Recombinant Human Endothelin-1 Receptor (EDNRA) Protein (His)

Name: Recombinant Human Endothelin-1 Receptor (EDNRA) Protein (His)
Brand: Beta LifeScience
SKU: BLC-04398P
Availability: InStock

Greater than 90% as determined by SDS-PAGE.

Collections: All products, High-quality recombinant proteins, Other recombinant proteins

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Product Overview

Description	Recombinant Human Endothelin-1 Receptor (EDNRA) Protein (His) is produced by our Yeast expression system. This is a protein fragment.
Purity	Greater than 90% as determined by SDS-PAGE.
Uniprotkb	P25101
Target Symbol	EDNRA
Synonyms	EDNRA; ETA; ETRA; Endothelin-1 receptor; Endothelin receptor type A; ET-A; ETA-R; hET-AR
Species	Homo sapiens (Human)
Expression System	Yeast
Tag	N-6His
Target Protein Sequence	DNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLPSNGSMHNYCPQQTKITSAFK
Expression Range	21-80aa
Protein Length	Partial
Mol. Weight	8.8kDa
Research Area	Signal Transduction
Form	Liquid or Lyophilized powder
Buffer	Liquid form: default storage buffer is Tris/PBS-based buffer, 5%-50% glycerol. Lyophilized powder form: the buffer before lyophilization is Tris/PBS-based buffer, 6% Trehalose, pH 8.0.
Reconstitution	Briefly centrifuged the vial prior to opening to bring the contents to the bottom. Reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL. It is recommended to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20°C/-80°C. The default final concentration of glycerol is 50%.
Storage	1. Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. 2. Avoid repeated freeze-thaw cycles. 3. Store working aliquots at 4°C for up to one week. 4. In general, protein in liquid form is stable for up to 6 months at -20°C/-80°C. Protein in lyophilized powder form is stable for up to 12 months at -20°C/-80°C.
Notes	Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.

