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 ...

... 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). "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. ...

"Entrez Gene: GPR37 G protein-coupled receptor 37 (endothelin receptor type B-like)". Bolinger AA, Frazier A, La JH, Allen JA, ... Zeng Z, Su K, Kyaw H, Li Y (April 1997). "A novel endothelin receptor type-B-like gene enriched in the brain". Biochemical and ... G protein-coupled receptors, All stub articles, Transmembrane receptor stubs). ... Probable G-protein coupled receptor 37 is a protein that in humans is encoded by the GPR37 gene. GPR37 is primarily found in ...

It is a dual endothelin receptor antagonist, see also: Endothelin receptor antagonist. Zavesca (miglustat): is currently the ... Uptravi is an oral medication that should be used along with a phosphodiesterase-5 inhibitor, an ERA(endothelin receptor ... Endothelin Receptor Antagonist) that has been used to slow down the prohibit the advancement of diseases and PAH. Actelion ... Actelion scientists were among the first to work in the field of endothelian receptor antagonists. Actelion was initially ...

Eventually, his interest in endothelin diminished and Yanagisawa switched his focus to orphan receptors, which are receptors ... 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 ... "Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor". Nature. 348 (6303): 732-735. doi: ...

... is a competitive antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors. Under normal ... endothelin-1 binding of ET-A receptors causes constriction of the pulmonary blood vessels. Conversely, binding of endothelin-1 ... June 2000). "Acute endothelin A receptor blockade causes selective pulmonary vasodilation in patients with chronic heart ... Bosentan, sold under the brand name Tracleer and Safebo among others, is a dual endothelin receptor antagonist medication used ...

It has potent activity as an endothelin receptor antagonist and anti-osteoporosis agent. Elansolid A3 is a quinone methide from ...

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 ...

It has potent activity as an endothelin receptor antagonist and anti-osteoporosis agent. It also has strong cytotoxicity ...

December 2004). "Tezosentan, an endothelin receptor antagonist, limits liver injury in endotoxin challenged cirrhotic rats". ... Endothelin receptor antagonists, Isopropyl compounds, Diaryl ethers, All stub articles, Cardiovascular system drug stubs). ... Tezosentan is a non-selective ETA and ETB receptor antagonist. It acts as a vasodilator and was designed by Actelion as a ...

"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 ...

... role of endothelin-1". Am. J. Physiol. Endocrinol. Metab. 285 (2): E390-6. doi:10.1152/ajpendo.00509.2002. PMID 12721154. ... "Glucagon Receptor Family: GIP". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... Brubaker PL, Drucker DJ (2002). "Structure-function of the glucagon receptor family of G protein-coupled receptors: the ... Tseng CC, Zhang XY (2000). "Role of G protein-coupled receptor kinases in glucose-dependent insulinotropic polypeptide receptor ...

Shraga-Levine Z, Sokolovsky M (2000). "Functional coupling of G proteins to endothelin receptors is ligand and receptor subtype ... AbdAlla S, Lother H, Abdel-tawab AM, Quitterer U (2001). "The angiotensin II AT2 receptor is an AT1 receptor antagonist". J. ... 1996). "The human thyrotropin receptor: a heptahelical receptor capable of stimulating members of all four G protein families ... Offermanns S, Simon MI (1995). "G alpha 15 and G alpha 16 couple a wide variety of receptors to phospholipase C". J. Biol. Chem ...

Bosentan belongs to a new class of drugs and works by blocking endothelin receptors. It is specifically indicated only for the ... Angiotensin II receptor antagonists work by antagonizing the activation of angiotensin receptors.[citation needed] azilsartan ... Aldosterone receptor antagonists:[citation needed] eplerenone spironolactone Aldosterone receptor antagonists are not ... On the other hand, β-blockers, diuretics, ACE inhibitors, angiotensin receptor blockers, and aldosterone receptor antagonists ...

The use of endothelin receptor antagonism could have the potential effect to be renally protective. Microalbuminuria is an ... This is because sFLT-1 prevents the binding of vascular endothelial growth factor (VEGF) to a splice variant of its receptor ( ... The hypoxia also causes the over expression of endothelin-1 and functional nitric oxide deficiency and due to the chronic ... This nitric oxide deficiency alongside endothelin-1 overproduction leads to the inability to properly respond to stress and ...

