Endothelins are peptides with receptors and effects in many body organs.[1][2][3] Endothelin constricts blood vessels and raises blood pressure. The endothelins are normally kept in balance by other mechanisms, but when overexpressed, they contribute to high blood pressure (hypertension), heart disease, and potentially other diseases.[1][4]
Endothelins are 21-amino acid vasoconstricting peptides produced primarily in the endothelium having a key role in vascular homeostasis. Endothelins are implicated in vascular diseases of several organ systems, including the heart, lungs, kidneys, and brain.[5][6] As of 2018, endothelins remain under extensive basic and clinical research to define their roles in several organ systems.[1][7][8][9]
^ abcDavenport AP, Hyndman KA, Dhaun N, Southan C, Kohan DE, Pollock JS, et al. (April 2016). "Endothelin". Pharmacological Reviews. 68 (2): 357–418. doi:10.1124/pr.115.011833. PMC 4815360. PMID 26956245.
^Kawanabe Y, Nauli SM (January 2011). "Endothelin". Cellular and Molecular Life Sciences. 68 (2): 195–203. doi:10.1007/s00018-010-0518-0. PMC 3141212. PMID 20848158.
^Kedzierski RM, Yanagisawa M (2001). "Endothelin system: the double-edged sword in health and disease". Annual Review of Pharmacology and Toxicology. 41: 851–76. doi:10.1146/annurev.pharmtox.41.1.851. PMID 11264479.
^Maguire JJ, Davenport AP (December 2014). "Endothelin@25 - new agonists, antagonists, inhibitors and emerging research frontiers: IUPHAR Review 12". British Journal of Pharmacology. 171 (24): 5555–72. doi:10.1111/bph.12874. PMC 4290702. PMID 25131455.
^Agapitov AV, Haynes WG (March 2002). "Role of endothelin in cardiovascular disease". Journal of the Renin-Angiotensin-Aldosterone System. 3 (1): 1–15. doi:10.3317/jraas.2002.001. PMID 11984741. S2CID 11382836.
^Schinelli S (2006). "Pharmacology and physiopathology of the brain endothelin system: an overview". Current Medicinal Chemistry. 13 (6): 627–38. doi:10.2174/092986706776055652. PMID 16529555.
^Kuang HY, Wu YH, Yi QJ, Tian J, Wu C, Shou WN, Lu TW (March 2018). "The efficiency of endothelin receptor antagonist bosentan for pulmonary arterial hypertension associated with congenital heart disease: A systematic review and meta-analysis". Medicine. 97 (10): e0075. doi:10.1097/MD.0000000000010075. PMC 5882424. PMID 29517668.
^Iljazi A, Ayata C, Ashina M, Hougaard A (March 2018). "The Role of Endothelin in the Pathophysiology of Migraine-a Systematic Review". Current Pain and Headache Reports. 22 (4): 27. doi:10.1007/s11916-018-0682-8. PMID 29557064. S2CID 35440852.
^Lu YP, Hasan AA, Zeng S, Hocher B (2017). "Plasma ET-1 Concentrations Are Elevated in Pregnant Women with Hypertension -Meta-Analysis of Clinical Studies". Kidney & Blood Pressure Research. 42 (4): 654–663. doi:10.1159/000482004. PMID 29212079.
Endothelins are peptides with receptors and effects in many body organs. Endothelin constricts blood vessels and raises blood pressure. The endothelins...
is proteolytically processed to release endothelin 1. Endothelin 1 is one of three isoforms of human endothelin. Preproendothelin is precursor of the peptide...
An endothelin receptor antagonist (ERA) is a drug that blocks endothelin receptors. Three main kinds of ERAs exist: selective ETA receptor antagonists...
There are at least four known endothelin receptors, ETA, ETB1, ETB2 and ETC, all of which are G protein-coupled receptors whose activation result in elevation...
Endothelin receptor type B, (ET-B) is a protein that in humans is encoded by the EDNRB gene. Endothelin receptor type B is a G protein-coupled receptor...
Endothelin receptor type A, also known as ETA, is a human G protein-coupled receptor. Endothelin receptor type A has been shown to interact with HDAC7A...
Matsuda, Yoichi; Akiyama, Toyoko (February 2012). "Gene Duplication of endothelin 3 Is Closely Correlated with the Hyperpigmentation of the Internal Organs...
Endothelin converting enzyme 1, also known as ECE1, is an enzyme which in humans is encoded by the ECE1 gene. Endothelin-converting enzyme-1 is involved...
taken by mouth. Aprocitentan is a dual endothelin-1 antagonist that targets both endothelin A and endothelin B receptors. Aprocitentan was approved for...
Macitentan, sold under the brand name Opsumit, is an endothelin receptor antagonist (ERA) developed by Actelion and approved for the treatment of pulmonary...
activity) decreases. Endothelin-1 is a peptide (comprising 21 amino acids) that is produced in endothelial cells. It acts on the endothelin receptors ETA and...
Bosentan, sold under the brand name Tracleer among others, is a dual endothelin receptor antagonist medication used in the treatment of pulmonary artery...
Endothelin-3 is a protein that in humans is encoded by the EDN3 gene. The protein encoded by this gene is a member of the endothelin family. Endothelins...
Endothelin 2 (ET-2) is a protein encoded by the EDN2 gene in humans. It was first discovered in 1988 by Yanagisawa and team and belongs to a family of...
to Hirschsprung's disease in humans. A mutation in the middle of the endothelin receptor type B (EDNRB) gene causes lethal white syndrome when homozygous...
the brand name Tyvalzi) is a synthetic analog of endothelin-1 that works as a selective endothelin-B receptor agonist. In May 2023, it was approved in...
decrease collagen degradation and increase extracellular matrix production. Endothelin signalling is implicated in the pathophysiology of fibrosis. Vitamin D...
the treatment of primary immunoglobulin A nephropathy. Sparsentan is an endothelin and angiotensin II receptor antagonist. It is taken by mouth. It was approved...
hormones; angiotensin II, endothelin-1 and the catecholamines (e.g. noradrenaline).[citation needed] Angiotensin-II and endothelin-1 are hormones that bind...
the treatment of pulmonary hypertension. It is an endothelin receptor antagonist. The peptide endothelin constricts muscles in blood vessels, increasing...
vasoconstriction, including the release of vasoconstrictor substances such as endothelin and angiotensin II, both of which play crucial roles in the modulation...
sympathetic drive in hypertension include reactive oxygen species and endothelin. Some studies have shown that hypertensive patients manifest greater vasoconstrictor...
intermingling of fetal and maternal blood occurs ("placental barrier"). Endothelin and prostanoids cause vasoconstriction in placental arteries, while nitric...
transmembrane zinc-dependent endopeptidase which is responsible for cleaving endothelin-3. The KEL gene encodes a type II transmembrane glycoprotein that is the...
thought there is a massive degranulation of vasoconstrictors, including endothelins and free radicals, that cause the vasospasm. Intracranial aneurysms may...
EtBr may refer to: Bromoethane Endothelin_B_receptor (when written as ETBR) Ethidium bromide This disambiguation page lists articles associated with the...
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