Target Details

Target Function	Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3.
Subcellular Location	Cell membrane; Multi-pass membrane protein.
Protein Families	G-protein coupled receptor 1 family, Endothelin receptor subfamily, EDNRA sub-subfamily
Database References	HGNC: 3179 OMIM: 131243 KEGG: hsa:1909 STRING: 9606.ENSP00000315011 UniGene: PMID: 29849817 miR200c regulates the proliferation, apoptosis and invasion of gastric carcinoma cells through the downregulation of EDNRA expression. PMID: 29286062 Presence of SST5, CXCR4 and ETA on tumor cells and of SST3, CXCR4 and ETA on microvessels gradually increased from grade II to grade IV tumors. PMID: 29696364 There is no association between the C+70G polymorphism of the EDNRA gene and the development of ischemic atherothrombotic stroke. PMID: 29064794 endothelin-A receptor-activated ABCB1 expression has a role in nintedanib resistance in FGFR1-driven small cell lung cancer PMID: 27367030 Endothelin-1 possesses an anti-apoptotic effect in vascular endothelial cells and this effect is mediated, to a great extent, via the activation of EDNRB, with a minor contribution via activation of EDNRA. PMID: 28732172 ETA and ETB receptors are present in human haemorrhoids with ETB receptors predominating PMID: 28095606 ETAR stimulation acted via downstream G-protein Galphaq/11 and Rho GTPase to suppress the Hippo pathway, thus leading to YAP/TAZ activation, which was required for ETAR-induced tumorigenesis. Overall, these results indicate a critical role of the YAP/TAZ axis in ETAR signaling PMID: 28249901 Data show that endothelin A receptor drives invadopodia function by direct interaction of beta-arrestin-1 (beta-arr1) with Rho guanine nucleotide exchange factor (GEF) 11 protein (PDZ-RhoGEF). PMID: 26522724 In control arteries, ETAR was expressed by vascular smooth muscle cells in the media whereas ETBR was hardly detected. In giant cell arteritis, both ETAR and ETBR receptors were expressed by alphaSMA-positive cells at the intima-media border. Endothelial cells and inflammatory cells also expressed both ET receptors. PMID: 28606962 Data suggest that TNFalpha (tumor necrosis factor-alpha) induces proliferation of airway smooth muscle cells via ET1 (endothelin-1), GM-CSF (granulocyte-macrophage colony-stimulating factor), and IL6 (interleukin 6) signaling; ET1 induces cell proliferation via ETAR (endothelin receptor type A); ETBR (endothelin receptor type B) is up-regulated by TNFalpha and appears to mediate ET1 effects on cell proliferation. PMID: 27422754 presence of ET-1 receptors in the chronic thrombus in proximal CTEPH suggests ET-1 could act not only on the distal vasculopathy in the unobstructed vessels but may also stimulate smooth muscle cell proliferation within chronic clot PMID: 26874031 Data show that auriculo-condylar syndrome (ACS)-associated mutations in G protein subunit alpha i3 (GNAI3) produce dominant-negative Galpha(i3) mutant proteins that couple to endothelin type A receptor (ET(A)R). PMID: 27072656 Patients with lung fibrosis and patients with high modified Rodnan skin score showed a reduced endothelin 1 Type A receptor (ETAR)/ETBR ratio. PMID: 26773103 High ETAR expression is associated with ovarian carcinoma. PMID: 26675258 Data show that macitentan interferes with the profibrotic action of transforming growth factor-beta (TGF-beta), blocking the endothelin receptor type A (ET-1 receptor) portion of the ET-1/TGF-beta receptor complex. PMID: 26357964 Ednra, encoding Endothelin receptor A (ETA)-the target of Endothelin 1 (ET-1)-was significantly increased in Systemic Capillary Leak Syndrome blood-outgrowth endothelial cells compared to healthy controls. PMID: 26176954 Genebased analyses revealed associations of the EDNRA gene with longitudinal Blood Pressure phenotypes, associations with essential hypertension, Blood Pressure salt sensitivity, preeclampsia, or preclinical stages of atherosclerosis. PMID: 25424718 Endothelin receptor A was detected in all patients with squamous cell carcinoma and psoriasis, with a higher frequency and grade of expression than controls and basal cell carcinoma. PMID: 25946671 The aim was to quantify the density of ETA and ETB receptors in cardiopulmonary tissue from pulmonary arterial hypertension patients and the monocrotaline (MCT) rat. PMID: 24582810 findings suggest a role for agonistic autoantibodies-induced activation of immune cells mediated by the AT1R and the ETAR in the pathogenesis or even the onset of systemic sclerosis PMID: 24612997 Polymorphisms of EDNRA have been associated with the development of group I pulmonary hypertension, dilated cardiomyopathy and essential hypertension PMID: 24570333 Mutations in the endothelin receptor type A cause mandibulofacial dysostosis with alopecia. PMID: 25772936 significant single nucleotide polymorphism associations with birth weight near coding regions for two genes involved in oxygen sensing and vascular control, PRKAA1 and EDNRA, respectively, were identified. PMID: 25225183 no significant association between EDNRA (C+70G, G-231A) allele and Hashimoto's thyroiditis in Turkish population; this polymorphism relates to decreased risk for early disease onset PMID: 24815860 Data show that upon endothelin-1 (ET-1) stimulation, ET type A receptor (ETAR) is recycled back to plasma membrane, whereas ET type B receptor (ETAR) is targeted to lysosome for degradation. PMID: 25381251 Suggest a functional link between endothelin receptor autoantibody formation and down-regulated midkine serum levels, that may be relevant in the pathogenesis of clinically relevant peripheral artery occlusive disease. PMID: 25056169 genetic association study in population in India: Data suggest that (in addition to mutations in cystic fibrosis transmembrane conductance regulator) an SNP in EDNRA (rs5335) is associated with congenital absence of vas deferens in population studied. PMID: 24958810 our findings reveal the existence of a novel mechanism by which ETAR/beta-arr1 signaling is integrated with the Wnt/beta-catenin pathway to sustain chemoresistance in epithelial ovarian cancer, and they offer a solid rationale for clinical evaluation PMID: 25377471 no association between Graves' disease and genetic polymorphism PMID: 24291390 EDNRA mRNA expression was increased in reflux esophagitis and Barrett's esophagus compared to controls. PMID: 23384184 ETAR and CXCR4 expression levels are potential prognostic biomarkers in nasopharyngeal carcinoma patients. PMID: 23987636 Mutation of EDNRA is involved in ACTH-independent macronodular adrenal hyperplasia. PMID: 23754170 We used this sample of 250 surgical patients to describe the distribution of ET-1, ETA and ETB polymorphisms in the aneurysmal subarachnoid hemorrhage population. PMID: 22997346 ETAR overexpression promoted colon cancer liver metastases. PMID: 23818293 Report serum levels ETAR autoantibodies in peripheral arterial disease. PMID: 24627317 the positive correlation between ET-1 and ETAR in lesional compared with perilesional normal epidermis suggest an important role of this receptor in vitiligo. PMID: 23683481 Desensitization and internalization of endothelin receptor A: impact of G protein-coupled receptor kinase 2 (GRK2)-mediated phosphorylation. PMID: 24064210 The presence ETr-A and ETr-B in rheumatic mitral valves suggests its interaction with the system of c endothelins, particularly ETr-B detected in a greater proportion, which could explain the lack of expression of endothelin in rheumatic mitral valve. PMID: 23515723 Genetic deletion of a nephron-specific endothelin A receptor causes very modest fluid retention that does not alter arterial pressure, nor doea it play a major role in regulating sodium excretion or systemic hemodynamics. PMID: 23217151 The mRNA expressions of endothelin A and B receptors and endothelin-1 are significantly increased in failed Fontan patients. PMID: 21356562 A significant difference existed between migraineurs & controls with AA genotype vs. AG+GG. Pooled relative risk with fixed effect was 4.04. This meta-analysis suggests a significant association between EDNRA -231G>A polymorphism and migraine. PMID: 23058564 Right ventricular hypertrophy myocardial endothelin type A receptor level is increased compared to nonhypertrophied right ventricular endothelin receptor level. PMID: 23233754 Findings suggest a potential link between specific genotypes in the ednra gene and susceptibility to pulmonary arterial hypertension. PMID: 21773759 Both endothelin A and B receptors were reduced in pulmonary arterial hypertension, particularly type B, and type B signaling through protein kinases was markedly reduced in vascular smooth cells with a mutation in bone morphogenetic protein receptor 2. PMID: 22688668 endothelin A receptor and epidermal growth factor receptor signaling converge on beta-catenin to promote ovarian cancer metastasis PMID: 22480520 ETB receptors predominated in normal human liver and displayed the highest ratio (ETB:ETA 63:47) compared with other peripheral tissues; liver ETB expression was upregulated in cirrhosis (ETB:ETA 83:17) PMID: 22365955 Expressed recombinant ET(A) as a fusion protein with phi6 p9 envelope protein. The purified protein showed specific binding to ET-1 and the alpha subunit of G(q) protein. PMID: 22561246 SNP, rs6842241, near EDNRA at chromosome 4q31.22 (combined P-value = 9.58 x 10(-9); odds ratio = 1.25), was found to be significantly associated with intracranial aneurysm PMID: 22286173 Data show that optical imaging with a fluorescent ET(A)R tracer allows the noninvasive imaging of tumor-associated ET(A)R expression in vivo. PMID: 22510270

