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Vasoconstricting peptide family
genes for endothelin-1 (ET-1), endothelin-2 (ET-2), and endothelin-3 (ET-3) are located on chromosomes 6, 1, and 20, respectively. Endothelin functions
Endothelin
Protein found in humans
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
Endothelin_2
Protein-coding gene in the species Homo sapiens
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_3
Vasoconstricting peptide
Endothelin 1 (ET-1), also known as preproendothelin-1 (PPET1), is the most potent vasoconstrictor produced by the human body. It is a peptide produced
Endothelin_1
Drug that blocks endothelin receptors
An endothelin receptor antagonist (ERA) is a drug that blocks endothelin receptors. Three main kinds of ERAs exist: Dual ET Receptor Antagonists, which
Endothelin receptor antagonist
Endothelin_receptor_antagonist
G protein-coupled receptor
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
Chemical compound
the treatment of pulmonary hypertension. It is an endothelin receptor antagonist. The peptide endothelin constricts muscles in blood vessels, increasing
Ambrisentan
Chemical compound
both endothelin A and endothelin B receptors. Aprocitentan was approved for medical use in the United States in March 2024. It is the first endothelin receptor
Aprocitentan
Chemical compound
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
Sovateltide
Protein-coding gene in the species Homo sapiens
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_B
Protein-coding gene in the species Homo sapiens
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
Endothelin_A_receptor
Mammalian protein found in humans
keratinocytes and endothelial cells. Endothelin-converting enzyme-1 is involved in the proteolytic processing of endothelin-1 (EDN1), -2 (EDN2), and -3 (EDN3) to
Endothelin converting enzyme 1
Endothelin_converting_enzyme_1
Medication
Bosentan, sold under the brand name Tracleer among others, is a dual endothelin receptor antagonist medication used in the treatment of pulmonary artery
Bosentan
Chemical compound
BQ-123 is a selective ETA endothelin receptor antagonist. As such, it is used as a biochemical tool in the study of endothelin receptor function. BQ-123
BQ-123
Breed of chicken from Indonesia
their 20th chromosome involving the endothelin 3 gene (EDN3). The roosters weigh 2–2.5 kg (4.4–5.5 lb) and the hens 1.5–2 kg (3.3–4.4 lb). The hens lay tinted
Ayam_Cemani
Chemical compound
Macitentan, sold under the brand name Opsumit, is an endothelin receptor antagonist developed by Actelion and approved for the treatment of pulmonary arterial
Macitentan
Urocortin Antagonists: Astressin-B See here instead. Agonists: Endothelin 1 Endothelin 2 Endothelin 3 IRL-1620 Sarafotoxin Antagonists: A-192621 Ambrisentan
List of signaling peptide/protein receptor modulators
List_of_signaling_peptide/protein_receptor_modulators
High blood pressure in the pulmonary arteries
vasodilation. Endothelin receptor antagonists cause vasodilation as well by blocking the action of the potent vasoconstrictor endothelin-1. Prostacyclins
Pulmonary arterial hypertension
Pulmonary_arterial_hypertension
Breed of chicken
Carl-Johan (2016-02-16). "A Complex Genomic Rearrangement Involving the Endothelin 3 Locus Causes Dermal Hyperpigmentation in the Chicken". PLOS Genet. 7
Svarthöna
276.249 – endothelins MeSH D12.644.276.249.225 – endothelin-1 MeSH D12.644.276.249.235 – endothelin-2 MeSH D12.644.276.249.245 – endothelin-3 MeSH D12
List_of_MeSH_codes_(D12.644)
Chemical compound
brand name Pivlaz) is a drug belonging to the class of endothelin receptor antagonists. The endothelin 1 receptor is one of the strongest known vasoconstrictors
Clazosentan
Chemical compound
BQ-788 is a selective ETB antagonist. Endothelin Okada, M; Nishikibe, M (Winter 2002). "BQ-788, a selective endothelin ET(B) receptor antagonist". Cardiovascular
BQ-788
Cell surface receptors
hormone Sauvagine Urocortin Antagonists Astressin-B Agonists Endothelin 1 Endothelin 2 Endothelin 3 IRL-1620 Sarafotoxin Antagonists A-192621 Ambrisentan Aprocitentan
