Endothelins. Medical search

21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.

A 21-amino acid peptide produced predominantly within the kidney and intestine, with smaller amounts produced in the myocardium, placenta, and uterus, but the cells of origin are not clear. Endothelin-2 has no unique physiologic functions, as compared with endothelin-1. (N Eng J Med 1995;333(6):356-63)

A 21-amino acid peptide that circulates in the plasma, but its source is not known. Endothelin-3 has been found in high concentrations in the brain and may regulate important functions in neurons and astrocytes, such as proliferation and development. It also is found throughout the gastrointestinal tract and in the lung and kidney. (N Eng J Med 1995;333(6):356-63)

Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.

A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.

A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)

Venoms from SNAKES of the viperid family. They tend to be less toxic than elapid or hydrophid venoms and act mainly on the vascular system, interfering with coagulation and capillary membrane integrity and are highly cytotoxic. They contain large amounts of several enzymes, other factors, and some toxins.

A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.

Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).

Rapidly decreasing response to a drug or physiologically active agent after administration of a few doses. In immunology, it is the rapid immunization against the effect of toxic doses of an extract or serum by previous injection of small doses. (Dorland, 28th ed)

Enzyme that is a major constituent of kidney brush-border membranes and is also present to a lesser degree in the brain and other tissues. It preferentially catalyzes cleavage at the amino group of hydrophobic residues of the B-chain of insulin as well as opioid peptides and other biologically active peptides. The enzyme is inhibited primarily by EDTA, phosphoramidon, and thiorphan and is reactivated by zinc. Neprilysin is identical to common acute lymphoblastic leukemia antigen (CALLA Antigen), an important marker in the diagnosis of human acute lymphocytic leukemia. There is no relationship with CALLA PLANT.

A sub-subclass of endopeptidases that depend on an ASPARTIC ACID residue for their activity.

A group of compounds that contain the structure SO2NH2.

Drugs that act on adrenergic receptors or affect the life cycle of adrenergic transmitters. Included here are adrenergic agonists and antagonists and agents that affect the synthesis, storage, uptake, metabolism, or release of adrenergic transmitters.

ENDOPEPTIDASES which use a metal such as ZINC in the catalytic mechanism.

Drugs used to cause constriction of the blood vessels.

A family of hexahydropyridines.

Poly-2-methylpropenoic acids. Used in the manufacture of methacrylate resins and plastics in the form of pellets and granules, as absorbent for biological materials and as filters; also as biological membranes and as hydrogens. Synonyms: methylacrylate polymer; poly(methylacrylate); acrylic acid methyl ester polymer.

Proteins which contain carbohydrate groups attached covalently to the polypeptide chain. The protein moiety is the predominant group with the carbohydrate making up only a small percentage of the total weight.

Peptides composed of between two and twelve amino acids.

The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.

A thermostable extracellular metalloendopeptidase containing four calcium ions. (Enzyme Nomenclature, 1992) 3.4.24.27.

Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.

Single pavement layer of cells which line the luminal surface of the entire vascular system and regulate the transport of macromolecules and blood components.

A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.

A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.

Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)

A free radical gas produced endogenously by a variety of mammalian cells, synthesized from ARGININE by NITRIC OXIDE SYNTHASE. Nitric oxide is one of the ENDOTHELIUM-DEPENDENT RELAXING FACTORS released by the vascular endothelium and mediates VASODILATION. It also inhibits platelet aggregation, induces disaggregation of aggregated platelets, and inhibits platelet adhesion to the vascular endothelium. Nitric oxide activates cytosolic GUANYLATE CYCLASE and thus elevates intracellular levels of CYCLIC GMP.

RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.

Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are linear polypeptides that are normally synthesized on RIBOSOMES.

Body organ that filters blood for the secretion of URINE and that regulates ion concentrations.

A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.

Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.

Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.

The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.

The relationship between the dose of an administered drug and the response of the organism to the drug.

Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.

The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.

PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.

Inhibition of in vitro enteric neuronal development by endothelin-3: mediation by endothelin B receptors. (1/1796)

The terminal colon is aganglionic in mice lacking endothelin-3 or its receptor, endothelin B. To analyze the effects of endothelin-3/endothelin B on the differentiation of enteric neurons, E11-13 mouse gut was dissociated, and positive and negative immunoselection with antibodies to p75(NTR )were used to isolate neural crest- and non-crest-derived cells. mRNA encoding endothelin B was present in both the crest-and non-crest-derived cells, but that encoding preproendothelin-3 was detected only in the non-crest-derived population. The crest- and non-crest-derived cells were exposed in vitro to endothelin-3, IRL 1620 (an endothelin B agonist), and/or BQ 788 (an endothelin B antagonist). Neurons and glia developed only in cultures of crest-derived cells, and did so even when endothelin-3 was absent and BQ 788 was present. Endothelin-3 inhibited neuronal development, an effect that was mimicked by IRL 1620 and blocked by BQ 788. Endothelin-3 failed to stimulate the incorporation of [3H]thymidine or bromodeoxyuridine. Smooth muscle development in non-crest-derived cell cultures was promoted by endothelin-3 and inhibited by BQ 788. In contrast, transcription of laminin alpha1, a smooth muscle-derived promoter of neuronal development, was inhibited by endothelin-3, but promoted by BQ 788. Neurons did not develop in explants of the terminal bowel of E12 ls/ls (endothelin-3-deficient) mice, but could be induced to do so by endothelin-3 if a source of neural precursors was present. We suggest that endothelin-3/endothelin B normally prevents the premature differentiation of crest-derived precursors migrating to and within the fetal bowel, enabling the precursor population to persist long enough to finish colonizing the bowel. (+info)

Endogenous plasma endothelin concentrations and coronary circulation in patients with mild dilated cardiomyopathy. (2/1796)

OBJECTIVE: To determine whether increased plasma concentrations of endothelin-1 (ET-1) and big endothelin (BET) play a role in the regulation of coronary circulation in patients with idiopathic dilated cardiomyopathy (IDCM). SETTING: Tertiary referral centre for cardiac diseases. PATIENTS: Fourteen patients (eight male/six female; mean (SD) age 59 (9) years) with IDCM (ejection fraction 36 (9)%) and five normotensive subjects (two male/three female; age 52 (7) years) serving as controls were studied. METHODS: Functional status was classified according to New York Heart Association (NYHA) class. Endogenous ET-1 and BET plasma concentrations from the aorta and the coronary sinus were determined by radioimmunoassay. Coronary blood flow, using the inert chromatographic argon method, myocardial oxygen consumption, and coronary sinus oxygen content under basal conditions were determined. RESULTS: In the aorta, mean (SD) concentrations of ET-1 (IDCM 0.76 (0.25) v controls 0.31 (0.06) fmol/ml; p = 0.002) and BET (IDCM 3.58 (1.06) v controls 2.11 (0.58) fmol/ml; p = 0.014) were increased in patients with IDCM. Aortic ET-1 concentrations correlated positively with NYHA class (r = 0. 731; p < 0.001), myocardial oxygen consumption (r = 0.749; p < 0. 001), and coronary blood flow (r = 0.645; p = 0.003), but inversely with coronary sinus oxygen content (r = -0.633; p = 0.004), which was significantly decreased in IDCM patients (IDCM 4.68 (1.05) v controls 6.70 (1.06) vol%; p = 0.003). CONCLUSIONS: The coronary circulation in patients with IDCM is exposed to an increased endothelin load. ET-1 concentrations correlate with functional deterioration. A decrease of the coronary sinus content of oxygen suggests a mismatch between coronary blood flow and metabolic demand. Thus, ET-1 might be a marker of a disequilibrium between myocardial oxygen demand and coronary blood flow in IDCM. (+info)

Endothelin up-regulation and localization following renal ischemia and reperfusion. (3/1796)