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Proteins are sensitive to heat, and freeze-drying can preserve the activity of the majority of proteins. It improves protein stability, extends storage time, and reduces shipping costs. However, freeze-drying can also lead to the loss of the active portion of the protein and cause aggregation and denaturation issues. Nonetheless, these adverse effects can be minimized by incorporating protective agents such as stabilizers, additives, and excipients, and by carefully controlling various lyophilization conditions.

Commonly used protectant include saccharides, polyols, polymers, surfactants, some proteins and amino acids etc. We usually add 8% (mass ratio by volume) of trehalose and mannitol as lyoprotectant. Trehalose can significantly prevent the alter of the protein secondary structure, the extension and aggregation of proteins during freeze-drying process; mannitol is also a universal applied protectant and fillers, which can reduce the aggregation of certain proteins after lyophilization.

Our protein products do not contain carrier protein or other additives (such as bovine serum albumin (BSA), human serum albumin (HSA) and sucrose, etc., and when lyophilized with the solution with the lowest salt content, they often cannot form A white grid structure, but a small amount of protein is deposited in the tube during the freeze-drying process, forming a thin or invisible transparent protein layer.

Reminder: Before opening the tube cap, we recommend that you quickly centrifuge for 20-30 seconds in a small centrifuge, so that the protein attached to the tube cap or the tube wall can be aggregated at the bottom of the tube. Our quality control procedures ensure that each tube contains the correct amount of protein, and although sometimes you can't see the protein powder, the amount of protein in the tube is still very precise.

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