Genomes and Genes
endothelin a receptor
Summary: A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.
- He G, Liu M, Yang Q, Furnary A, Yim A. Role of endothelin-1 receptor antagonists in vasoconstriction mediated by endothelin and other vasoconstrictors in human internal mammary artery. Ann Thorac Surg. 2007;84:1522-7 pubmed..We studied the role of antagonists for both ET(A) and ET(B) receptors in vasoconstriction mediated by endothelin-1 and other vasoconstrictors in the human internal mammary artery (IMA)...
- Meens M, Fazzi G, van Zandvoort M, De Mey J. Calcitonin gene-related peptide selectively relaxes contractile responses to endothelin-1 in rat mesenteric resistance arteries. J Pharmacol Exp Ther. 2009;331:87-95 pubmed publisher..This does not involve NO, cAMP, or ATP-sensitive K(+) channels. ..
- Yoo K, Yim H, Jang G, Bae I, Choi B, Hong Y, et al. Endothelin A receptor blockade influences apoptosis and cellular proliferation in the developing rat kidney. J Korean Med Sci. 2009;24:138-45 pubmed publisher..Newborn rat pups were treated with either Bristol-Myers Squibb-182874 (30 mg/kg/day), a selective endothelin A receptor (ET(A)R) antagonist, or vehicle for 7 days...
- Nilsson D, Gustafsson L, Wackenfors A, Gesslein B, Edvinsson L, Paulsson P, et al. Up-regulation of endothelin type B receptors in the human internal mammary artery in culture is dependent on protein kinase C and mitogen-activated kinase signaling pathways. BMC Cardiovasc Disord. 2008;8:21 pubmed publisher..Inhibiting these intracellular signal transduction pathways may provide a future therapeutic target for hindering the development of vascular endothelin ETB receptor changes in cardiovascular disease. ..
- Halcox J, Nour K, Zalos G, Quyyumi A. Endogenous endothelin in human coronary vascular function: differential contribution of endothelin receptor types A and B. Hypertension. 2007;49:1134-41 pubmed..Our data suggest that selective ET(A) blockade may have greater therapeutic potential than nonselective agents, particularly for treatment of endothelial dysfunction in atherosclerosis. ..
- Lättig J, Oksche A, Beyermann M, Rosenthal W, Krause G. Structural determinants for selective recognition of peptide ligands for endothelin receptor subtypes ETA and ETB. J Pept Sci. 2009;15:479-91 pubmed publisher..A narrow tunnel shape in ET(A) is restrictive for a selected group of peptide ligands' N-termini, whereas a broad funnel-shaped entrance in ET(B) accepts a variety of different shapes and properties of ligands. ..
- Su W, Dai D, Liu H, Na T, Dai Y. Upregulated endothelin system in diabetic vascular dysfunction and early retinopathy is reversed by CPU0213 and total triterpene acids from Fructus Corni. Clin Exp Pharmacol Physiol. 2007;34:1228-33 pubmed..Total triterpene acid, in terms of pharmacological properties resembling the endothelin receptor antagonist CPU0213, is effective in normalizing expression of the ET system and iNOS in early diabetic retinopathy and vasculaopathy...
- Plant T, Zöllner C, Kepura F, Mousa S, Eichhorst J, Schaefer M, et al. Endothelin potentiates TRPV1 via ETA receptor-mediated activation of protein kinase C. Mol Pain. 2007;3:35 pubmed..We conclude that ET-1 potentiates TRPV1 by a PKC-dependent mechanism and that this could play a major role in the algogenic and hyperalgesic effects of ET-1 described in previous studies. ..
- Cui B, Cheng Y, Dai D, Li N, Zhang T, Dai Y. CPU0213, a non-selective ETA/ETB receptor antagonist, improves pulmonary arteriolar remodeling of monocrotaline-induced pulmonary hypertension in rats. Clin Exp Pharmacol Physiol. 2009;36:169-75 pubmed publisher..Furthermore, CPU0213 may have promise in treating PH secondary to connective tissue disease. ..