Signaling_peptide_receptor
Genetic disorder in horses
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
Lethal_white_syndrome
Chemical compound
brand name Vanrafia, is a medication used to reduce proteinuria. It is an endothelin receptor antagonist. It is taken by mouth. Atrasentan was approved for
Atrasentan
Protein toxin family
derivations of previously mentioned ones. The main differences in the family of endothelin and sarafotoxins appear at N-terminal of peptides, as C-terminal in all
Sarafotoxin
Investigational drug
Biopharmaceutics for the treatment of diabetic nephropathy. It is an endothelin A receptor antagonist. "Diosuxentan". AdisInsight. Springer Nature Switzerland
Diosuxentan
Protein-coding gene in the species Homo sapiens
Endothelin-converting enzyme-like 1 is a protein that in humans is encoded by the ECEL1 gene. This gene encodes a member of the neutral endopeptidase (NEP)-related
ECEL1
Medical condition
D – sensorineural deafness. The syndrome is caused by mutation in the endothelin B receptor gene (EDNRB). In the beginning, medical officials defined ABCD
ABCD_syndrome
Class of drugs
receptors. The alpha-adrenergic receptor has two subclasses, α1 and α2. Alpha 2 receptors are associated with sympatholytic properties, while alpha 1 receptors
Alpha-adrenergic_agonist
Chemical compound
Tazi KA, Barriere E, Poirel O, et al. (December 2004). "Tezosentan, an endothelin receptor antagonist, limits liver injury in endotoxin challenged cirrhotic
Tezosentan
Increased blood pressure in lung arteries
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
Pulmonary_hypertension
Physiological processes of hypertension
of baroreceptor discharge by endothelin at high carotid sinus pressure". The American Journal of Physiology. 263 (1 Pt 2): R103–8. doi:10.1152/ajpregu
Pathophysiology of hypertension
Pathophysiology_of_hypertension
Protein family
The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi heterotrimeric G-protein. It consists
Alpha-2_adrenergic_receptor
Endocrine gland in the brain of most vertebrates
2004). "Cellular distribution of the endothelin system in the human brain". Journal of Chemical Neuroanatomy. 27 (2): 87–98. doi:10.1016/j.jchemneu.2003
Pineal_gland
Medical condition
hormones; angiotensin II, endothelin-1 and the catecholamines (e.g. noradrenaline).[citation needed] Angiotensin-II and endothelin-1 are hormones that bind
Right_ventricular_hypertrophy
Human blood group classification
endopeptidase which is encoded by the gene KEL, and is responsible for cleaving endothelin-3. The KEL gene encodes a type II transmembrane glycoprotein that is the
Kell_antigen_system
Chemical compound
experimental anti-cancer drug candidate in development by AstraZeneca. It is an endothelin receptor antagonist. Zibotentan was granted fast track status for the
Zibotentan
Protein and coding gene in humans
within pharyngeal arch 1 through ectoderm-mesenchyme signaling via the endothelin-Dlx5/6 pathway. In dogs, a variant on the Rspo2 gene is associated moustache
R-spondin_2
Medical condition
4A is an extremely rare congenital disorder caused by a mutation in an endothelin receptor gene. It results in common Waardenburg syndrome symptoms such
Waardenburg_syndrome_type_4A
Chemical compound
enzyme thermolysin, of the membrane metallo-endopeptidase, and of the endothelin converting enzyme. Chemically, phosphoramidon differs from its closely
Phosphoramidon
Medical condition
prostacyclin and thromboxane (from Kupffer cells) or nitric oxide (NO) and endothelin-1 (ET-1). ET-1 is the most potent vasoconstrictor under investigation
Portopulmonary_hypertension
Human chromosome
alpha 2 DES: Desmin protein DIS3L2: DIS3 mitotic control homolog-like 2 ECEL1: Endothelin converting enzyme like 1 EPC2: Enhancer of polycomb homolog 2 EPB41L5:
Chromosome_2
Mammalian protein found in humans
The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor that binds epinephrine (adrenaline)
