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*  Atrasentan
It is an endothelin receptor antagonist selective for subtype A (ETA). While other drugs of this type (sitaxentan, ambrisentan ... an Endothelin A Receptor Antagonist, in Combination with Paclitaxel and Carboplatin as First-Line Therapy in Advanced Non-Small ... atrasentan blocks endothelin induced cell proliferation.[citation needed] In April 2014, de Zeeuw et al. showed that 0.75 mg ... "The endothelin antagonist atrasentan lowers residual albuminuria in patients with type 2 diabetic nephropathy". Journal of the ...
*  Endothelin receptor
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 antagonist Walter F. Boron, Emile L. Boulpaep, eds. (2009). Medical physiology a cellular and molecular ... Update on endothelin receptor nomenclature". Pharmacol. Rev. 54 (2): 219-26. doi:10.1124/pr.54.2.219. PMID 12037137. Hynynen MM ...
*  Endothelin receptor antagonist
A endothelin receptor antagonist (ERA) is a drug that blocks endothelin receptors. Three main kinds of ERAs exist: selective ... Edonentan is an endothelin receptor antagonist drug. Endothelin receptor antagonists. ... which affect both endothelin A and B receptors. selective ETB receptor antagonists (BQ-788 and A192621) which affect endothelin ... ETA receptor antagonists (sitaxentan, ambrisentan, atrasentan, BQ-123, zibotentan), which affect endothelin A receptors. dual ...
*  Endothelin A receptor
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 ... Shraga-Levine Z, Sokolovsky M (June 2000). "Functional coupling of G proteins to endothelin receptors is ligand and receptor ... EDNRA endothelin receptor type A". Lee HJ, Chun M, Kandror KV (May 2001). "Tip60 and HDAC7 interact with the endothelin ...
*  Endothelin B receptor
Endothelin receptor type B, also known as ETB is a protein that in humans is encoded by the EDNRB gene. Endothelin receptor ... "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 ...
*  Zibotentan
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 ...
*  Ambrisentan
... is an endothelin receptor antagonist, and is selective for the type A endothelin receptor (ETA). Ambrisentan significantly ... As such, endothelin receptor antagonists such as Ambrisentan are known to be teratogenic. Ambrisentan has a high risk of liver ... Endothelin receptor activation mediates strong pulmonary vasoconstriction and positive inotropic effect on the heart. These ... In addition to this, endothelin receptors are also known to play a role in neural crest cell migration, growth, and ...
*  Darusentan
... (LU-135252; HMR-4005) is an endothelin receptor antagonist. Gilead Colorado, a subsidiary of Gilead Sciences, under ...
*  Oxidation of primary alcohols to carboxylic acids
"Practical Asymmetric Synthesis of an Endothelin Receptor Antagonist". J. Org. Chem. 64 (26): 9658. doi:10.1021/jo991292t. ...
*  ABCD syndrome
It has been found to be caused by mutation in the endothelin B receptor gene (EDNRB). ABCD syndrome is defined as albinism, ... The endothelin receptor B produces Waardenburg syndrome type IV. Researchers began discussing the possibility that ABCD ... New findings introduced an important break in the beliefs about ABCD syndrome because the endothelin B gene is a gene involved ... April 2008). "Epistatic connections between microphthalmia-associated transcription factor and endothelin signaling in ...
*  Lethal white syndrome
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 ...
*  BQ-123
... is a selective ETA endothelin receptor antagonist. As such, it is used as a biochemical tool in the study of endothelin ... "Cyclic pentapeptide endothelin antagonists with high ETA selectivity. Potency- and solubility-enhancing modifications". Journal ... receptor function. BQ-123 at Sigma-Aldrich Ishikawa, Kiyofumi; Fukami, Takehiro; Nagase, Toshio; Fujita, Kagari; Hayama, ...
*  Streptomyces misakiensis
Ihara, M; Fukuroda, T; Saeki, T; Nishikibe, M; Kojiri, K; Suda, H; Yano, M (15 July 1991). "An endothelin receptor (ETA) ... Streptomyces 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 ...
