysiological remodeling of LVHM in SHR.

4. Wakchaure P B., et al. Synthesis of enantiopure angiotensin II type 2 receptor [AT(2)R] antagonist EMA401. Tetrahedron. 2015, 71(38): 6881-6887.

This article reported a facile synthesis of the angiotensin II type 2 receptor antagonist EMA401 in high overall yield.

5. Gianzo M., et al. Angiotensin II type 2 receptor is expressed in human sperm cells and is involved in sperm motility. Fertility & Sterility. 2016, 105(3): 608-616. PMID: 26616438

This study investigated the presence of angiotensin II type 2 receptor (AT2R) in human spermatozoa and its implication in sperm fertility status. The results showed that AT2R was present in human semen and might be involved in the control of sperm motility.

AGTR2 Preparation Options

Membrane proteins are one of the most attractive and challenging objects as they are important therapeutic targets but difficulties exist in the study of their structure and function. Over the years Creative Biolabs has committed to this particular research field and has accomplished a number of difficult projects. We can incorporate your target membrane protein into the different systems. Our scientists are willing to share their expertise to help analyze your project and select the most suitable reconstitution strategy based on your research demands. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-AGTR2 antibody development services.

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To learn more about our membrane protein preparation services, please contact us for more detailed information.

Reference

1. Nouet, S. and Nahmias, C. (2000). Signal transduction from the angiotensin II AT2 receptor. Trends in Endocrinology & Metabolism Tem. 11(1), 1-6.

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