Beta-2_adrenergic_receptor
Autoimmune diseases of the skin
dysregulation of the renin–angiotensin system, elevated blood levels of endothelin 1, and increased oxidative stress. The number of new cases of the heart
Psoriasis
Swiss biopharmaceutical company
treatment. Actelion scientists were among the first to work in the field of endothelin receptor antagonists. Actelion was initially financed with venture capital
Actelion
Type of pharmaceutical drug
Adenosine reuptake inhibitor (AdoRI) Angiotensin II receptor antagonist Endothelin receptor antagonist NK1 receptor antagonist Vasopressin receptor antagonist
Reuptake_modulator
Disorder of depression and mood episodes
signaling, cardiac hypertrophy signaling, Wnt signaling, Notch signaling, and endothelin 1 signaling. Of the 16 genes identified in these pathways, three were
Bipolar_disorder
Class of drugs used to treat high blood pressure
inhibition Bosentan belongs to a new class of drugs and works by blocking endothelin receptors. It is specifically indicated only for the treatment of pulmonary
Antihypertensive
inhibitor) Azabon Apricoxib (COX-2 inhibitor) Celecoxib (COX-2 inhibitor) Parecoxib (COX-2 inhibitor) Bosentan (endothelin receptor antagonist) Diazoxide
List_of_sulfonamides
Group of autoimmune diseases resulting in abnormal growth of connective tissue
decrease collagen degradation and increase extracellular matrix production. Endothelin signalling is implicated in the pathophysiology of fibrosis. Vitamin D
Scleroderma
Chemical compound
PMID 12297490. Maguire JJ, Davenport AP (Nov 2002). "Is urotensin-II the new endothelin?". British Journal of Pharmacology. 137 (5): 579–88. doi:10.1038/sj.bjp
Urotensin-II
Protein-coding gene in the species Homo sapiens
S2CID 447070. Miller CT, Yelon D, Stainier DY, Kimmel CB (April 2003). "Two endothelin 1 effectors, hand2 and bapx1, pattern ventral pharyngeal cartilage and
NKX3-2
Medication
nephropathy and focal segmental glomerulosclerosis. Sparsentan is an endothelin and angiotensin II receptor antagonist. It is taken by mouth. The most
Sparsentan
Chemical compound
Mechanisms for Contraction to Angiotensin II and Endothelin-1". Journal of the American Society of Hypertension. 3 (2): 84–95. doi:10.1016/j.jash.2008.09.002.
Fimasartan
Compounds that bind to and activate adrenergic beta-2 receptors
development of β2 agonists β3-adrenergic agonist Hsu E, Bajaj T (2022). "Beta 2 Agonists". StatPearls. Treasure Island (FL): StatPearls Publishing. PMID 31194406
Beta2-adrenergic_agonist
Chemical compound
Darusentan (LU-135252; HMR-4005) is an endothelin receptor antagonist. Gilead Colorado, a subsidiary of Gilead Sciences, under license from Abbott Laboratories
Darusentan
Drugs blocking alpha-2 adrenergic receptors
Alpha-2 blockers (or α2 blockers) are a subset of the alpha blocker class of drugs and are antagonists to the α2 adrenergic receptor. They are mainly
Alpha-2_blocker
Protein-coding gene in the species Homo sapiens
Parathyroid hormone 2 receptor is a protein that in humans is encoded by the PTH2R gene. The protein encoded by this gene is a member of the G protein-coupled
Parathyroid hormone 2 receptor
Parathyroid_hormone_2_receptor
Protein-coding gene in the species Homo sapiens
Hydroxycarboxylic acid receptor 3 (HCA3), also known as niacin receptor 2 (NIACR2) and GPR109B, is a protein which in humans is encoded by the HCAR3 gene
Hydroxycarboxylic acid receptor 3
Hydroxycarboxylic_acid_receptor_3
Compound that increases the activity of a protein
Adenosine reuptake inhibitor (AdoRI) Angiotensin II receptor antagonist Endothelin receptor antagonist NK1 receptor antagonist Vasopressin receptor antagonist
Enzyme_inducer
Substance that binds to a receptor to change its response to stimuli
a receptor. One is its capability or incapability to activate a receptor (2 possibilities). The other two are agonist affinity and efficacy. They may
Allosteric_modulator
Chemical compound
"Development of a Scalable Process for CI-1034, an Endothelin Antagonist". Organic Process Research & Development. 8 (2): 201–212. doi:10.1021/op034104g. Chinchilla