BACKGROUND: Endothelin (ET), a potent vasoconstrictor, is known to play a role in ischemic acute renal failure. Although preproET-1 (ppET-1) mRNA is known to be up-regulated following ischemia/reperfusion injury, it has not been determined which component of the injury (ischemia or reperfusion) leads to initial gene up-regulation. Likewise, although ET-1 peptide expression has been localized in the normal kidney, its expression pattern in the ischemic kidney has not been determined. Therefore, the purpose of this study was twofold: (a) to determine whether ischemia alone or ischemia plus reperfusion is required for the up-regulation of ppET-1 mRNA to occur, and (b) to localize ET-1 peptide expression following ischemia in the rat kidney to clarify better the role of ET in the pathophysiology of ischemia-induced acute renal failure. METHODS: Male Lewis rats underwent clamping of the right renal vascular pedicle for either 30 minutes of ischemia (group 1), 60 minutes of ischemia (group 2), 30 minutes of ischemia followed by 30 minutes of reperfusion (group 3), or 60 minutes of ischemia followed by three hours of reperfusion (group 4). The contralateral kidney acted as a control. ppET-1 mRNA up-regulation and ET-1 peptide expression were examined using the reverse transcription-polymerase chain reaction and immunohistochemistry, respectively. RESULTS: Reverse transcription-polymerase chain reaction yielded a control (nonischemic) value of 0.6 +/- 0.2 densitometric units (DU) of ppET-1 mRNA in the kidney. Group 1 levels (30 min of ischemia alone) were 1.8 +/- 0.4 DU, a threefold increase (P < 0.05). Group 2 levels (60 min of ischemia alone) increased almost six times above baseline, 3.5 +/- 0.2 DU (P < 0.01), whereas both group 3 and group 4 (ischemia plus reperfusion) did not experience any further significant increases in mRNA levels (1.9 +/- 0.4 DU and 2.8 +/- 0.6 DU, respectively) beyond levels in group 1 or 2 animals subjected to similar ischemic periods. ET-1 peptide expression in the ischemic kidneys was significantly increased over controls and was clearly localized to the endothelium of the peritubular capillary network of the kidney. CONCLUSIONS: Initial ET-1 gene up-regulation in the kidney occurs secondary to ischemia, but reperfusion most likely contributes to sustaining this up-regulation. The marked increase of ET-1 in the peritubular capillary network suggests that ET-induced vasoconstriction may have a pathophysiological role in ischemic acute tubular necrosis. (+info)

Nitric oxide limits the eicosanoid-dependent bronchoconstriction and hypotension induced by endothelin-1 in the guinea-pig. (4/1796)

1. This study attempts to investigate if endogenous nitric oxide (NO) can modulate the eicosanoid-releasing properties of intravenously administered endothelin-1 (ET-1) in the pulmonary and circulatory systems in the guinea-pig. 2. The nitric oxide synthase blocker N(omega)-nitro-L-arginine methyl ester (L-NAME; 300 microM; 30 min infusion) potentiated, in an L-arginine sensitive fashion, the release of thromboxane A2 (TxA2) stimulated by ET-1, the selective ET(B) receptor agonist IRL 1620 (Suc-[Glu9,Ala11,15]-ET-1(8-21)) or bradykinin (BK) (5, 50 and 50 nM, respectively, 3 min infusion) in guinea-pig isolated and perfused lungs. 3. In anaesthetized and ventilated guinea-pigs intravenous injection of ET-1 (0.1-1.0 nmol kg(-1)), IRL 1620 (0.2-1.6 nmol kg(-1)), BK (1.0-10.0 nmol kg(-1)) or U 46619 (0.2-5.7 nmol kg(-1)) each induced dose-dependent increases in pulmonary insufflation pressure (PIP). Pretreatment with L-NAME (5 mg kg(-1)) did not change basal PIP, but increased, in L-arginine sensitive manner, the magnitude of the PIP increases (in both amplitude and duration) triggered by each of the peptides (at 0.25, 0.4 and 1.0 nmol kg(-1), respectively), without modifying bronchoconstriction caused by U 46619 (0.57 nmol kg(-1)). 4. The increases in PIP induced by ET-1, IRL 1620 (0.25 and 0.4 nmol kg(-1), respectively) or U 46619 (0.57 nmol kg(-1)) were accompanied by rapid and transient increases of mean arterial blood pressure (MAP). Pretreatment with L-NAME (5 mg kg(-1); i.v. raised basal MAP persistently and, under this condition, subsequent administration of ET-1 or IRL 1620, but not of U-46619, induced hypotensive responses which were prevented by pretreatment with the cyclo-oxygenase inhibitor indomethacin. 5. Thus, endogenous NO appears to modulate ET-1-induced bronchoconstriction and pressor effects in the guinea-pig by limiting the peptide's ability to induce, possibly via ET(B) receptors, the release of TxA2 in the lungs and of vasodilatory prostanoids in the systemic circulation. Furthermore, it would seem that these eicosanoid-dependent actions of ET-1 in the pulmonary system and on systemic arterial resistance in this species are physiologically dissociated. (+info)

Blockade and reversal of endothelin-induced constriction in pial arteries from human brain. (5/1796)

BACKGROUND AND PURPOSE: Substantial evidence now implicates endothelin (ET) in the pathophysiology of cerebrovascular disorders such as the delayed vasospasm associated with subarachnoid hemorrhage and ischemic stroke. We investigated the ET receptor subtypes mediating vasoconstriction in human pial arteries. METHODS: ET receptors on human pial and intracerebral arteries were visualized with the use of autoradiography, and the subtypes mediating vasoconstriction were identified by means of wire myography. RESULTS: ET-1 was more potent than ET-3 as a vasoconstrictor, indicating an ETA-mediated effect. Similarly, the selective ETB agonist sarafotoxin S6c had no effect on contractile action at concentrations up to 30 nmol/L. The nonpeptide ETA receptor antagonist PD156707 (3 to 30 nmol/L) caused a parallel rightward shift of the ET-1-induced response, yielding a pA2 of 9.2. Consistent with these results, PD156707 (30 nmol/L) fully reversed an established constriction in pial arteries induced by 1 nmol/L ET-1, while the selective ETB receptor antagonist BQ788 (1 micromol/L) had little effect. The calcium channel blocker nimodipine (0.3 to 3 micromol/L) significantly attenuated the maximum response to ET-1 in a concentration-dependent manner without changing potency. In agreement with the functional data, specific binding of [125I]PD151242 to ETA receptors was localized to the smooth muscle layer of pial and intracerebral blood vessels. In contrast, little or no [125I]BQ3020 binding to ETB receptors was detected. CONCLUSIONS: These data indicate an important role for ETA receptors in ET-1-induced constriction of human pial arteries and suggest that ETA receptor antagonists may provide additional dilatory benefit in cerebrovascular disorders associated with raised ET levels. (+info)

Endothelin-1 and its mRNA in the wall layers of human arteries ex vivo. (6/1796)

BACKGROUND: The participation of endothelin-1 (ET-1) in the control of vascular tone in humans has been questioned, on the basis of the finding of subthreshold immunoreactive (ir) ET-1 plasma levels. However, because most ET-1 is secreted abluminally, it might attain a higher concentration in the tunica media than in plasma. Furthermore, evidence indicates that vascular smooth muscle cells (VSMCs) can synthesize ET-1 on stimulation in vitro. We therefore looked for irET-1 in the different layers of the wall of human arteries, including renal, gastric, and internal thoracic artery wall, obtained ex vivo from consenting patients with coronary artery disease and/or high blood pressure undergoing surgery, as well as from young organ donors. METHODS AND RESULTS: We performed immunohistochemistry with specific anti-ET-1 and anti-vWF antibodies followed by detection with an avidin-biotin complex ultrasensitive kit. The presence of preproET-1 and human endothelin-converting enzyme-1 (hECE-1) mRNA was also investigated by reverse transcription-polymerase chain reaction in homogenates of vessel wall, including preparations deprived of both endothelium and adventitia, and in isolated VSMCs. We detected irET-1 in the endothelium of all arteries and in the tunica media of internal thoracic artery from most patients with coronary artery disease. PreproET-1 and hECE-1 mRNA was also detected in VSMCs isolated from these vessels. irET-1 and irvWF staining in endothelium and tunica media was measured by use of microscope-coupled computer-assisted technology. Significant correlations between the amount of irET-1 in the tunica media and mean blood pressure (P<0.05), total serum cholesterol (P<0.05), and number of atherosclerotic sites (P<0.001) were found. Thus, in organ donors, irET-1 was detectable almost exclusively in endothelial cells, whereas in patients with coronary artery disease and/or arterial hypertension, sizable amounts of irET-1 were detectable in the tunica media of different types of arteries. In addition, VSMCs isolated from these vessels coexpressed the preproET-1 and hECE-1 genes. CONCLUSIONS: Collectively, these findings are consistent with the contention that endothelial damage occurs in most patients with atherosclerosis and/or hypertension and that ET-1 is synthesized in VSMCs of these patients. (+info)

