Introduction of AGTR1

AGTR1 or AT₁ is a classic seven-transmembrane domain G-protein coupled receptor (GPCR). It is the most frequently studied and best-characterized angiotensin receptor. It activates a classical Gq/11 protein and phospholipase C pathway to produce second messengers, such as inositol trisphosphate and diacylglycerol, leading to the intracellular calcium flux and activation of protein kinases including the extracellular regulated kinases, ERK1/2. In murine species, the AT₁ receptor is subdivided into AT_1A and AT_1B subtypes, while in other mammalian species, including human, this subdivision does not exist.

Functions of AGTR1 Membrane Protein

AGTR1 functions by binding to angiotensin II, which is the octapeptide hormone product of the renin-angiotensin system (RAS). Most of the physiological actions of Angiotensin II, including vasoconstriction, aldosterone secretion, and sodium / potassium / water balance, are mediated by the AGTR1 receptor. It plays a critical role in the controlling of blood pressure and volume in the cardiovascular system. The polymorphism of AGTR1 gene has been reported to be associated with antihypertensive treatment and myocardial infarction risk. Because AGTR1 is a major therapeutic target in treating hypertension and cardiovascular and renal diseases, the pharmacology of this receptor has been extensively studied. As a result, many peptide agonists and antagonists, as well as nonpeptide ADRB1 receptor blockers have been developed.

Fig.1 The mechanism by which Ang II mediates vasoconstriction. (Kirabo, 2010)

Applications of AGTR1 Membrane Protein in Literature

1. Wiwattanathum P., et al. Successful treatment of anti-angiotensin II type 1 receptor antibody-associated rejection in kidney transplantation: a case report. Transplantation Proceedings. 2018, 50(3): 877-880. PMID: 29331505

This article presented a kidney transplant recipient who experienced anti-angiotensin II type 1 receptor antibody-associated allograft rejection.

2. Amina S., et al. Role of angiotensin II and angiotensin type-1 receptor in scorpion venom-induced cardiac and aortic tissue inflammation. Experimental & Molecular Pathology. 2016, 102(1): 32-40. PMID: 27955986

This article investigated the involvement of angiotensin II and angiotensin type-1 receptor in cardiac and aortic inflammatory response induced by scorpion venom.

3. Sas A., et al. Histopathological relevance of angiotensin II type 1 receptor (AT1-Receptor) in renal transplant biopsy. Transplantation Proceedings. 2018, 50(6): 1847-1849. PMID: 30056913

This article evaluated the expression of AT1-receptor and its relationship with graft loss in patients who had a renal transplant biopsy for the cause. The results showed that this receptor could be used for transplant immunological risk assessment.

4. Hamilton K., et al. Endothelium-derived contraction in a model of rheumatoid arthritis is mediated via angiotensin II type 1 receptors. Vascular Pharmacology. 2017, 100: 51-57. PMID: 29122658

This article examined the role of endothelium-derived constricting factors and the angiotensin II type 1 receptor (AGTR1) pathway in the vascular impairment in a rat model of rheumatoid arthritis. The results showed that endothelium-derived contraction was mediated via AGTR1.

5. Aggarwal S., et al. A longitudinal analysis of angiotensin II type 1 receptor antibody and angiogenic markers in pregnancy. American Journal of Obstetrics and Gynecology. 2017, 216(2): 170.e1-170. PMID: 27793555

This article assessed the longitudinal changes and utility of biomarker angiotensin II type 1 receptor antibodies and angiogenic markers in hypertensive disorders of pregnancy, gestational hypertension, and preeclampsia.

AGTR1 Preparation Options

High yields of functional and stable membrane proteins are hard to be obtained. Recent years have seen the refinement of classical and new technologies, which has resulted in a significant step forward in the field of membrane protein research. Creative Biolabs has mastered the most commonly used strategies and methods for membrane protein reconstitution. Our versatile Magic™ Platform enables many flexible options, from which you can always find a suitable format for your particular project at hand. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-AGTR1 antibody development services.

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Having successfully generated a number of difficult-to-prepare membrane proteins, Creative Biolabs is confident in providing our clients with functional formats of your target protein with high purity, stability, and yields. Please feel free to contact us for more information.

Reference

1. Kirabo, A. and Sayeski, P. P. (2010). Jak2 tyrosine kinase: a potential therapeutic target for at1 receptor mediated cardiovascular disease. Pharmaceuticals. 3(11), 3478-3493.

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