Bis(triphenylphosphine)palladium chloride
Bis(triphenylphosphine)palladium_chloride
Ballooning or rupturing of a blood vessel in the brain
perlecan, elastin, collagen type 1 A2, endothelial nitric oxide synthase, endothelin receptor A and cyclin dependent kinase inhibitor. Recently, several genetic
Intracranial_aneurysm
Mammalian protein found in humans
The cannabinoid receptor 2 (CB2) is a G protein-coupled receptor from the cannabinoid receptor family that in humans is encoded by the CNR2 gene. It is
Cannabinoid_receptor_2
Protein-coding gene in humans
Endothelin B receptor-like protein 2 is a protein that in humans is encoded by the GPR37L1 gene. GRCh38: Ensembl release 89: ENSG00000170075 – Ensembl
GPR37L1
Type of medication
disorder: drugs and implications". Military Medical Research. 2 24. doi:10.1186/s40779-015-0053-2. ISSN 2095-7467. PMC 4620711. PMID 26504586. Kaplan HI, Sadock
Sympatholytic
Narrowing of blood vessels due to the constriction of smooth muscle cells
Chamber". Annals of Allergy, Asthma & Immunology. 102 (2): 116–120. doi:10.1016/s1081-1206(10)60240-2. PMID 19230461. Halberstadt, Adam L. (2017). "Pharmacology
Vasoconstriction
Chemical compound
of endothelin (ET) on the endothelin-A (ETA) receptor selectively (by a factor of 6000 compared with the ETB). It is a sulfonamide class endothelin receptor
Sitaxentan
Inner layer of blood vessel
been shown to release local chemicals called endothelins which are powerful vasoconstrictors. Endothelins help to regulate capillary exchange and alter
Tunica_intima
Impaired function of the inner lining of blood/lymph vessels
stress by releasing mediators, such as nitric oxide, prostacyclin and endothelin, and by controlling local angiotensin-II activity. Dysfunctional endothelium
Endothelial_dysfunction
Birth defect in which the intestine lacks certain nerves
Metallinos DL, Bowling AT, Rine J (Jun 1998). "A missense mutation in the endothelin-B receptor gene is associated with Lethal White Foal Syndrome: an equine
Hirschsprung's_disease
Mammalian protein found in humans
receptor also known as the melanocortin receptor 2 or MC2 receptor is a type of melanocortin receptor (type 2) which is specific for ACTH. A G protein–coupled
ACTH_receptor
Protein-coding gene in the species Homo sapiens
Protease activated receptor 2 (PAR2) also known as coagulation factor II (thrombin) receptor-like 1 (F2RL1) or G-protein coupled receptor 11 (GPR11) is
Protease-activated_receptor_2
Subclass of purinergic P2 receptors
). Cleveland, OH: Elsevier Inc. pp. 375–378. doi:10.1016/B978-0-12-378630-2.00350-9. ISBN 978-0-12-378631-9. Zhang K, Zhang J, Gao ZG, Zhang D, Zhu L
P2Y_receptor
Measurable indicators of diabetes
therapeutic targets for patients with prediabetes or Type 2 diabetes mellitus. Oxytocin (OXT) Omentin Endothelin-1 Nesfatin-1 Irisin Betatrophin Hepatocyte growth
Biomarkers_of_diabetes
transporters and dopaminergic activity". Journal of Neurochemistry. 116 (2): 164–176. doi:10.1111/j.1471-4159.2010.07109.x. PMC 3005101. PMID 21073468
Reverse_transport
Genetic condition involving hearing loss and depigmentation
American Paint Horses by phenotype, brainstem auditory-evoked responses, and endothelin receptor B genotype". Journal of the American Veterinary Medical Association
Waardenburg_syndrome
Small arteries in the microcirculation
hormones influence arteriole tone such as angiotensin II (vasoconstrictive), endothelin (vasoconstrictive), bradykinin (vasodilation), atrial natriuretic peptide
Arteriole
British scientist
Vane's work focused on selective inhibitors of COX-2, and the interplay between nitric oxide and endothelin in the regulation of vascular function. Vane was
John_Vane
Indian biophysicist (born 1944)
targets such as phospholipase A2, cyclooxygenase, lipoxygenase, endothelin receptor, endothelin converting enzyme, breast cancer regression proteins and matrix
Tej_P._Singh
Protein-coding gene in the species Homo sapiens
