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Endothelin receptor antagonists [PDF]
Pharmacology & Therapeutics, 2006 Endothelin receptor antagonists (ERAs) have been developed to block the effects of endothelin-1 (ET-1) in a variety of cardiovascular conditions. ET-1 is a powerful vasoconstrictor with mitogenic or co-mitogenic properties, which acts through the stimulation of 2 subtypes of receptors [endothelin receptor subtype A (ETA) and endothelin receptor subtype
Robert Naeije
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Endothelin Receptor Antagonists in Cancer Therapy
Cancer Investigation, 2007Endothelins are a family of peptide compounds which exert regulatory control over cellular processes important for growth, survival, invasion, and angiogenesis. In particular, endothelin-1, acting primarily through the endothelin-A receptor, is implicated in the neoplastic growth of multiple tumor types.
Douglas G Mcneel +2 more
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The renoprotective potential of endothelin receptor antagonists
Expert Opinion on Investigational Drugs, 2000The endothelin system has been identified as having a substantial role in renal failure, both acute and chronic. Beside its well characterised haemodynamic effects, its mitogenic and pro-fibrotic properties have gained increased interest in the pathophysiology of chronic renal failure.
Claude Braun, Peter Rohmeiss, T Knoll
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Endothelin receptor antagonists
World Journal of Urology, 2005Hormone refractory prostate cancer remains true to its middle name: it is largely refractory to attempts to delay its progression. New targets and new therapies are demanded. Through a review of the available literature on endothelin and several preclinical observations, the endothelin axis has emerged as one such target.
Michael, Kirchengast, Matthias, Luz
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The endothelin system and endothelin receptor antagonists
Current Opinion in Nephrology & Hypertension, 2012There is increasing evidence that endothelin receptor blockade and, in particular, ET(A) receptor blockade not only confers protection against proteinuric renal disease in diabetes but also confers vasculoprotection.Recent clinical trials using ET(A) receptor blockade in treating proteinuria and chronic kidney disease as well as atherosclerosis show ...
Karin A M, Jandeleit-Dahm +1 more
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Peptoids as endothelin receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2001A series of new peptoids as endothelin receptor antagonists has been synthesized. Screening them for their ability to bind with endothelin receptors (ET(A) and ET(B)) competitively in the presence of (125I) endothelin led to the discovery of compounds as possible leads with IC50s in the low micromolar concentrations.
F, Dasgupta +5 more
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Endothelin Receptor Antagonists - An Overview
Current Medicinal Chemistry, 2002In thirteen years since the appearance of Endothelin (ET) on the international scene, possibility of its involvement in a variety of diseases has attracted the attention of medicinal chemists in search of novel therapeutics for various cardiovascular diseases (CVDs).
Falguni, Dasgupta +2 more
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Endothelin Receptor Antagonists
2013Three pathways have been identified in the pathogenesis of pulmonary arterial hypertension (PAH): the endothelin (ET), nitric oxide (NO) and prostacyclin pathways. These pathways represent the targets of approved PAH therapies and their discovery has facilitated significant progress in the understanding and treatment of PAH.
Martine, Clozel +2 more
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Endothelin receptor antagonist for subarachnoid haemorrhage
Cochrane Database of Systematic Reviews, 2010A subarachnoid hemorrhage (SAH) is a serious and potentially life-threatening condition where blood leaks out of blood vessels over the surface of the brain. Delayed ischemic neurological deficit (DIND) and the related feature of vasospasm, where patients experience a delayed deterioration, have long been recognized as the leading potentially treatable
Jia, Guo +4 more
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Endothelin, endothelin receptors, and endothelin antagonists
Current Opinion in Nephrology and Hypertension, 1994Endothelin is a peptide with potent biologic effects in vascular and nonvascular cells. Its effects are mediated by two receptors, ETA and ETB, and possibly also by a third receptor, ETC. In vascular smooth muscle cells, endothelin causes profound contraction and also has proliferative effects, mainly through activation of ETA but also through ETB ...
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