Endothelin Receptor B Antibodies
ETB receptors couple to Gq and Gi. Coupling to Gs occurs through the second and third intracellular loops of the receptor. In order to couple with Gi through the third intracellular loop, palmitoylation of the C-terminal cysteine residues is important. BQ788 (peptides) and Ro 46-8443 (non-peptide) are selective ETB receptor antagonists. 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).