Endothelin@ 25–new agonists, antagonists, inhibitors and emerging research frontiers: IUPHAR R eview 12

JJ Maguire, AP Davenport - British journal of pharmacology, 2014 - Wiley Online Library
Since the discovery of endothelin (ET)‐1 in 1988, the main components of the signalling
pathway have become established, comprising three structurally similar endogenous 21 …

Endothelin

AP Davenport, KA Hyndman, N Dhaun, C Southan… - Pharmacological …, 2016 - ASPET
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

AP Davenport, JJ Maguire - The Vascular Endothelium I, 2006 - Springer
In humans, the endothelins (ETs) comprise a family of three 21-amino-acid peptides, ET-1,
ET-2 and ET-3. ET-1 is synthesised from a biologically inactive precursor, Big ET-1, by an …

Endothelin receptor antagonists: an overview of their synthesis and structure-activity relationship

J Iqbal, R Sanghi, SK Das - Mini Reviews in Medicinal …, 2005 - ingentaconnect.com
Endothelins (ETs) are potent vasoconstrictor peptides and are associated with several
disease states like pulmonary hypertension, systemic hypertension and heart failure …

The endothelin system as a therapeutic target in cardiovascular disease: great expectations or bleak house?

NS Kirkby, PWF Hadoke, AJ Bagnall… - British journal of …, 2008 - Wiley Online Library
There is considerable evidence that the potent vasoconstrictor endothelin‐1 (ET‐1)
contributes to the pathogenesis of a variety of cardiovascular diseases. As such …

Endothelins and endothelin receptor antagonists: therapeutic considerations for a novel class of cardiovascular drugs

TF Luscher, M Barton - Circulation, 2000 - Am Heart Assoc
The 21-amino acid peptide endothelin-1 (ET-1) is the predominant isoform of the endothelin
peptide family, which includes ET-2, ET-3, and ET-4. It exerts various biological effects …

Endothelin: setting the scene in PAH

J Dupuis - European Respiratory Review, 2007 - Eur Respiratory Soc
Endothelin (ET), a 21-amino acid peptide secreted by the vascular endothelial cells, is
frequently reported to be one of the most potent vasoconstrictors. ET induces endothelial …

Endothelin‐1 and endothelin receptor antagonists as potential cardiovascular therapeutic agents

A Ergul - … : The Journal of Human Pharmacology and Drug …, 2002 - Wiley Online Library
Endothelin (ET)‐1 is an endothelium‐derived peptide with potent vasoconstrictor and
proliferative properties. The ET system is activated in several cardiovascular disease states …

Endothelin: new discoveries and rapid progress in the clinic

DJ Webb, JC Monge, TJ Rabelink… - Trends in pharmacological …, 1998 - cell.com
Meeting REPORT demonstrating that ETB receptor stimulation by sarafotoxin 6c (S6c) can
also increase the secretion of adrenomedullin, a circulating vasodilatory and natriuretic …

Endothelins in cardiovascular biology and therapeutics

N Dhaun, DJ Webb - Nature Reviews Cardiology, 2019 - nature.com
Cardiovascular disease is a major contributor to global morbidity and mortality and is the
common end point of many chronic diseases. The endothelins comprise three structurally …