Trace amine-associated receptor 2 (TAAR2), formerly known as G protein-coupled receptor 58 (GPR58), is a protein that in humans is encoded by the TAAR2
TAAR2
Measure of relative response to a drug
Stephenson". Pharmacology Hall of Fame. British Pharmacological Society. 2 June 2016. Brunton L, Chabner BA, Knollman B (2011). Goodman and Gilman's
Intrinsic_activity
Chemical compound
(1996). "2,4-Diarylpyrrolidine-3-carboxylic AcidsPotent ETASelective Endothelin Receptor Antagonists. 1. Discovery of A-127722". Journal of Medicinal
Piperonal
G protein-coupled receptor
antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl)ethyl]-4-[4-(2-methoxynaphthalen-1-yl)butyl]piperazine), a
Melanocortin_receptor
Protein-coding gene in the species Homo sapiens
Vasopressin receptor 2 (V2R), or arginine vasopressin receptor 2 (officially called AVPR2), is a protein that acts as receptor for vasopressin. AVPR2
Vasopressin_receptor_2
Adenosine reuptake inhibitor (AdoRI) Angiotensin II receptor antagonist Endothelin receptor antagonist NK1 receptor antagonist Vasopressin receptor antagonist
Melatonergic
Protein-coding gene in the species Homo sapiens
channels by endothelin-1". Journal of Molecular Medicine. 84 (1): 46–56. doi:10.1007/s00109-005-0707-8. PMID 16258766. S2CID 2081384. Kir2.2+channel at
KCNJ12
Medical condition
dobesilate and aldose reductase inhibitors in diabetic microangiopathies and endothelin receptor antagonists for pulmonary hypertension. "microangiopathy" at
Microangiopathy
Protein-coding gene in the species Homo sapiens
TAS2R16 (taste receptor, type 2, member 16) is a bitter taste receptor and one of the 25 TAS2Rs. TAS2Rs are receptors that belong to the G-protein-coupled
TAS2R16
Medical condition
ischemia and pulmonary hypertension in Raynaud's phenomenon, and the endothelin receptor antagonist bosentan is used to manage severe pulmonary hypertension
Raynaud_syndrome
Organ found in humans and other animals
with a thin layer of connective tissue. The endocardium, by secreting endothelins, may also play a role in regulating the contraction of the myocardium
Heart
Pseudogene in the species Homo sapiens
Taste 2 receptor member 12 is a pseudogene that in humans is encoded by the TAS2R12P gene. Taste receptor "Human PubMed Reference:". National Center for
TAS2R12P
Protein found in humans
blood sugar level and around a 20 percent elevated risk of developing type 2 diabetes. MTNR1B mRNA is expressed in human islets, and immunocytochemistry
Melatonin_receptor_1B
Species of fungus
Psilocybe cubensis and Panaeolus cyanescens magic mushroom extracts on endothelin-1-induced hypertrophy and cell injury in cardiomyocytes". Scientific Reports
Psilocybe_cubensis
Protein-coding gene in the species Homo sapiens
which is inhibited by SP1. BMPER is inhibited by endothelin-1, which may be mediated by endothelin inhibition of KLF15. GRCh38: Ensembl release 89: ENSG00000164619
BMP binding endothelial regulator
BMP_binding_endothelial_regulator
Enkephalin Peptide Kidney Chromaffin cells Opioid receptor Regulate pain 24 Endothelin Peptide Vascular endothelium Endothelial cells ET receptor Smooth muscle
List_of_human_hormones
Protein-coding gene in the species Homo sapiens
Taste receptor 2 member 38 is a protein that in humans is encoded by the TAS2R38 gene. TAS2R38 is a bitter taste receptor; varying genotypes of TAS2R38
TAS2R38
Protein-coding gene in the species Homo sapiens
Prostaglandin E2 receptor 2, also known as EP2, is a prostaglandin receptor for prostaglandin E2 (PGE2) encoded by the human gene PTGER2: it is one of
Prostaglandin_EP2_receptor
Pharmaceutical compound
Stewart K, Czopek A, Menzies RI, Thomson A, Moran CM, et al. (May 2020). "Endothelin-1 Mediates the Systemic and Renal Hemodynamic Effects of GPR81 Activation"
AZ'5538
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ENDOTHELIN 2
ENDOTHELIN 2
ENDOTHELIN 2
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ENDOTHELIN 2
ENDOTHELIN 2
ENDOTHELIN 2
ENDOTHELIN 2
ENDOTHELIN 2
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