- An S, Boyd R, Zhu M, Chapman A, Pimentel D, Wang H. NADPH oxidase mediates angiotensin II-induced endothelin-1 expression in vascular adventitial fibroblasts. Cardiovasc Res. 2007;75:702-9 pubmed..Functionally, this mechanism stimulates collagen expression thereby implicating the adventitia as a potential contributor to the vascular pathophysiology associated with oxidative stress and vascular remodeling. ..
- James N, Caty A, Payne H, Borre M, Zonnenberg B, Beuzeboc P, et al. Final safety and efficacy analysis of the specific endothelin A receptor antagonist zibotentan (ZD4054) in patients with metastatic castration-resistant prostate cancer and bone metastases who were pain-free or mildly symptomatic for pain: a double-b. BJU Int. 2010;106:966-73 pubmed publisher..To report the final analysis of a Phase II trial, which investigated the safety and efficacy of the specific endothelin A receptor antagonist zibotentan (AstraZeneca, Macclesfield, UK) in patients with metastatic castration-resistant ..
- Nilsson D, Wackenfors A, Gustafsson L, Edvinsson L, Paulsson P, Ingemansson R, et al. Increased ET(A) and ET(B) receptor contraction in the left internal mammary artery from patients with hypertension. J Hum Hypertens. 2008;22:226-9 pubmed
- Nilsson D, Wackenfors A, Gustafsson L, Ugander M, Paulsson P, Ingemansson R, et al. Endothelin receptor-mediated vasodilatation: effects of organ culture. Eur J Pharmacol. 2008;579:233-40 pubmed..Down-regulation of endothelial endothelin ET(B) receptors may in part explain the increased endothelin ET(B) receptor-mediated vasoconstriction frequently studied in organ culture. ..
- Xu J, Li N, Dai D, Yu F, Dai Y. The endothelin receptor antagonist CPU0213 is more effective than aminoguanidine to attenuate isoproterenol-induced vascular abnormality by suppressing overexpression of NADPH oxidase [correction of oxidas], ETA, ETB, and MMP9 in the vasculature. J Cardiovasc Pharmacol. 2008;52:42-8 pubmed publisher
- Settergren M, Pernow J, Brismar K, Jörneskog G, Kalani M. Endothelin-A receptor blockade increases nutritive skin capillary circulation in patients with type 2 diabetes and microangiopathy. J Vasc Res. 2008;45:295-302 pubmed publisher..There were no significant changes in LDF parameters during infusion of BQ123 in either group. ET(A) receptor blockade improves nutritive skin capillary circulation in patients with type 2 diabetes and microangiopathy. ..
- Rao V, Krishnamoorthy R, Yorio T. Endothelin-1, endothelin A and B receptor expression and their pharmacological properties in GFAP negative human lamina cribrosa cells. Exp Eye Res. 2007;84:1115-24 pubmed..This may have an implication in the normal physiology of LC cells and in POAG subjects where elevated levels of ET-1 could impact LC function. ..
- Miyamoto Y, Yamauchi J, Mizuno N, Itoh H. The adaptor protein Nck1 mediates endothelin A receptor-regulated cell migration through the Cdc42-dependent c-Jun N-terminal kinase pathway. J Biol Chem. 2004;279:34336-42 pubmed..Nck1, but not Grb2 or CrkII, mediated the inhibition of cell migration induced by the endothelin-1 and endothelin A receptor. The small interference RNA and dominant negative mutants of Nck1 diminished the endothelin-1-induced ..
- Granström B, Xu C, Nilsson E, Bengtsson U, Edvinsson L. Up-regulation of endothelin receptor function and mRNA expression in airway smooth muscle cells following Sephadex-induced airway inflammation. Basic Clin Pharmacol Toxicol. 2004;95:43-8 pubmed
- Henriksson M, Xu C, Edvinsson L. Importance of ERK1/2 in upregulation of endothelin type B receptors in cerebral arteries. Br J Pharmacol. 2004;142:1155-61 pubmed..Since there is a similar upregulation in models of focal ischaemia and subarachnoid haemorrhage, this may be an important pathophysiological event. ..
