There are at least four known endothelin receptors, ETA, ETB1, ETB2 and ETC, all of which are G protein-coupled receptors whose ... 2016) 'Endothelin' Pharmacol. Rev. 68: 357-418. pmid =26956245 doi =10.1124/pr.115.011833 "Endothelin Receptors". IUPHAR ... Endothelin+receptor at the U.S. National Library of Medicine Medical Subject Headings (MeSH) v t e (Articles with short ... Endothelin receptor antagonist Walter F. Boron, Emile L. Boulpaep, eds. (2009). Medical physiology a cellular and molecular ...

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 ... which affect both endothelin A and B receptors. selective ETB receptor antagonists (BQ-788 and A192621) which affect endothelin ... which affect endothelin A receptors. dual antagonists (bosentan, macitentan, tezosentan), ...

Endothelin receptor type A, also known as ETA, is a human G protein-coupled receptor. Endothelin receptor type A has been shown ... "Endothelin Receptors: ETA". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... Han SG, Ko S, Lee WK, Jung ST, Yu YG (August 2017). "Determination of the endothelin-1 recognition sites of endothelin receptor ... Shraga-Levine Z, Sokolovsky M (June 2000). "Functional coupling of G proteins to endothelin receptors is ligand and receptor ...

... , (ET-B) is a protein that in humans is encoded by the EDNRB gene. Endothelin receptor type B is a G ... "Endothelin Receptors: ETB". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... "Phosphorylation and desensitization of human endothelin A and B receptors. Evidence for G protein-coupled receptor kinase ... "Interaction of endothelin-3 with endothelin-B receptor is essential for development of epidermal melanocytes and enteric ...

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

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 ...

Ariza AC, Bobadilla NA, Halhali A (2007). "[Endothelin 1 and angiotensin II in preeeclampsia]". Rev. Invest. Clin. 59 (1): 48- ... Bradykinin receptor B2 is a G-protein coupled receptor for bradykinin, encoded by the BDKRB2 gene in humans. The B2 receptor is ... "Bradykinin Receptors: B2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... Kallidin also signals through the B2 receptor. An antagonist for the receptor is Hoe 140 (icatibant). The 9 amino acid ...

Ariza AC, Bobadilla NA, Halhali A (2007). "[Endothelin 1 and angiotensin II in preeeclampsia]". Revista de Investigacion ... Angiotensin II receptor type 1 (AT1) is the best characterized angiotensin receptor. It is encoded in humans by the AGTR1 gene ... The angiotensin receptor is activated by the vasoconstricting peptide angiotensin II. The activated receptor in turn couples to ... "Angiotensin Receptors: AT1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ...

... is an endothelin receptor antagonist, and is selective for the type A endothelin receptor (ETA). Ambrisentan significantly ... 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 ...

... (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 ...

It acts on the endothelin receptors ETA and ETB in various cell types including vascular smooth muscle cells and fibroblasts, ... The dual (ETA and ETB) endothelin receptor antagonist bosentan was approved in 2001. Sitaxentan (Thelin) was approved for use ... Three of these pathways are important since they have been targeted with drugs - endothelin receptor antagonists, ... Moderate quality evidence suggests that endothelin receptor antagonists improve exercise capacity and decrease symptoms ...

... is a selective ETA endothelin receptor antagonist. As such, it is used as a biochemical tool in the study of endothelin ... Atkinson RA, Pelton JT (January 1992). "Conformational study of cyclo[D-Trp-D-Asp-Pro-D-Val-Leu], an endothelin-A receptor- ... Büyükgebiz O, Aktan AO, Haklar G, Yalçin AS, Yeğen C, Yalin R, Ercan ZS (1996). "BQ-123, a specific endothelin (ETA) receptor ... Clavell AL, Stingo AJ, Margulies KB, Brandt RR, Burnett JC (March 1995). "Role of endothelin receptor subtypes in the in vivo ...

Characterization of receptors". Hypertension. 19 (2): 49-55. doi:10.1161/01.hyp.19.2_suppl.ii49. PMID 1735595. Phillips, PA. " ... "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 ... Effects of angiotensin converting enzyme inhibition and angiotensin II type 1 receptor blockade". Basic Research in Cardiology ...