Effects of hypertension, diabetes mellitus, and hypercholesterolemia on endothelin type B receptor-mediated nitric oxide release from rat kidney. (7/1796)

BACKGROUND: Although endothelin-1 is a potent vasoconstrictor peptide, stimulation of endothelin type B receptor (ETBR) causes bidirectional changes in vascular tone, ie, vasodilation and vasoconstriction. Roles of ETBR in pathological conditions are largely unknown. METHODS AND RESULTS: We studied the effect of BQ-3020, a highly selective ETBR agonist, on renal vascular resistance and nitric oxide (NO) release in the isolated, perfused kidney of rats with hypertension, diabetes mellitus, and hypercholesterolemia. Immunohistochemistry of endothelial NO synthase and ETBR was also examined. Infusion of BQ-3020 at concentrations of +info)

Maintenance of blood pressure in normotensive dogs by endothelin. (8/1796)

The role of endothelin (ET)-1 in blood pressure homeostasis and the interaction with the renin-angiotensin system (RAS) was investigated in normotensive conscious dogs. ETA receptors were blocked by LU-135252 (1-30 mg/kg); trandolapril (2 mg/kg) or losartan (10 mg/kg) was used to inhibit the RAS. LU-135252 in oral doses of 3-30 mg/kg significantly reduced mean arterial pressure (MAP) by approximately 10 mmHg maximally, whereas trandolapril or losartan were without any effect. MAP reduction was more pronounced when LU-135252 was combined with either losartan (-15.5 +/- 3.2 mmHg; 2 h postadministration; P < 0.05) or trandolapril (-30.9 +/- 3.6 mmHg; P < 0.05). When endogenous nitric oxide (NO) generation was blocked but NO concomitantly infused, this synergistic effect on MAP was prevented. The data show that ET-1 contributes to the maintenance of blood pressure via ETA receptors. Furthermore, ET-1 and ANG II play a prominent role in the control of blood pressure by opposing the effects of NO. The pronounced blood pressure fall after combined blockade of ETA receptors and the RAS may be mediated by an enhanced release of NO. (+info)

The human genes for endothelin-1 (ET-1), endothelin-2 (ET-2), and endothelin-3 (ET-3) are located on chromosomes 6, 1, and 20, ... Endothelins are peptides with receptors and effects in many body organs. Endothelin constricts blood vessels and raises blood ... Endothelin-1 is the most powerful endogenous chemical affecting vascular tone across organ systems. Secretion of endothelin-1 ... Endothelins are the most potent vasoconstrictors known. Overproduction of endothelin in the lungs may cause pulmonary ...

https://en.wikipedia.org/wiki/Endothelin

1991). "Chromosomal assignments of the human endothelin family genes: the endothelin-1 gene (EDN1) to 6p23-p24, the endothelin- ... 1993). "Presence of messenger ribonucleic acid for endothelin-1, endothelin-2, and endothelin-3 in human endometrium and a ... 1995). "Interaction of endothelin-3 with endothelin-B receptor is essential for development of epidermal melanocytes and ... The active peptide is a ligand for endothelin receptor type B (EDNRB). The interaction of this endothelin with EDNRB is ...

https://en.wikipedia.org/wiki/Endothelin_3

Barnes K, Turner AJ; Turner (August 1997). "The endothelin system and endothelin-converting enzyme in the brain: molecular and ... 2016) 'Endothelin' Pharmacol. Rev. 68: 357-418. pmid =26956245 doi =10.1124/pr.115.011833 "Endothelin Receptors". IUPHAR ... Endothelin+receptor at the US National Library of Medicine Medical Subject Headings (MeSH) v t e (Articles with short ... There are at least four known endothelin receptors, ETA, ETB1, ETB2 and ETC, all of which are G protein-coupled receptors whose ...

https://en.wikipedia.org/wiki/Endothelin_receptor

The association between endothelins, poor prognosis and invasion suggests the endothelin axis is an interesting therapeutic ... ET-2 acts by binding to two different G-protein coupled receptors (GCPRs), the endothelin A receptor (EDNRA) and the endothelin ... As a strong positive inotrope, endothelin-2 has an impact on the human myocardium and for this reason, endothelin-2 antagonists ... Arjomand-Nahad F, Landt O, Stangl K, Diefenbach K, Roots I (2006). "Fifteen polymorphisms in endothelin-1, endothelin-2 and ...

https://en.wikipedia.org/wiki/Endothelin_2

The protein encoded by this gene - EDN1 - is proteolytically processed to release endothelin 1. Endothelin 1 is one of three ... Endothelin 1 (ET-1), also known as preproendothelin-1 (PPET1), is a potent vasoconstrictor peptide produced by vascular ... Endothelin-1 receptor antagonists (Bosentan) are used in the treatment of pulmonary hypertension. Use of these antagonists ... Overview of all the structural information available in the PDB for UniProt: P05305 (Endothelin-1) at the PDBe-KB. This article ...

https://en.wikipedia.org/wiki/Endothelin_1

An endothelin receptor antagonist (ERA) is a drug that blocks endothelin receptors. Three main kinds of ERAs exist: selective ... Endothelin receptor antagonists v t e (Articles with short description, Short description matches Wikidata, Endothelin receptor ... selective ETB receptor antagonists (BQ-788 and A192621) which affect endothelin B receptors are used in research but have not ... dual antagonists (bosentan, macitentan, tezosentan), which affect both endothelin A and B receptors. ...

https://en.wikipedia.org/wiki/Endothelin_receptor_antagonist

Endothelin receptor type B, also known as ETB is a protein that in humans is encoded by the EDNRB gene. Endothelin receptor ... "Interaction of endothelin-3 with endothelin-B receptor is essential for development of epidermal melanocytes and enteric ... "Entrez Gene: EDNRB endothelin receptor type B". Sato-Jin K, Nishimura EK, Akasaka E, Huber W, Nakano H, Miller A, Du J, Wu M, ... Its ligand, endothelin, consists of a family of three potent vasoactive peptides: ET1, ET2, and ET3. A splice variant, named ...

https://en.wikipedia.org/wiki/Endothelin_B_receptor

Endothelin receptor type A, also known as ETA, is a human G protein-coupled receptor. Endothelin receptor type A has been shown ... Han SG, Ko S, Lee WK, Jung ST, Yu YG (August 2017). "Determination of the endothelin-1 recognition sites of endothelin receptor ... "Entrez Gene: EDNRA endothelin receptor type A". Lee HJ, Chun M, Kandror KV (May 2001). "Tip60 and HDAC7 interact with the ... Lee HJ, Chun M, Kandror KV (May 2001). "Tip60 and HDAC7 interact with the endothelin receptor a and may be involved in ...

https://en.wikipedia.org/wiki/Endothelin_A_receptor

... (EC 3.4.24.71, endothelin-converting enzyme, ECE-1) is an enzyme. This enzyme catalyses the ... bond in big endothelin to form endothelin 1 This metalloendopeptidase belongs to the peptidase family M13. Takahashi M, ... Endothelin-converting+enzyme+1 at the US National Library of Medicine Medical Subject Headings (MeSH) Portal: Biology v t e (EC ... Shimada K, Takahashi M, Tanzawa K (July 1994). "Cloning and functional expression of endothelin-converting enzyme from rat ...