- Isaka M, Kudo A, Imamura M, Kawakami H, Yasuda K. Endothelin receptors, localized in sympathetic nerve terminals of the heart, modulate norepinephrine release and reperfusion arrhythmias. Basic Res Cardiol. 2007;102:154-62 pubmed..These studies provide the first evidence that both ETA and ETB receptors, located in the sympathetic nerve varicosities, modulate NE release, at least in part, in association with reperfusion arrhythmias. ..
- Mitchell A, Lückebergfeld B, Bührmann S, Rushentsova U, Nürnberger J, Siffert W, et al. Effects of systemic endothelin A receptor antagonism in various vascular beds in men: in vivo interactions of the major blood pressure-regulating systems and associations with the GNB3 C825T polymorphism. Clin Pharmacol Ther. 2004;76:396-408 pubmed
- Palmes D, Skawran S, Stratmann U, Armann B, Minin E, Herbst H, et al. Amelioration of microcirculatory damage by an endothelin A receptor antagonist in a rat model of reversible acute liver failure. J Hepatol. 2005;42:350-7 pubmed..We studied a selective endothelin A receptor (ETAR) antagonist for its potential influence on the microcirculation in the setting of ALF...
- Barst R, Langleben D, Badesch D, Frost A, Lawrence E, Shapiro S, et al. Treatment of pulmonary arterial hypertension with the selective endothelin-A receptor antagonist sitaxsentan. J Am Coll Cardiol. 2006;47:2049-56 pubmed..Treatment with the selective ET(A) receptor antagonist sitaxsentan, orally once daily at a dose of 100 mg, improves exercise capacity and WHO FC in PAH patients, with a low incidence of hepatic toxicity. ..
- Wang Y, Wang D. Prevention of endothelin-1-induced increases in blood pressure: role of endogenous CGRP. Am J Physiol Heart Circ Physiol. 2004;287:H1868-74 pubmed..3 +/- 0.2) groups. Therefore, our data show that ET-1 infusion leads to increased CGRP release via activation of the ET(A) receptor, which plays a compensatory role in preventing ET-1-induced elevation in blood pressure. ..
- Yamamoto H, Kawamata T, Ninomiya T, Omote K, Namiki A. Endothelin-1 enhances capsaicin-evoked intracellular Ca2+ response via activation of endothelin a receptor in a protein kinase Cepsilon-dependent manner in dorsal root ganglion neurons. Neuroscience. 2006;137:949-60 pubmed..6+/-11.6 nM to 414.8+/-62.3 nM (71 of 156 neurons). The inhibition of endothelin A receptor (BQ-123) significantly suppressed the enhancing effect of endothelin-1...
- Forni M, Mazzola S, Ribeiro L, Pirrone F, Zannoni A, Bernardini C, et al. Expression of endothelin-1 system in a pig model of endotoxic shock. Regul Pept. 2005;131:89-96 pubmed
- Kuklin V, Kirov M, Sovershaev M, Andreasen T, Ingebretsen O, Ytrehus K, et al. Tezosentan-induced attenuation of lung injury in endotoxemic sheep is associated with reduced activation of protein kinase C. Crit Care. 2005;9:R211-7 pubmed..In endotoxemic sheep, ET-1 receptor blockade alleviates lung injury as assessed by a decrease in EVLWI paralleled by a reduction in Pmo and the prevention of activation of PKC-alpha. ..
- Bohm F, Settergren M, Gonon A, Pernow J. The endothelin-1 receptor antagonist bosentan protects against ischaemia/reperfusion-induced endothelial dysfunction in humans. Clin Sci (Lond). 2005;108:357-63 pubmed..Bosentan may thus be a feasible therapeutic agent in the treatment of ischaemia/reperfusion injury in humans. ..