ET-2 acts by binding to two different G-protein coupled receptors (GPCRs), the endothelin A receptor (EDNRA) and the endothelin ... endothelin-2 and endothelin-receptor-A genotyped by four duplex assays and seven simple assays on a LightCycler using ... Grimshaw MJ, Hagemann T, Ayhan A, Gillett CE, Binder C, Balkwill FR (April 2004). "A role for endothelin-2 and its receptors in ... Ko C, Meidan R, Bridges PJ (October 2012). "Why two endothelins and two receptors for ovulation and luteal regulation?". Life ...

Most endothelin receptors in the human cerebral cortex (~90%) are of the ETB subtype. Endothelin-1 is the most powerful ... Endothelins are peptides with receptors and effects in many body organs. Endothelin constricts blood vessels and raises blood ... Endothelin functions through activation of two G protein-coupled receptors, endothelinA and endothelinB receptor (ETA and ETB, ... Endothelin-2 differs from endothelin-1 by two amino acids, and sometimes has the same affinity as endothelin-1 for ETA and ETB ...

"Practical Asymmetric Synthesis of an Endothelin Receptor Antagonist". J. Org. Chem. 64 (26): 9658. doi:10.1021/jo991292t. ...

Ihara, M; Fukuroda, T; Saeki, T; Nishikibe, M; Kojiri, K; Suda, H; Yano, M (15 July 1991). "An endothelin receptor (ETA) ... Kitasatospora misakiensis produces tubermycin A, tubermycin B, misakimycin and the endothelin receptor antagonist BE-18257B. ... "An endothelin receptor (ETA) antagonist isolated from Streptomyces misakiensis". Biochemical and Biophysical Research ... "An endothelin receptor (ETA) antagonist isolated from Streptomyces misakiensis". Biochemical and Biophysical Research ...

... is an endothelin and angiotensin II receptor antagonist. It was approved for medical use in the United States in ...

The endothelin receptor B produces Waardenburg syndrome type IV. Discovering that the same gene is involved in both ABCD and ... The syndrome is caused by mutation in the endothelin B receptor gene (EDNRB). In the beginning, medical officials defined ABCD ... April 2008). "Epistatic connections between microphthalmia-associated transcription factor and endothelin signaling in ... New findings introduced an important break in the beliefs about ABCD syndrome because the endothelin B gene is a gene involved ...

Yang GC, Croaker D, Zhang AL, Manglick P, Cartmill T, Cass D (June 1998). "A dinucleotide mutation in the endothelin-B receptor ... Metallinos DL, Bowling AT, Rine J (June 1998). "A missense mutation in the endothelin-B receptor gene is associated with Lethal ... A mutation in the middle of the endothelin receptor type B (EDNRB) gene causes lethal white syndrome when homozygous. Carriers ... Such regulatory genes include endothelin receptor type B (EDNRB). A mutation in the middle of the EDNRB gene, Ile118Lys, causes ...

... epidermal growth factor receptor, endothelin receptor type B, PDGFRB, PDGFRA, PTGS2, TRAF2, estrogen receptor alpha, caveolin 2 ... Yamaguchi T, Murata Y, Fujiyoshi Y, Doi T (April 2003). "Regulated interaction of endothelin B receptor with caveolin-1". ... TGF beta receptor 1,endothelial NOS,androgen receptor,amyloid precursor protein,gap junction protein, alpha 1,nitric oxide ... Yamamoto M, Toya Y, Jensen RA, Ishikawa Y (March 1999). "Caveolin is an inhibitor of platelet-derived growth factor receptor ...

"Increased pulmonary vascular endothelin B receptor expression and responsiveness to endothelin-1 in cirrhotic and portal ... Endothelin-1 has two receptors in the pulmonary arterial tree, ET-A which mediates vasoconstriction and ET-B which mediates ... Kuntzen, C; Gülberg, V; Gerbes, AL (January 2005). "Use of a mixed endothelin receptor antagonist in portopulmonary ... Bosentan is a nonspecific endothelin-receptor antagonist capable of neutralizing the most identifiable cirrhosis associated ...