*  Sarafotoxin
... and thus activate endothelin-receptors, endothelin receptor type A (ETA) and endothelin receptor type B (ETB). These receptors ... doi:10.1016/s0041-0101(97)00019-6. L├╝scher, Thomas F.; Barton, Matthias (2000-11-07). "Endothelins and Endothelin Receptor ... "Molecular characterization of endothelin receptors". Trends in Pharmacological Sciences. 13: 103-108. doi:10.1016/0165-6147(92) ... ETB receptors bind ETs and SRTXs with little selectivity whereas ETA receptors show greater affinity for ET-1, ET-2 and SRTX-b ...
*  Piperonal
4-Diarylpyrrolidine-3-carboxylic AcidsPotent ETASelective Endothelin Receptor Antagonists. 1. Discovery of A-127722". Journal ...
*  Macitentan
Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial ... Macitentan is a dual ERA, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB. However ... ET receptors are G protein coupled receptors and, when activated, lead to an increase in intracellular calcium levels via the G ... Macitentan (trade name Opsumit) is an endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial ...
*  GPR37
"Entrez Gene: GPR37 G protein-coupled receptor 37 (endothelin receptor type B-like)". Imai Y, Soda M, Hatakeyama S, Akagi T, ... Zeng Z, Su K, Kyaw H, Li Y (1997). "A novel endothelin receptor type-B-like gene enriched in the brain". Biochem. Biophys. Res ... Probable G-protein coupled receptor 37 is a protein that in humans is encoded by the GPR37 gene. GPR37 has been shown to ... It was previously thought to be a receptor for head activator, a neuropeptide found in the hydra, but early reports of head ...
*  Actelion
It is a dual endothelin receptor antagonist, see also: Endothelin receptor antagonist. Zavesca (miglustat): is currently the ... Actelion scientists were among the first to work in the field of endothelian receptor antagonists. The company name might be a ... the company established the Actelion Endothelin Research Award programme which supports selected clinical research projects. In ... reminder for its first product, an endothelian receptor antagonist and the verb "action", "act upon". Actelion was initially ...
*  Riociguat
Endothelin receptor antagonist, another class of drugs used in PAH "Background Riociguat". Bayer HealthCare. Archived from the ...
*  Quinone methide
It has potent activity as an endothelin receptor antagonist and anti-osteoporosis agent. Elansolid A3 is a quinone methide from ...
*  Hermann Mucke (bioscientist)
Small-molecule endothelin receptor antagonists: a review of patenting activity across therapeutic areas. IDrugs 12(6): 366-75 ( ... Sitaxentan for the Oral Treatment of Pulmonary Arterial Hypertension: Benefits from Endothelin Receptor Subtype Selectivity? ... and endothelin receptor antagonists. By 2009 Hermann Mucke had authored or co-authored about 50 peer reviewed original research ...
*  Kendomycin
It has potent activity as an endothelin receptor antagonist and anti-osteoporosis agent. It also has strong cytotoxicity ...
*  Tezosentan
... an endothelin receptor antagonist, limits liver injury in endotoxin challenged cirrhotic rats". Gut. BMJ Publishing Group Ltd ... Tezosentan is a non-selective ETA and ETB receptor antagonist. It acts as a vasodilator and was designed as a therapy for ...
*  GNAI2
"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 ...
*  Portopulmonary hypertension
Endothelin-1 has two receptors in the pulmonary arterial tree, ET-A which mediates vasoconstriction and ET-B which mediates ... 2005;128:164-8 Wilkins et al.Sildenafil versus Endothelin Receptor Antagonist for Pulmonary Hypertension (SERAPH) study. Am J ... Use of a mixed endothelin receptor antagonist in portopulmonary hypertension: a safe and effective therapy? Gastroenterology. ... Bosentan is a nonspecific endothelin-receptor antagonist capable of neutralizing the most identifiable cirrhosis associated ...
*  Tej P. Singh
... endothelin receptor, endothelin converting enzyme, breast cancer regression proteins and matrix metanosomal proteins as well as ... exploited for making specific peptides to act as tight inhibitors of target enzymes and potent antagonists of target receptors ...