https://en.wikipedia.org/wiki/Endothelin-converting_enzyme_1

... , also known as ECE1, is an enzyme which in humans is encoded by the ECE1 gene. Endothelin- ... 2003). "Shear stress attenuates endothelin and endothelin-converting enzyme expression through oxidative stress". Regul. Pept. ... "Entrez Gene: ECE1 endothelin converting enzyme 1". Schmidt M, Kröger B, Jacob E, Seulberger H, Subkowski T, Otter R, Meyer T, ... 1996). "Human endothelin converting enzyme gene (ECE1) mapped to chromosomal region 1p36.1". Cytogenet. Cell Genet. 72 (4): 322 ...

https://en.wikipedia.org/wiki/Endothelin_converting_enzyme_1

It can inhibit endothelin converting enzymes even in the live rat, probably by chelating metals required by metalloproteases. ... Huggins, John P.; Pelton, John T. (1996-12-23). Endothelins in Biology and Medicine. CRC Press. p. 121. ISBN 9780849369759. ... "Pharmacological profiles of aspergillomarasmines as endothelin converting enzyme inhibitors". The Japanese Journal of ...

https://en.wikipedia.org/wiki/Aspergillomarasmine_A

1998). Endothelin molecular biology, physiology, and pathology. Totowa, N.J.: Humana Press. ISBN 1-4757-2783-6. Hay, edited by ... Ihara, M; Fukuroda, T; Saeki, T; Nishikibe, M; Kojiri, K; Suda, H; Yano, M (15 July 1991). "An endothelin receptor (ETA) ... 2001). Endothelin and Its Inhibitors. Berlin, Heidelberg: Springer Berlin Heidelberg. ISBN 3-642-56899-8. Ihara, Masaki; ... Kitasatospora misakiensis produces tubermycin A, tubermycin B, misakimycin and the endothelin receptor antagonist BE-18257B. ...

https://en.wikipedia.org/wiki/Kitasatospora_misakiensis

... endothelin).[citation needed] Local metabolic control (based on metabolic demand) is the most important mechanism of control of ...

https://en.wikipedia.org/wiki/Vascular_resistance

... for example discovering one of the mechanisms to activate endothelin and that a mutation in endothelin receptor can cause ... including working with Takeshi Sakurai to identify the receptor for endothelin. He kept studying endothelin after moving to the ... Vane, John (1990). "Endothelins come home to roost" (PDF). Nature. 348 (6303): 673. doi:10.1038/348673a0. PMID 2175394. S2CID ... Yanagisawa is most well known for his discovery of the hormone endothelin and the neuropeptide orexin. Early 1980s saw the ...

https://en.wikipedia.org/wiki/Masashi_Yanagisawa

His publications include first-in-human studies with renin inhibitors and endothelin antagonists, including exploration of the ... Haynes WG, Webb DJ (September 1994). "Contribution of endogenous generation of endothelin-1 to basal vascular tone". Lancet. ... Dhaun N, Webb DJ (August 2019). "Endothelins in cardiovascular biology and therapeutics". Nature Reviews. Cardiology. 16 (8): ... role of endothelin antagonists as treatment for vascular and renal disease. He has also contributed to the current ...

https://en.wikipedia.org/wiki/David_Webb_(pharmacologist)

Endothelin Okada, M; Nishikibe, M (Winter 2002). "BQ-788, a selective endothelin ET(B) receptor antagonist". Cardiovascular ...

https://en.wikipedia.org/wiki/BQ-788

Endothelin-1 is a peptide (comprising 21 amino acids) that is produced in endothelial cells. It acts on the endothelin ... The dual (ETA and ETB) endothelin receptor antagonist bosentan was approved in 2001. Sitaxentan (Thelin) was approved for use ... Fonseca C, Abraham D, Renzoni EA (January 2011). "Endothelin in pulmonary fibrosis". American Journal of Respiratory Cell and ... Liu, Chao; Chen, Junmin; Gao, Yanqiu; Deng, Bao; Liu, Kunshen (2021-03-25). Cochrane Airways Group (ed.). "Endothelin receptor ...

https://en.wikipedia.org/wiki/Pulmonary_hypertension

"Interaction between endothelin and angiotensin II." Clinical and Experimental Pharmacology and Physiology. 26.7. (1999): 517- ... Indirectly, angiotensin II stimulates of the production of endothelin 1 and 3 (ET1, ET3) and the transforming growth factor ...

https://en.wikipedia.org/wiki/Moexipril

Endothelin is a potent vasoactive peptide produced by endothelial cells that has both vasoconstrictor and vasodilator ... Circulating endothelin levels are increased in some hypertensive patients, particularly African Americans and persons with ... For example, local nitric oxide and endothelin, which are secreted by the endothelium, are the major regulators of vascular ... Ergul S, Parish DC, Puett D, Ergul A (October 1996). "Racial differences in plasma endothelin-1 concentrations in individuals ...

https://en.wikipedia.org/wiki/Pathophysiology_of_hypertension

Role of endothelin-nitric oxide imbalance". The Journal of Clinical Investigation. 100 (6): 1520-1528. doi:10.1172/JCI119675. ...

https://en.wikipedia.org/wiki/Fabiola_Terzi

Maguire JJ, Davenport AP (Nov 2002). "Is urotensin-II the new endothelin?". British Journal of Pharmacology. 137 (5): 579-88. ...

https://en.wikipedia.org/wiki/Urotensin-II

Phillips PA (July 1999). "Interaction between endothelin and angiotensin II". Clinical and Experimental Pharmacology & ... "Vascular Smooth Muscle Cell Signaling Mechanisms for Contraction to Angiotensin II and Endothelin-1". Journal of the American ... and unnecessary cell proliferation via blockage of AT1 activation conceivably through decreased Endothelin 1 production, a ...

https://en.wikipedia.org/wiki/Fimasartan

It is an endothelin receptor antagonist. Zibotentan was granted fast track status for the treatment of prostate cancer by the ... September 2011). "Preliminary study of the specific endothelin a receptor antagonist zibotentan in combination with docetaxel ...

https://en.wikipedia.org/wiki/Zibotentan

... and thus activate endothelin receptors, endothelin receptor type A (ETA) and endothelin receptor type B (ETB). These receptors ... Lüscher TF, Barton M (November 2000). "Endothelins and endothelin receptor antagonists: therapeutic considerations for a novel ... 1989-01-01). "Synthesis of endothelin-1 analogues, endothelin-3, and sarafotoxin S6b: structure-activity relationships". ... Together with endothelins (ETs), they form a homogenous family of strong vasoconstrictor isopeptides. Among them, a few ...

https://en.wikipedia.org/wiki/Sarafotoxin

... , which relaxes those muscles, is an endothelin receptor antagonist, and is selective for the type A endothelin ... endothelin 1 clearance, and antiproliferation of cells. Endothelin receptor activation mediates strong pulmonary ... Endothelin binds to two receptors, ETA and ETB. ETA is responsible for cell growth in the vessels as well as vasoconstriction, ... As such, endothelin receptor antagonists such as Ambrisentan are known to be teratogenic. Ambrisentan has a high risk of liver ...

https://en.wikipedia.org/wiki/Ambrisentan

... is a fungal isolate that can inhibit endothelin binding. Ohashi, H; Akiyama, H; Nishikori, K; Mochizuki, J (1992 ... "Asterric acid, a new endothelin binding inhibitor". The Journal of Antibiotics. 45 (10): 1684-5. doi:10.7164/antibiotics. ...

https://en.wikipedia.org/wiki/Asterric_acid

Ariza AC, Bobadilla NA, Halhali A (2007). "[Endothelin 1 and angiotensin II in preeeclampsia]". Rev. Invest. Clin. 59 (1): 48- ...

https://en.wikipedia.org/wiki/Bradykinin_receptor_B2

Nelson J, Bagnato A, Battistini B, Nisen P (February 2003). "The endothelin axis: emerging role in cancer". Nat. Rev. Cancer. 3 ... Said N, Smith S, Sanchez-Carbayo M, Theodorescu D (January 2011). "Tumor endothelin-1 enhances metastatic colonization of the ... Targeting this axis with orally available endothelin receptor antagonists may prove efficacious in mimicking the inhibitory ... Evidence demonstrates that RhoGDI2 inhibits the endothelin axis and crosstalk with macrophages within the micrometastatic ...