- Denton C, Humbert M, Rubin L, Black C. Bosentan treatment for pulmonary arterial hypertension related to connective tissue disease: a subgroup analysis of the pivotal clinical trials and their open-label extensions. Ann Rheum Dis. 2006;65:1336-40 pubmed..The long-term follow-up of these patients suggests that first-line bosentan, with the subsequent addition of other PAH treatments if required, is safe for long-term treatment and may have a positive effect on outcome. ..
- Plant T, Zöllner C, Mousa S, Oksche A. Endothelin-1 potentiates capsaicin-induced TRPV1 currents via the endothelin A receptor. Exp Biol Med (Maywood). 2006;231:1161-4 pubmed..Thus, ET(A) receptor antagonists may be of importance in painful states with increased circulating ET-1 levels, as found in cancer and in chronic inflammation. ..
- Schneider M, Boesen E, Pollock D. Contrasting actions of endothelin ET(A) and ET(B) receptors in cardiovascular disease. Annu Rev Pharmacol Toxicol. 2007;47:731-59 pubmed..Considerable questions remain regarding whether ET(A)-selective or nonselective ET(A)/ET(B) receptor antagonists would be useful in a range of clinical settings. ..
- Ge Y, Stricklett P, Hughes A, Yanagisawa M, Kohan D. Collecting duct-specific knockout of the endothelin A receptor alters renal vasopressin responsiveness, but not sodium excretion or blood pressure. Am J Physiol Renal Physiol. 2005;289:F692-8 pubmed..Furthermore, the CD ET(A) receptor does not appear to be involved in modulation of systemic blood pressure or renal Na excretion under physiological conditions. ..
- Zhang Y, Adner M, Cardell L. Interleukin-1beta attenuates endothelin B receptor-mediated airway contractions in a murine in vitro model of asthma: roles of endothelin converting enzyme and mitogen-activated protein kinase pathways. Clin Exp Allergy. 2004;34:1480-7 pubmed..Presence of IL-1beta in the airways attenuate the contractile response mediated via ETB receptors, an effect dependent on ECE, JNK and ERK 1/2 pathways. ..
- Balonov K, Khodorova A, Strichartz G. Tactile allodynia initiated by local subcutaneous endothelin-1 is prolonged by activation of TRPV-1 receptors. Exp Biol Med (Maywood). 2006;231:1165-70 pubmed
- Naidoo V, Naidoo S, Mahabeer R, Raidoo D. Localization of the endothelin system in human diffuse astrocytomas. Cancer. 2005;104:1049-57 pubmed..The mitogenic and antiapoptotic properties of ET-1, as well as the vasodilatory signaling of ETB receptors, may promote tumorigenesis. ..
- Zemanova L, Schenk A, Hunt N, Nienhaus G, Heilker R. Endothelin receptor in virus-like particles: ligand binding observed by fluorescence fluctuation spectroscopy. Biochemistry. 2004;43:9021-8 pubmed..we have studied the binding of tetramethylrhodamine-labeled endothelin-1 (TMR-ET-1) to VLiP-integrated endothelin A receptor (ET(A)R) by fluorescence fluctuation spectroscopy...
- Gregan B, Jürgensen J, Papsdorf G, Furkert J, Schaefer M, Beyermann M, et al. Ligand-dependent differences in the internalization of endothelin A and endothelin B receptor heterodimers. J Biol Chem. 2004;279:27679-87 pubmed..Heterodimer dissociation along the endocytic pathway only occurs upon ET(B)-selective stimulation. ..
- Bhalla S, Zhang Z, Patterson N, Gulati A. Effect of endothelin-A receptor antagonist on mu, delta and kappa opioid receptor-mediated antinociception in mice. Eur J Pharmacol. 2010;635:62-71 pubmed publisher..Therefore, endothelin ET(A) receptor antagonists could be useful in the restoration of antinociceptive effect during tolerance to opiates. ..
