Endothelin
University of Alabama at Birmingham · University of Edinburgh · +4 more institutions
Abstract
The endothelins comprise three structurally similar 21-amino acid peptides. Endothelin-1 and -2 activate two G-protein coupled receptors, ETA and ETB, with equal affinity, whereas endothelin-3 has a lower affinity for the ETA subtype. Genes encoding the peptides are present only among vertebrates. The ligand-receptor signaling pathway is a vertebrate innovation and may reflect the evolution of endothelin-1 as the most potent vasoconstrictor in the human cardiovascular system with remarkably long lasting action. Highly selective peptide ETA and ETB antagonists and ETB agonists together with radiolabeled analogs have accurately delineated endothelin pharmacology in humans and animal models, although surprisingly…
Citation impact
- FWCI
- 42.68
- Percentile
- 100%
- References
- 678
Authors
9- APAnthony P. DavenportCorresponding
University of Alabama at Birmingham, University of Edinburgh, University of Cambridge, Edinburgh Royal Infirmary, British Heart Foundation, University of Utah
- KAKelly A. Hyndman
British Heart Foundation, University of Edinburgh, University of Cambridge, Edinburgh Royal Infirmary, University of Alabama at Birmingham, University of Utah
- NDNeeraj Dhaun
University of Alabama at Birmingham, Edinburgh Royal Infirmary, British Heart Foundation, University of Edinburgh, University of Utah, University of Cambridge
- CSChristopher Southan
University of Edinburgh, University of Utah, British Heart Foundation, University of Alabama at Birmingham, University of Cambridge, Edinburgh Royal Infirmary
- DEDonald E. Kohan
University of Cambridge, University of Edinburgh, Edinburgh Royal Infirmary, British Heart Foundation, University of Utah, University of Alabama at Birmingham
Topics & keywords
- Endothelin receptor
- Endothelins
- Bosentan
- Pharmacology
- Ambrisentan
- Receptor
- Agonist
- Biology
- Industry, innovation and infrastructure