https://en.wikipedia.org/wiki/ARHGDIB

Ariza AC, Bobadilla NA, Halhali A (2007). "[Endothelin 1 and angiotensin II in preeeclampsia]". Revista de Investigacion ...

https://en.wikipedia.org/wiki/Angiotensin_II_receptor_type_1

... (LU-135252; HMR-4005) is an endothelin receptor antagonist. Gilead Colorado, a subsidiary of Gilead Sciences, under ... Ambrisentan Enseleit F, Lüscher TF, Ruschitzka F (August 2010). "Darusentan, a selective endothelin A receptor antagonist, for ... Endothelin receptor antagonists, Barbiturates, Experimental drugs, Lactims, Carboxylic acids, Diphenylmethanol ethers, Aromatic ...

https://en.wikipedia.org/wiki/Darusentan

... we examined whether endothelin-1 (ET-1) increases acidification of in vivo perfused distal tubules of anesthetized rats. ET-1 ... Because endothelin receptor inhibition blunts increased distal tubule acidification induced by dietary acid, ... Endothelin-1 increases rat distal tubule acidification in vivo Am J Physiol. 1997 Oct;273(4):F586-94. doi: 10.1152/ajprenal. ... Because endothelin receptor inhibition blunts increased distal tubule acidification induced by dietary acid, we examined ...

https://pubmed.ncbi.nlm.nih.gov/9362336/

SEARCH RESULTS for: Endothelin Receptor Antagonist [Drug Class] (23 results) *Share : JavaScript needed for Sharing tools. ...

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Endothelin receptors are relatively enriched in pulmonary vasculature and their inibition results in a decrease in pulmonary ... The endothelin receptor antagonists inhibit the binding of endothelin, a vasoconstrictive peptide, to its receptors on smooth ... Endothelin and endothelin antagonists: pharmacology and clinical implications. Lüscher TF, Wenzel RR. Lüscher TF, et al. Agents ... The endothelin receptor antagonists inhibit the binding of endothelin, a vasoconstrictive peptide, to its receptors on smooth ...

https://www.ncbi.nlm.nih.gov/pubmed/31644032

https://pubmed.ncbi.nlm.nih.gov/31644032

Here, the authors show that endothelin-1 mediated activation of β-arrestin interacts with YAP to recruit mutant p53 to the TEAD ... This interaction allows β-arr1 to recruit mutp53 to the YAP-TEAD transcriptional complex upon activation of endothelin-1 ... The endothelin-1 (ET-1) receptors (ET-1R) ETAR and ETBR, members of G-protein coupled receptors (GPCR) family, are well-known ... Endothelin B receptor mediates the endothelial barrier to T cell homing to tumors and disables immune therapy. Nat. Med. 14, 28 ...

https://www.nature.com/articles/s41467-019-11045-8?error=cookies_not_supported&code=c1988f35-6ee7-4a15-a258-22d715986de6

Disruption of ECE-1 and ECE-2 reveals a role for endothelin-converting enzyme-2 in murine cardiac development. ... Disruption of ECE-1 and ECE-2 reveals a role for endothelin-converting enzyme-2 in murine cardiac development. ... Endothelin-converting enzyme-1 and -2 (ECE-1 and -2) are membrane-bound metalloproteases that can cleave biologically the ... inactive endothelin-1 (ET-1) precursor to form active ET-1 in vitro. We previously reported developmental defects in specific ...

https://www.jci.org/articles/view/7447/figure/7

Acetylated endothelin-1 is a constrictor in guinea pig lung vasculature but not in isolated vascular strips.. H I Magazine, A B ... Acetylated endothelin-1 is a constrictor in guinea pig lung vasculature but not in isolated vascular strips.. H I Magazine, A B ... Acetylated endothelin-1 is a constrictor in guinea pig lung vasculature but not in isolated vascular strips.. H I Magazine, A B ... In contrast, endothelin-1 had an EC50 of 1.46 +/- 0.32 to 1.88 +/- 0.19 nM in various vessel preparations. The differences in ...

https://jpet.aspetjournals.org/content/260/2/632

This effect can be completely prevented by chronic ETA receptor blockade, suggesting that endothelin modulates increased ... modulatory role of endothelin Tobias TRAUPE; Tobias TRAUPE ... modulatory role of endothelin. Clin Sci (Lond) 1 September 2002 ...

https://portlandpress.com/clinsci/article-abstract/103/s2002/13S/69620/Effects-of-obesity-on-endothelium-dependent?redirectedFrom=fulltext

Contractile effects of endothelin-1 on the proximal (A) and distal (B) parts of the ileum in the homozygous endothelin ETB ... Addition of endothelin-1 (0.1-3×100 nM), a non-selective agonist of endothelin ETA and ETB receptors, produced concentration ... A mutation in endothelin-B receptor gene causes myenteric aganglionosis and coat color spotting in rats. DNA Res1996;3:101-5. ... Lack of endothelin ETB receptor binding and function in the rat with a mutant ETB receptor gene. Biochem Biophys Res Commun1996 ...

https://gut.bmj.com/content/50/3/355

Stenman, E, Waldsee, R, Henriksson, M, Maddahi, A & Edvinsson, L 2007, Cooperative effect of angiotensin AT, and endothelin ... Cooperative effect of angiotensin AT, and endothelin ETA receptor antagonism limits the brain damage after ischemic stroke in ... The combined inhibition of angiotensin AT, and endothelin ETA receptors however decreased the brain damage and improved the ... In conclusion, the present study shows that combined inhibition of angiotensin AT, and endothelin ETA receptors reduces the ...

https://portal.research.lu.se/sv/publications/cooperative-effect-of-angiotensin-at-and-endothelin-eta-receptor-

Moreover, previous studies have shown that the endothelin B receptor (EDNRB) gene is abnormally methylated in a high proportion ...

https://edrn.nci.nih.gov/data-and-resources/publications/12499435-986-endothelin-b-receptor-gene-hypermethylation-in-prostate-adenocarcinoma/

Endothelins (ETs) 1 and 3 are expressed in the rat kidney, but the factors that regulate this expression remain unknown. To try ... Expression of endothelins 1 and 3 in the rat kidney. Share Share Share ... Endothelins (ETs) 1 and 3 are expressed in the rat kidney, but the factors that regulate this expression remain unknown. To try ... Animals, Constriction, Denervation, Diet, Sodium-Restricted, Diuretics, Endothelins, Furosemide, Hemorrhage, Kidney, Male, Rats ...

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Endothelial expression of endothelin receptor A in the systemic capillary leak syndrome. Thursday, September 17, 2015. - Poster ... Ednra, encoding Endothelin receptor A (ETA), was significantly increased in SCLS BOEC compared to healthy controls. Although ...

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Blocking endothelin: breaking new ground. Source: Eur Respir Rev 2008; 17: 24-29. Year: 2007. ... Endothelin receptor antagonist (ETRA) bosentan (B) in patients with severe pulmonary hypertension (PH) associated with ... Endothelin receptor expression in idiopathic pulmonary arterial hypertension: effect of bosentan and epoprostenol treatment. ... Effects of endothelin receptor antagonist (ERA) bosentan on myocardial glucose metabolism in pulmonary arterial hypertension ( ...

https://www.ers-education.org/lr/show-details/?idP=920

El Sayed, M., Sherif, L., Said, R., El-Wakkad, A., & El-Refay, A. (2011). Endothelin-1 and L -arginine in preterm infants with ...

https://hsrc.himmelfarb.gwu.edu/smhs_peds_facpubs/5454/

":"Endothelin Receptor Antagonists","data":{"category":"Medicine","linkRef":"Endothelin Receptor Antagonists"}},{"value":" ...

https://schedule.pharmac.govt.nz/ScheduleOnline.php?code=A074005&

Plasma endothelin and big endothelin levels in cardiovascular subjects and effects of Bosentan Yumi Miyauchi, Seiji Maeda, ... Structure-activity relationship of Endothelin-1 and Endothelin-2, revisited. isolated rat mesenteric resistance arteries. ... Pharmacology of Endothelin Receptors and Antagonists - Results from New Clinical Studies. Potential role of ET-1 in ischaemic ... Endothelin receptors in normal and cirrhotic human liver Lowell Ling, Rhoda Kuc, Janet Maguire, Neil Davie, Paul Gibbs, Graeme ...

https://www.endothelins.com/Conferences/Cambridge2011/program/Scientific/Posters%20I/

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Endothelin Antagonists. Renal inflammation and fibrosis has been associated with endothelin activation. Endothelin A (ETA) ... Endothelin antagonists for diabetic and non-diabetic chronic kidney disease. Br J Clin Pharmacol. 2013 Oct. 76 (4):573-9. [QxMD ... Endothelin B (ETB) decreases arterial pressure by inhibiting salt and water reabsorption in the kidneys. A trial of an ...