- Ameri P, Bertero E, Meliota G, Cheli M, Canepa M, Brunelli C, et al. Neurohormonal activation and pharmacological inhibition in pulmonary arterial hypertension and related right ventricular failure. Heart Fail Rev. 2016;21:539-47 pubmed publisher..While neurohormonal inhibitors cannot be recommended at present for treatment of PAH and PAH-RVF, they are worth being further investigated. ..
- Sprogar S, Vaupotic T, Cor A, Drevensek M, Drevensek G. The endothelin system mediates bone modeling in the late stage of orthodontic tooth movement in rats. Bone. 2008;43:740-7 pubmed publisher..These data suggest that ET-1 increases osteoclastic bone resorption via ET(A) in the late stage of OTM. ..
- Lu Y, Wang C, Zhou L, Chen Y, Su S, Feng Y, et al. Synthesis of platelet-activating factor and its receptor expression in Kupffer cells in rat carbon tetrachloride-induced cirrhosis. World J Gastroenterol. 2008;14:764-70 pubmed..ETA receptor did not appear in activated Kupffer cells, which may exacerbate the hepatic and extrahepatic complications of cirrhosis. ..
- Sultana N, Nag K, Kato A, Hirose S. Pillar cell and erythrocyte localization of fugu ET(A) receptor and its implication. Biochem Biophys Res Commun. 2007;355:149-55 pubmed..Immunohistochemistry revealed its pillar cell and erythrocyte localization. These results suggest an endothelin/ET(A)-mediated coordinated regulation of the pillar cell shape and erythrocyte membrane flexibility. ..
- Gholam P, Sehr T, Enk A, Hartmann M. Successful treatment of systemic-sclerosis-related digital ulcers with a selective endothelin type A receptor antagonist (sitaxentan). Dermatology. 2009;219:171-3 pubmed publisher..During the 6 months of treatment, we noticed a remarkable decrease in pain, a nearly complete healing of the preexistent ulcers and no development of new ulcers. No side effects were noted. ..
- Nair S, Li W, Cornell R, Schilling T. Requirements for Endothelin type-A receptors and Endothelin-1 signaling in the facial ectoderm for the patterning of skeletogenic neural crest cells in zebrafish. Development. 2007;134:335-45 pubmed..Collectively, our results indicate that Edn1 from the pharyngeal ectoderm signals through Ednra proteins to direct early dorsoventral patterning of the skeletogenic neural crest. ..
- Gabbay E, Reed A, Williams T. Assessment and treatment of pulmonary arterial hypertension: an Australian perspective in 2006. Intern Med J. 2007;37:38-48 pubmed..These new approaches to therapy are already substantially improving quality of life and prognosis. ..
- Thijssen D, Rongen G, van Dijk A, Smits P, Hopman M. Enhanced endothelin-1-mediated leg vascular tone in healthy older subjects. J Appl Physiol (1985). 2007;103:852-7 pubmed..the increased baseline vascular tone in aging is at least in part mediated by the endothelin. Eight-weeks cycling training in older sedentary men decreased leg vascular tone and seems to partly decrease the ET-1-mediated vascular tone. ..
- Ruest L, Clouthier D. Elucidating timing and function of endothelin-A receptor signaling during craniofacial development using neural crest cell-specific gene deletion and receptor antagonism. Dev Biol. 2009;328:94-108 pubmed publisher..These observations suggest that the advent of Ednra signaling in cranial NCCs may have been a crucial event in the evolution of the mammalian middle ear ossicles. ..
- Chen Y, Hanaoka M, Droma Y, Chen P, Voelkel N, Kubo K. Endothelin-1 receptor antagonists prevent the development of pulmonary emphysema in rats. Eur Respir J. 2010;35:904-12 pubmed publisher..ET-1 may cause emphysematous changes through molecular pathogenesis pathways involving apoptosis, proteinase and antiproteinase imbalance, inflammation and oxidative stress. ..