Endothelin Receptor B Antibodies

The endothelin type A receptor (ETₐ), encoded by EDNRA, is a class A G protein-coupled receptor with higher affinity for endothelin-1 and endothelin-2 than for endothelin-3. It signals predominantly through Gq/11, activating phospholipase C and increasing intracellular calcium, and can also engage G12/13–RhoA signaling. ETₐ is expressed predominantly in vascular smooth muscle and is also found in cardiomyocytes, fibroblasts, and several other cell types. In vascular smooth muscle, endothelin-1 activation of ETₐ produces potent, sustained vasoconstriction. Persistent ETₐ signaling can promote cell proliferation, fibrosis, and vascular remodeling. Agonist exposure can induce receptor phosphorylation, β-arrestin recruitment, and internalization, after which ETₐ can recycle to the plasma membrane. The selective ETₐ antagonist ambrisentan is used clinically to treat pulmonary arterial hypertension. Atrasentan, another selective ETₐ antagonist, is approved in the United States to reduce proteinuria in adults with primary IgA nephropathy at risk of rapid disease progression. ETB activity is regulated by phosphorylation of carboxyl-terminal serine435/serine436 (pS435/pS436-ETB). This nomenclature refers to the human ETB receptor. This phosphorylation motif is highly conserved and is identical in mice, rats and humans. For more information on ETB pharmacology please refer to the IUPHAR database. For further reading refer to:
Barton M, Yanagisawa M. Endothelin: 30 Years From Discovery to Therapy. Hypertension. 2019 Dec;74(6):1232-1265. doi: 10.1161/HYPERTENSIONAHA.119.12105.Epub 2019 Nov 4. PMID: 31679425.
Davenport AP, Hyndman KA, Dhaun N, Southan C, Kohan DE, Pollock JS, Pollock DM, Webb DJ, Maguire JJ. Endothelin. Pharmacol Rev. 2016 Apr;68(2):357-418. doi: 10.1124/pr.115.011833. PMID: 26956245; PMCID: PMC4815360.
Davenport AP, D'Orléans-Juste P, Godfraind T, Maguire JJ, Ohlstein EH, Ruffolo RR. Endothelin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database. IUPHAR/BPS Guide to Pharmacology CITE. 2019; 2019(4).