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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).
Ashis K. Mukherjee +2 more
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Endothelin Receptor Antagonism
1995Following the original report by Yanagisawa et al. (1988) more than 7 years ago, compelling evidence that ET plays an important role in the local regulation of smooth muscle tone and cell growth has been reported. In addition, many studies point to a significant role for endothelin in nonvascular function. The investigation of the endothelin system has
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Effect of castration on endothelin receptors
Clinical Science, 2002Endothelin (ET) plays a pivotal role in the pathogenesis of cell growth disorders such as cancer. Atrasentan (ABT-627), a selective antagonist for the ET receptor A (ETA), has shown benefit in controlling disease progression in men with hormone refractory prostate cancer who have undergone aggressive hormone ablation therapy.
Robert J. Padley +2 more
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Characterization of Endothelin Receptor Subtypes
Journal of Cardiovascular Pharmacology, 1991Scatchard-plot analysis of [125I]ET-1 and [125I]ET-3 binding to rat lung membranes exhibited almost the same Kd values whereas the concentration of the binding sites of ET-1 is approximately four times higher than that of ET-3. This result suggests the presence of at least two distinct subtypes of ET receptors: an ET-1-specific type and an ET-3 ...
Takeshi Shibata +5 more
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Endothelin Receptors and Receptor Antagonists
1998Multiple receptor subtypes for endothelin have been identified in pharmacological studies both in vitro and in vivo. As can be evidenced in the study by Yanagisawa et al, at least two receptor subtypes may be responsible for the biphasic nature of the hemodynamic response to intravenous injection of ET-1: a transient hypotension followed by a sustained
David M. Pollock, Andrew S. Tasker
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Evolution of endothelin receptors in vertebrates
General and Comparative Endocrinology, 2014Endothelin receptors are G protein coupled receptors (GPCRs) of the β-group of rhodopsin receptors that bind to endothelin ligands, which are 21 amino acid long peptides derived from longer prepro-endothelin precursors. The most basal Ednr-like GPCR is found outside vertebrates in the cephalochordate amphioxus, but endothelin ligands are only present ...
Ingo Braasch, Manfred Schartl
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Desensitization of Human Endothelin A Receptor
Journal of Cardiovascular Pharmacology, 1993The response of G-protein-coupled receptors is modulated by homologous desensitization. Because endothelin A receptor (ETA) plays a part in vasoconstriction, the extent of desensitization and resensitization of endothelin responsiveness was studied.
C. Cyr, R. M. Kris
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Endothelins and sarafotoxins: Receptor heterogeneity
International Journal of Biochemistry, 19941. Endothelins (ETs) and sarafotoxins (SRTXs) belong to a family of 21-amino-acid peptides comprising at least eight isoforms. 2. ET exerts multiple pharmacological effects through its receptors. 3. This review summarizes the observations and findings pointing to the existence of receptor subtypes and leading to their identification. 4.
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Molecular characterization of endothelin receptors
Trends in Pharmacological Sciences, 1992Following the first report on the identification of endothelin (ET), an increasing body of work has accumulated on this endothelium-derived 21-amino acid vasoconstrictor peptide. Subsequently, the existence of three distinct isoforms of ET, designated ET-1, ET-2 and ET-3, was predicted from the finding of three separate genes.
Masashi Yanagisawa +2 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.
Simi Sarin +5 more
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