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SEARCH RESULTS for: Endothelin Receptor Antagonist [Drug Class] (23 results) *Share : JavaScript needed for Sharing tools. ...

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Purchase QuantiGlo Chemiluminescent Human Endothelin-1 ELISA Kit (QET00B) from R&D Systems, a Bio-Techne brand. Sensitivity: ... Background: Endothelin-1 Endothelin-1 (ET-1), a peptide of 21 amino acid (aa) residues, is a pleiotropic molecule best known ... Human Endothelin-1 QuantiGlo ELISA Kit Summary: The QuantiGlo Human Endothelin-1 Chemiluminescent Immunoassay is a 4.5 hour ... This immunoassay has been shown to accurately quantitate human Endothelin-1. Results obtained using natural human Endothelin-1 ...

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Endothelin (ET) is found to be increased in kidney disease secondary to hyperglycaemia, hypertension, acidosis, and the ... Endothelin Receptor Antagonists in Kidney Disease. Martínez-Díaz, Irene; Martos, Nerea; Llorens-Cebrià, Carmen; Álvarez, ... Therefore, endothelin receptor antagonists (ERAs) have been proposed as a therapeutic strategy to reduce proteinuria and slow ... The use of a dual angiotensin-II type 1/endothelin receptor blocker (sparsentan) is also being evaluated to treat kidney ...

https://pesquisa.bvsalud.org/portal/resource/pt/mdl-36834836

Human being leukocyte antigens (HLA) have been extensively studied as being antigen presenting receptors, but many aspects of their function remain elusive, especially their association with numerous autoimmune diseases. and propose the possibility that the 70-74 DR epitope may contribute to disease risk by mechanisms other than antigen presentation. associates with both type-1 diabetes and celiac disease (7, 8). Moreover, there are certain HLA alleles, e.g. associates with human being RA and also confers susceptibility to inflammatory arthritis in mice (12). Such cross-species susceptibility is definitely hard to explain in terms of HLA-restricted antigen demonstration. The allele-dose impact on disease severity that has been observed in RA (13-15), or the allele-dose effects on concordance rates in monozygotic twins (16) are hard to explain with antigen presentation-based hypotheses. 3. PV, Desmoglein CSF2RA 3 and is one of the better-characterized alleles (23-25). In fact, over 95% of PV ...

http://www.insulin-receptor.info/category/endothelin-receptors/

深入研究「Lipopolysaccharide enhanced renal vascular response to endothelin-1 through ETA overexpression in portal hypertensive rats ... Lipopolysaccharide enhanced renal vascular response to endothelin-1 through ETA overexpression in portal hypertensive rats. ...

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The new fluorogenic hexapeptide substrate CMC-Ala-Gly-Gly-Trp-Phe-Arg was used as substrate for endothelin-converting enzyme ( ... Gureeva T.A. et al., Study of substrate specificity of a new peptide substrate of endothelin converting enzyme. ... E., Solovyeva, N. I. (2007). Study of substrate specificity of a new peptide substrate of endothelin converting enzyme. ... Study of substrate specificity of a new peptide substrate of endothelin converting enzyme // Biomeditsinskaya Khimiya. - 2007 ...

http://pbmc.ibmc.msk.ru/en/article-en/PBMC-2007-53-2-172/

Focal injections of endothelin-1 into specific areas of the rat CNS represent a model to investigate therapeutic approaches to ... Twenty-four hours after microinjection of 10 pmoles of endothelin-1, we observed a loss of neurons in the grey matter. At 72 ... In this study we investigate whether the vasoactive peptide, endothelin-1, can generate a focal ischemic lesion in the white ... Using a minimally invasive technique to microinject endothelin-1 into selected brain regions, we observed an acute reduction in ...

https://www.immunology.ox.ac.uk/publications/383075?b9b1d8d2-ff45-11ed-bff9-061b866677b4

Endothelin-1 and peak oxygen consumption in patients with heart failure with preserved ejection fraction.. ... Endothelin-1 and peak oxygen consumption in patients with heart failure with preserved ejection fraction. Heart Lung 2021 May- ... While Endothelin -1 (ET-1) plays a mechanistic role in pulmonary hypertension, its role in exercise intolerance in HFpEF is not ... Home Publications Endothelin-1 and peak oxygen consumption in patients with heart failure with preserved ejection fraction. ...

https://biolincc.nhlbi.nih.gov/publications/ac0eeff63ec847fbb682e7cd107a29bb

... Hippocampal cannabinoid-1 receptor upregulation upon endothelin-B receptor deficiency: A neuroprotective substitution effect ? ... 2005). Hippocampal cannabinoid-1 receptor upregulation upon endothelin-B receptor deficiency: A neuroprotective substitution ...

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The endothelin receptor antagonists inhibit the binding of endothelin, a vasoconstrictive peptide, to its receptors on smooth muscle cells which results in vasodilation. (nih.gov)
Endothelin receptors are relatively enriched in pulmonary vasculature and their inibition results in a decrease in pulmonary vascular pressure. (nih.gov)
This interaction allows β-arr1 to recruit mutp53 to the YAP-TEAD transcriptional complex upon activation of endothelin-1 receptors (ET-1R) in patient-derived HG-SOC cells and in cell lines bearing mutp53. (nature.com)
The endothelin-1 (ET-1) receptors (ET-1R) ET A R and ET B R, members of G-protein coupled receptors (GPCR) family, are well-known drivers of tumor progression in many human malignancies, including OC 3 . (nature.com)
Cerebral ischemia results in enhanced expression of smooth muscle cell endothelin and angiotensin receptors in cerebral arteries. (lu.se)
In conclusion, the present study shows that combined inhibition of angiotensin AT, and endothelin ETA receptors reduces the brain damage and improves the neurological outcome after ischemic stroke in rat. (lu.se)

Endothelin-1 (ET-1) is a 21 amino acid peptide that acts in a paracrine and autocrine fashion as a potent vasoconstrictor. (nih.gov)
Endothelin-1 (ET-1), a peptide of 21 amino acid (aa) residues, is a pleiotropic molecule best known for its action as a potent vasoconstrictor (1). (bio-techne.com)
In this study we investigate whether the vasoactive peptide, endothelin-1, can generate a focal ischemic lesion in the white matter and compare the findings with endothelin-1-induced lesions in the grey matter. (ox.ac.uk)
BACKGROUND: Red wine consumption may influence on vasoconstrictive peptide endothelin-1 levels, and this may be one mechanism leading to improved vasodilation after red wine consumption. (lacienciadelvino.com)

Ednra, encoding Endothelin receptor A (ETA), was significantly increased in SCLS BOEC compared to healthy controls. (nih.gov)

