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Endothelins—from receptors to medicine
Trends in Pharmacological Sciences, 1993Since the discovery of endothelins, peptides with exceptional vasoconstrictor potency that were originally suggested to act by causing the opening of Ca2+ channels, it has emerged that these agents are important in intercellular communication in many tissues.
R.C. Miller, J.T. Pelton, J.P. Huggins
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Endothelins and endothelin receptor antagonists: Binding to plasma proteins
Life Sciences, 1996Endothelins (ET) are 21-amino acid peptides that bind to membrane receptors to initiate a wide range of pathophysiological effects. PD-156707, L-749329, Ro-470203, and A-127722 are potent non-peptide ET receptor antagonists developed recently. When tested in human and rat plasma, both ET-1 and -3 and the four aforementioned antagonists exhibited a high
Jinshyun R. Wu-Wong +5 more
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Role of endothelin and endothelin receptor antagonists in renal disease
European Journal of Clinical Investigation, 2006AbstractEndothelin (ET)‐1 is a potent vasoconstrictor peptide with pro‐inflammatory, mitogenic, and pro‐fibrotic properties that is closely involved in both normal renal physiology and pathology. ET‐1 exerts a wide variety of biological effects, including constriction of cortical and medullary vessels, mesangial cell contraction, stimulation of ...
W. Neuhofer, D. Pittrow
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Pharmacology of Renal Endothelin Receptors
2011Endothelin (ET)-1 is the major isoform in the human kidney where it interacts with two G protein-coupled receptors, ET(A) and ET(B). It contains high densities of ET receptors, but in contrast to most other peripheral organs, the majority (70%) are of the ET(B) subtype and largely have a differential distribution to ET(A) receptors within renal cells ...
Janet J. Maguire, Anthony P. Davenport
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Endothelin Receptor Antagonists
2015Endothelin-1 (ET-1) is a potent vasoconstrictor and mitogen that is secreted by the endothelium. Pulmonary vascular expression of endothelin is increased in pulmonary hypertension and plasma levels correlate with the severity of disease. Several endothelin receptor antagonists (ERAs) have been developed and are available for the treatment of pulmonary ...
Richard N. Channick +1 more
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Endothelin Receptor Antagonist
2017Endothelin (ET)-1, a peptide mainly produced by vascular endothelial cells, has potent and long-lasting vasoconstrictive effect. In addition, ET-1 has been shown to induce a variety of biological effects including cell proliferation, inflammation, and fibrosis.
Noriaki Emoto, Noriaki Emoto
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1998
Since the original discovery of endothelin (ET) by Yanagisawa et al in 1988,1 the scientific interest in this area of research has grown exponentially. It was originally hypothesized that ET interacts with two subtypes of receptors to mediate its biological functions and subsequent cloning of two ET receptors confirmed the original hypothesis.
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Since the original discovery of endothelin (ET) by Yanagisawa et al in 1988,1 the scientific interest in this area of research has grown exponentially. It was originally hypothesized that ET interacts with two subtypes of receptors to mediate its biological functions and subsequent cloning of two ET receptors confirmed the original hypothesis.
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Endothelin Receptors and Ligands
1999The discovery of endothelin led to a huge body of research, much of it aimed at elucidating the receptors through which the endothelins act. Clearly, it was reasoned, the ability to antagonise the effects of such a powerful vasoconstrictor could be of potential benefit in a number of disease states.
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