4-Diarylpyrrolidine-3-carboxylic AcidsPotent ETASelective Endothelin Receptor Antagonists. 1. Discovery of A-127722". Journal ...

S2CID 35240781.; (g) Neuhofer W, Pittrow D (September 2006). "Role of endothelin and endothelin receptor antagonists in renal ... IKK2 RELA Toll-like receptor TNF receptor superfamily Imd pathway In other words, c-Fos repression allows ΔFosB to accumulate ... Sheikh MS, Huang Y (2003). "Death receptor activation complexes: it takes two to activate TNF receptor 1". Cell Cycle. 2 (6): ... "Crosstalk between Peroxisome Proliferator-Activated Receptors and Toll-Like Receptors: A Systematic Review". Advanced ...

These tumor-associated endothelial cells have been found to over-express the endothelin B receptor, which suppresses T-cell ... Kandalaft, Lana E.; Facciabene, Andrea; Buckanovich, Ron J.; Coukos, George (2009-07-15). "Endothelin B Receptor, a New Target ... "Endothelin B receptor mediates the endothelial barrier to T cell homing to tumors and disables immune therapy". Nature Medicine ... Loss of pericyte growth factor (PDGFB) and its receptor on endothelial cells are molecular-level changes that can account for ...

1997). "Phosphorylation and desensitization of human endothelin A and B receptors. Evidence for G protein-coupled receptor ... G protein-coupled receptor kinases phosphorylate activated G protein-coupled receptors, which promotes the binding of an ... 1998). "β2-Adrenergic receptor regulation by GIT1, a G protein-coupled receptor kinase-associated ADP ribosylation factor ... 2001). "Determination of bradykinin B2 receptor in vivo phosphorylation sites and their role in receptor function". J. Biol. ...

... is a drug belonging to the class of endothelin receptor antagonists. The endothelin 1 receptor is one of the strongest known ... Endothelin receptor antagonists, Vasodilators, Tetrazoles, Pyridines, Sulfonamides, Pyrimidines, Methoxy compounds, Diaryl ...

"Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial ... There are two receptor subtypes that endothelin will bind to: ETA and ETB. ETA is associated with cell growth and ... Macitentan is a dual ERA, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB. However ... Macitentan, sold under the brand name Opsumit, is an endothelin receptor antagonist (ERA) developed by Actelion and approved ...

It is an endothelin receptor antagonist selective for subtype A (ETA). While other drugs of this type (sitaxentan, ambrisentan ... March 2008). "Phase I/II study of atrasentan, an endothelin A receptor antagonist, in combination with paclitaxel and ... Endothelin receptor antagonists, Experimental cancer drugs, Benzodioxoles, Carboxylic acids). ... May 2014). "The endothelin antagonist atrasentan lowers residual albuminuria in patients with type 2 diabetic nephropathy". ...

1997). "Endothelin-1 and ETA receptor expression in vascular smooth muscle cells from human placenta: a new ETA receptor ... 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 ... 1991). "Chromosomal assignments of the human endothelin family genes: the endothelin-1 gene (EDN1) to 6p23-p24, the endothelin- ...

"Molecular identification of guanine-nucleotide-binding regulatory proteins which couple to endothelin receptors". European ... Offermanns S, Schultz G, Rosenthal W (Feb 1991). "Evidence for opioid receptor-mediated activation of the G-proteins, Go and ... GNAI2 has been shown to interact with: EYA2, GPSM2, Interleukin 8 receptor, alpha, MDFI, RGS5, and RIC8A. GRCh38: Ensembl ... McClue SJ, Milligan G (Sep 1990). "The alpha 2B adrenergic receptor of undifferentiated neuroblastoma x glioma hybrid NG108-15 ...

... 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 ... ETB receptors bind ETs and SRTXs with little selectivity whereas ETA receptors show greater affinity for ET-1, ET-2 and SRTX-b ... Sokolovsky M, Ambar I, Galron R (October 1992). "A novel subtype of endothelin receptors". The Journal of Biological Chemistry ...