In patients with pulmonary arterial hypertension, (PAH) the endothelin receptor antagonists have been shown to improve exercise tolerance and slow progression of disease. (nih.gov)
We examined the relative importance of the two amino groups of endothelin-1 in mediating pulmonary vasoconstrictor activity. (aspetjournals.org)
Is there a role for endothelin-1 receptor antagonists in the treatment of lung fibrosis associated with pulmonary hypertension? (ers-education.org)
Potentiating Bradykinin Pathway by Genetic Suppression of Endothelin-converting Enzyme-1 Prevented Hypoxic induced Pulmonary Hypertension and Right Ventricular Hypertrophy. (endothelins.com)
While Endothelin -1 (ET-1) plays a mechanistic role in pulmonary hypertension, its role in exercise intolerance in HFpEF is not well established. (nih.gov)
Mehra Pratishtha, Mehta Vimal, Yusuf Jamal, Mukhopadhyay Saibal, Dabla Pradeep Kumar, Parashar Lokesh, Sukhija Rishi, Aronow Wilbert S.. Gender differences in genotypic distribution of endothelin-1 gene and endothelin receptor A gene in pulmonary hypertension associated with rheumatic mitral valve disease. (who.int)
Aim: We aimed to investigate whether there was a difference in genotypic distribution of endothelin-1 (ET-1) and endothelin receptor A (ETA) genes between female and male patients of pulmonary hypertension associated with rheumatic mitral valve disease (PH-MVD). (who.int)

In AD, amyloid-β (Aβ) accumulation may similarly raise cerebral vascular resistance by upregulation of the cerebral endothelin system. (nih.gov)

While all endothelin receptor antagonists have been associated with occasional transient serum enzyme elevations during therapy, only bosentan and sitaxentan have been clearly linked to instances of clinically apparent, acute liver injury. (nih.gov)
Endothelin-converting enzyme-1 and -2 (ECE-1 and -2) are membrane-bound metalloproteases that can cleave biologically the inactive endothelin-1 (ET-1) precursor to form active ET-1 in vitro. (jci.org)
Big ET-1 is then cleaved by the membrane-bound metalloprotease Endothelin-converting enzyme (ECE-1), producing the potent 21 aa mature form ET-1 (aa 1-21) (7, 8). (bio-techne.com)
Immunoreactive endothelin-1 (ET-1) in normal human plasma was determined by a sensitive sandwich-type enzyme immunoassay after being extracted with Seppak C18 cartridges. (elsevierpure.com)

Sitaxsentan, a forth endothelin receptor blocker, was approved in Europe, but not in the United States, and has subsequently been withdrawn because of cases of severe liver injury linked to its use. (nih.gov)
The use of a dual angiotensin -II type 1/ endothelin receptor blocker (sparsentan) is also being evaluated to treat kidney disease . (bvsalud.org)

Endothelin 3 functions by interacting with another protein, endothelin receptor type B (produced from the EDNRB gene), on the surface of cells. (medlineplus.gov)
Pingault V, Bondurand N, Lemort N, Sancandi M, Ceccherini I, Hugot JP, Jouk PS, Goossens M. A heterozygous endothelin 3 mutation in Waardenburg-Hirschsprung disease: is there a dosage effect of EDN3/EDNRB gene mutations on neurocristopathy phenotypes? (medlineplus.gov)

Endothelin B receptor gene hypermethylation in prostate adenocarcinoma. (nih.gov)
The EDN3 gene provides instructions for making a protein called endothelin 3. (medlineplus.gov)
Changes in the EDN3 gene disrupt the normal function of endothelin 3, preventing it from playing its usual role in the development of enteric nerves. (medlineplus.gov)
EDN3 gene variants change single nucleotides in the gene, preventing the production of a functional endothelin 3 protein. (medlineplus.gov)

Acetylated endothelin-1 is a constrictor in guinea pig lung vasculature but not in isolated vascular strips. (aspetjournals.org)
7] The histologic changes are mediated by increased endothelin 1, elevated thromboxane, platelet activation, and production of intrinsic elastase and vascular endothelial growth factors. (medscape.com)
The level of endothelin-1 in brain tissue correlates positively with Aβ load and negatively with markers of cerebral hypoperfusion such as increased vascular endothelial growth factor. (nih.gov)
Oral Zibotentan (3 mg/kg/d, administered for 31 d) abrogated the effects of Aβ40 infusion on baroreflex responsiveness and blood pressure, which declined, although without reduction in carotid blood flow, and Zibotentan caused uncoupling of the positive linear relationship between endothelin-1 and vascular endothelial growth factor, which as a sensor of tissue oxygenation would be expected to increase if there were hypoperfusion. (nih.gov)

and markers of cerebral oxygenation, in the (normotensive)Wistar rat, and the modulatory influence of the endothelin A receptor antagonist Zibotentan (ZD4054). (nih.gov)

Proteins in the endothelin family are produced in various cells and tissues, where they are involved in the development and function of blood vessels, the production of certain hormones, and the stimulation of cell growth and division (proliferation). (medlineplus.gov)
We report that endothelin-1 signalling reduced the generation and enhanced the repair of ultraviolet radiation (UV)-induced DNA photoproducts, and inhibited apoptosis of human melanocytes, without increasing cAMP levels, melanin content or proliferation. (nih.gov)

Originally isolated from porcine aortic endothelial cells, ET-1 is one of a family of three proteins encoded by distinct genes that also includes Endothelin-2 (ET-2) and Endothelin-3 (ET-3) (2, 3). (bio-techne.com)

We hypothesise that this phenomenon may be detrimental and that acute treatment with a combined non-hypotensive dose of the angiotensin AT, receptor inhibitor candesartan and the endothelin ETA receptor antagonist ZD 1611 reduces the infarct in experimental ischemic stroke. (lu.se)
The middle cerebral arteries were harvested for immunocytochemical studies of angiotensin AT, and endothelin ETA receptor expression. (lu.se)

Three endothelin receptor antagonists are currently approved and in use in the United States: bosentan (2001: Tracleer), ambrisentan (2007: Letairis) and macitentan (2013: Opsumit). (nih.gov)
Endothelin Receptor Antagonists in Kidney Disease. (bvsalud.org)
Therefore, endothelin receptor antagonists (ERAs) have been proposed as a therapeutic strategy to reduce proteinuria and slow the progression of kidney disease . (bvsalud.org)

Endothelin (ET) is found to be increased in kidney disease secondary to hyperglycaemia, hypertension , acidosis , and the presence of insulin or proinflammatory cytokines . (bvsalud.org)

Using a minimally invasive technique to microinject endothelin-1 into selected brain regions, we observed an acute reduction in local MRI perfusion in the injected hemisphere after 1 hour. (ox.ac.uk)
The purpose of this randomized trial was to determine the acute effects of these beverages on endothelin-1 levels and compare them to coronary artery epicardial diameter and flow rate. (lacienciadelvino.com)
CONCLUSIONS: Red wine and de-alcoholized red wine decreased plasma endothelin-1 levels after acute consumption, but this change was not reflected in coronary epicardial diameters or flow rate. (lacienciadelvino.com)

Our preclinical studies demonstrate an important role for renal endothelin-1 (ET-1) in regulating sodium excretion. (elsevierpure.com)

Because endothelin receptor inhibition blunts increased distal tubule acidification induced by dietary acid, we examined whether endothelin-1 (ET-1) increases acidification of in vivo perfused distal tubules of anesthetized rats. (nih.gov)

Endothelin-1 levels and their association with coronary epicardial diameter and flow rate, however, have not been studied in vivo after consumption of red wine and de-alcoholized red wine. (lacienciadelvino.com)
Endothelin-1 levels were determined and coronary artery diameter and flow rate assessed using transthoracic echocardiography before and acutely after intervention. (lacienciadelvino.com)

After injection of 10 pmoles endothelin-1 into the cortical white matter, we observed prolific amyloid precursor protein-positive immunostaining (indicative of axonal disruption) and an increase in tau-1 immunostaining in oligodendrocytes at 6 hours. (ox.ac.uk)

Expression of endothelins 1 and 3 in the rat kidney. (ox.ac.uk)
Endothelins (ETs) 1 and 3 are expressed in the rat kidney, but the factors that regulate this expression remain unknown. (ox.ac.uk)

The QuantiGlo Human Endothelin-1 Chemiluminescent Immunoassay is a 4.5 hour solid phase ELISA designed to measure human Endothelin-1 levels in cell culture supernates, serum, EDTA plasma, and urine without extraction. (bio-techne.com)