... is a small molecule that blocks the action of endothelin (ET) on the endothelin-A (ETA) receptor selectively (by a ... November 2007). "Selective endothelin A receptor antagonism with sitaxsentan for pulmonary arterial hypertension associated ... Adverse effects observed with sitaxentan are class effects of endothelin receptor antagonists, and include : liver enzyme ... an endothelin-A receptor antagonist, in patients with pulmonary arterial hypertension: open-label pilot study". Chest. 121 (6 ...

This corresponds with receptor expression at the pharyngeal arches. Pharyngeal arch 3 expresses EphrinA and EphrinB1 receptors ... A second signalling pathway that directs crest cell movement are the family of endothelin ligands. Migrating cardiac neural ...

Constriction has been shown in vitro to occur when NE is placed in the synapse and is taken up by astrocyte receptors. NE ... The peptides angiotensin II and endothelin-1 (ET-1) bind to pericytes and are vasoactive. Endothelial cells induce expression ... It has also been shown that agonists of metabotropic glutamate receptors (mGluR) also increase intracellular Ca2+ to produce ... Pericytes have both cholinergic (α2) and adrenergic (β2) receptors. Stimulation of the latter leads to vessel relaxation, while ...

RhoGDI2 suppresses endothelin 1 (ET1), a vasoconstrictor correlated with higher clinical stage in bladder cancer. CRSP3 and ... It acts by synthesizing a protein receptor. RHoGD12 is active in bladder cancer and inhibits proteins that aid in cancer cell ...

Angiotensin-II and endothelin-1 are hormones that bind to the angiotensin (AT) and endothelin (ET) receptors. These are G- ... Catecholamines can act on the alpha-adrenergic receptors and beta-adrenergic receptors which are G-protein coupled receptors. ... This binding initiates the same intracellular signalling pathways as angiotensin and endothelin. There is also activation of ... Targeting the renin-angiotensin (RAAS) system (using angiotensin-converting enzyme inhibitors and angiotensin-receptor blockers ...

The main cause of this syndrome is the mutation of the endothelin receptor type B gene (noted as EDNRB). Chandra Mohan, Setty. ... The abnormalities seen are caused in mutation such as the studied deletion of the endothelin‐B receptor gene, which is located ... Waardenburg Syndrome Type 4A is an extremely rare congenital disorder caused by a mutation in an endothelin receptor gene. It ... Syrris, Petros; Carter, Nicholas D.; Patton, Michael A. (1999). "Novel nonsense mutation of the endothelin-B receptor gene in a ...

Lee HJ, Chun M, Kandror KV (May 2001). "Tip60 and HDAC7 interact with the endothelin receptor a and may be involved in ... Lee HJ, Chun M, Kandror KV (May 2001). "Tip60 and HDAC7 interact with the endothelin receptor a and may be involved in ... "Tip60 and histone deacetylase 1 regulate androgen receptor activity through changes to the acetylation status of the receptor ... Brady ME, Ozanne DM, Gaughan L, Waite I, Cook S, Neal DE, Robson CN (Jun 1999). "Tip60 is a nuclear hormone receptor ...

... A has been shown to interact with: BCL6, Endothelin receptor type A, HDAC3, HTATIP, IKZF1, and Nuclear receptor co- ... Lee HJ, Chun M, Kandror KV (May 2001). "Tip60 and HDAC7 interact with the endothelin receptor a and may be involved in ... Lee HJ, Chun M, Kandror KV (May 2001). "Tip60 and HDAC7 interact with the endothelin receptor a and may be involved in ... This study also showed that signaling via the insulin/Insulin-like growth factor 1 receptor led to increased levels of HDAC7 in ...

Santschi EM, Vrotsos PD, Purdy AK, Mickelson JR (Jan 2001). "Incidence of the endothelin receptor B mutation that causes lethal ... "A missense mutation in the endothelin-B receptor gene is associated with Lethal White Foal Syndrome: an equine version of ...

"Endothelin B receptor mediates the endothelial barrier to T cell homing to tumors and disables immune therapy". Nature Medicine ... "A computationally designed chimeric antigen receptor provides a small-molecule safety switch for T-cell therapy". Nature ...

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 ...

Relaxin can also bind to a secondary receptor, endothelial B receptor,[clarification needed] which is upregulated as a result ... where it inhibits the potent vasoconstrictors angiotensin II and endothelin. In addition to vasodilation, the effects of ... Activation of the relaxin receptor RXFP1 activates several enzymes in a phosphorylation cascade that eventually results in the ... Relaxin binding to endothelial B receptor on endothelial cells also induces vasodilation. Relaxin causes vasodilation by an ...