In particular, endothelin 3 and its receptor are essential for the formation of nerves in the intestine (enteric nerves) and for the production of specialized cells called melanocytes. (medlineplus.gov)
Because active endothelin 3 is necessary for the formation of enteric nerves and melanocytes, these cell types do not form normally during embryonic development. (medlineplus.gov)
Baynash AG, Hosoda K, Giaid A, Richardson JA, Emoto N, Hammer RE, Yanagisawa M. Interaction of endothelin-3 with endothelin-B receptor is essential for development of epidermal melanocytes and enteric neurons. (medlineplus.gov)
Endothelin-1 protects human melanocytes from UV-induced DNA damage by activating JNK and p38 signalling pathways. (nih.gov)
Endothelin-1 is a paracrine factor with mitogenic, melanogenic and survival effects on cultured human melanocytes. (nih.gov)
Our results underscore the significance of endothelin-1 and endothelin B receptor signalling in reducing the genotoxic effects of UV via activating JNK and p38, hence restoring genomic stability of melanocytes. (nih.gov)

In this context, ET, via the endothelin receptor type A (ETA) activation, causes sustained vasoconstriction of the afferent arterioles that produces deleterious effects such as hyperfiltration, podocyte damage, proteinuria and, eventually, GFR decline. (bvsalud.org)
Objective: The main objective of this brief review was to highlight some of the recent advances in our understanding of the mechanisms whereby the endothelin (ET) system, via ET type A (ET A ) receptor activation, modulates blood pressure in preeclamptic women and in animal models of pregnancy-related hypertension. (umn.edu)
Activation of both JNK and p38 was required for reducing DNA photoproducts, but only JNK partially contributed to the survival effect of endothelin-1. (nih.gov)
ATF-2 activation depended mainly on JNK, yet was not sufficient for the effect of endothelin-1 on UV-induced DNA damage, suggesting the requirement for other JNK and p38 targets for this effect. (nih.gov)

0.0001) (paired t -test: increase of 3 (0.1-5.6) mmHg ( p = 0.040)), with evidence of reduced baroreflex responsiveness, and accumulation of Aβ and elevated endothelin-1 in the vicinity of the infusion. (nih.gov)

Future studies should explore Endothelin-1 antagonism to improve exercise tolerance in HFpEF. (nih.gov)

Focal injections of endothelin-1 into specific areas of the rat CNS represent a model to investigate therapeutic approaches to white matter ischemia. (ox.ac.uk)
Pathophysiology of hypertension in response to placental ischemia during pregnancy: A central role for endothelin? (umn.edu)

Background and aims: The endothelin ETB receptor null rat (ETB(−/−)R) has an intestinal segment without ganglia, and this rat is characterised by intestinal obstruction similar to that observed in human Hirschsprung's disease. (bmj.com)
Increased endothelin-1 (ET-1) levels disordered thiol protein status and erythrocyte hydration status play essential roles in sickle cell disease (SCD) through unresolved mechanisms. (cell-metabolism.com)

The effects of endothelin-1 were dependent on increasing intracellular calcium mobilization by endothelin B receptor signalling. (nih.gov)

In contrast, endothelin-1 had an EC50 of 1.46 +/- 0.32 to 1.88 +/- 0.19 nM in various vessel preparations. (aspetjournals.org)

During early development before birth, endothelin 3 and endothelin receptor type B together play an important role in neural crest cells. (medlineplus.gov)

Results obtained using natural human Endothelin-1 showed dose curves that were parallel to the standard curves obtained using the QuantiGlo kit standards. (bio-techne.com)
These results indicate that this kit can be used to determine relative mass values of natural human Endothelin-1. (bio-techne.com)

It contains synthetic human Endothelin-1 and antibodies raised against the synthetic factor. (bio-techne.com)
This immunoassay has been shown to accurately quantitate human Endothelin-1. (bio-techne.com)
The recovery of synthetic human Endothelin-1 spiked to three different levels throughout the range of the assay in various matrices was evaluated. (bio-techne.com)

The constricted muscle segments without ganglia had a greater increase in absolute force when stimulated by carbachol, high K + , and endothelin-1 compared with that of normal siblings. (bmj.com)

All members of the Endothelin family contain two essential disulfide bridges and six conserved aa residues at the C-terminus. (bio-techne.com)

Anatomy4

Organisms2

Chemicals and Drugs26

Analytical, Diagnostic and Therapeutic Techniques and Equipment3

Phenomena and Processes7

Technology, Industry, Agriculture1

Information Science2

Inhibition of in vitro enteric neuronal development by endothelin-3: mediation by endothelin B receptors. (1/1796)

Endogenous plasma endothelin concentrations and coronary circulation in patients with mild dilated cardiomyopathy. (2/1796)

Endothelin up-regulation and localization following renal ischemia and reperfusion. (3/1796)

Nitric oxide limits the eicosanoid-dependent bronchoconstriction and hypotension induced by endothelin-1 in the guinea-pig. (4/1796)

Blockade and reversal of endothelin-induced constriction in pial arteries from human brain. (5/1796)

Endothelin-1 and its mRNA in the wall layers of human arteries ex vivo. (6/1796)

Effects of hypertension, diabetes mellitus, and hypercholesterolemia on endothelin type B receptor-mediated nitric oxide release from rat kidney. (7/1796)

Maintenance of blood pressure in normotensive dogs by endothelin. (8/1796)

Endothelins

Endothelin-2

Endothelin-3

Receptors, Endothelin

Receptor, Endothelin B

Endothelin-1

Viper Venoms

Receptor, Endothelin A

Peptides, Cyclic

Tachyphylaxis

Neprilysin

Aspartic Acid Endopeptidases

Sulfonamides

Adrenergic Agents

Metalloendopeptidases

Vasoconstrictor Agents

Pyrrolidines

Piperidines

Polymethacrylic Acids

Glycopeptides

Oligopeptides

Vasoconstriction

Thermolysin

Peptide Fragments

Endothelium, Vascular

Protein Precursors

Rats, Wistar

Muscle Contraction

Muscle, Smooth

Nitric Oxide

RNA, Messenger

Peptides

Kidney

Rats, Sprague-Dawley

Molecular Sequence Data

Cells, Cultured

Binding, Competitive

Dose-Response Relationship, Drug

Chromatography, High Pressure Liquid

Amino Acid Sequence

Blood Pressure

Inhibition of in vitro enteric neuronal development by endothelin-3: mediation by endothelin B receptors. (1/1796)

Endogenous plasma endothelin concentrations and coronary circulation in patients with mild dilated cardiomyopathy. (2/1796)

Endothelin up-regulation and localization following renal ischemia and reperfusion. (3/1796)

Nitric oxide limits the eicosanoid-dependent bronchoconstriction and hypotension induced by endothelin-1 in the guinea-pig. (4/1796)

Blockade and reversal of endothelin-induced constriction in pial arteries from human brain. (5/1796)

Endothelin-1 and its mRNA in the wall layers of human arteries ex vivo. (6/1796)

Effects of hypertension, diabetes mellitus, and hypercholesterolemia on endothelin type B receptor-mediated nitric oxide release from rat kidney. (7/1796)

Maintenance of blood pressure in normotensive dogs by endothelin. (8/1796)

Endothelin

Endothelin 3

Endothelin receptor

Endothelin 2

Endothelin 1

Endothelin receptor antagonist

Endothelin B receptor

Endothelin A receptor

Endothelin-converting enzyme 1

Endothelin converting enzyme 1

Aspergillomarasmine A

Kitasatospora misakiensis

Vascular resistance

Masashi Yanagisawa

David Webb (pharmacologist)

BQ-788

Pulmonary hypertension

Moexipril

Pathophysiology of hypertension

Fabiola Terzi

Urotensin-II

Fimasartan

Zibotentan

Sarafotoxin

Ambrisentan

Asterric acid

Bradykinin receptor B2

ARHGDIB

Angiotensin II receptor type 1

Darusentan

Endothelin-1 increases rat distal tubule acidification in vivo