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Endothelin Receptors and Pain [PDF]
The endogenous endothelin (ET) peptides participate in a remarkable variety of pain-relatedprocesses. Pain that is elevated by inflammation, by skin incision, by cancer, during a Sickle Cell Disease crisis and by treatments that mimic neuropathic and inflammatory pain and are all reduced by local administration of antagonists of endothelin receptors ...
Khodorova, Alla+2 more
openaire +5 more sources
Endothelin‐receptor interactions [PDF]
The mechanism of action of endothelin‐receptor interactions was studied, using radioligand binding assays and SDS‐PAGE, to investigate the possibility of disulfide interchange. Electrophoretic analysis suggested involvement of disulfide bond(s) in the receptor‐ligand complex.
John A. Catena+6 more
openaire +3 more sources
Affinity labelling of endothelin receptor and characterization of solubilized endothelin–endothelin‐receptor complex [PDF]
Chick cardiac membranes were affinity labelled by cross‐linking to membrane‐bound 125I‐endothelin‐1 with disuccinimidyl tartarate. SDS/PAGE and autoradiographic analysis of the 125I‐endothelin‐1‐labelled material in the presence or absence of 2‐mercaptoethanol revealed one major labelled band, corresponding to a molecular mass of 53 kDa, whose ...
Tomoh Masaki+9 more
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Truncated human endothelin receptor A produced by alternative splicing and its expression in melanoma [PDF]
In this study, reverse transcriptase polymerase chain reaction was used to amplify human endothelin receptor A (ETA) and ETB receptor mRNA. A truncated ETA receptor transcript with exons 3 and 4 skipped was found.
Berry, PA+5 more
core +1 more source
Endothelin Receptors and Their Antagonists
All three members of the endothelin (ET) family of peptides, ET-1, ET-2, and ET-3, are expressed in the human kidney, with ET-1 being the predominant isoform. ET-1 and ET-2 bind to two G-protein-coupled receptors, ETA and ETB, whereas at physiological concentrations ET-3 has little affinity for the ET(A) receptor.
Maguire, Janet J, Davenport, Anthony P
openaire +4 more sources
Endothelin-1 Predicts Hemodynamically Assessed Pulmonary Arterial Hypertension in HIV Infection. [PDF]
BackgroundHIV infection is an independent risk factor for PAH, but the underlying pathogenesis remains unclear. ET-1 is a robust vasoconstrictor and key mediator of pulmonary vascular homeostasis.
AH Chester+51 more
core +8 more sources
The role of endothelin-1 in pulmonary arterial hypertension. [PDF]
Pulmonary arterial hypertension (PAH) is a rare but debilitating disease, which if left untreated rapidly progresses to right ventricular failure and eventually death. In the quest to understand the pathogenesis of this disease differences in the profile,
Chester, AH, Yacoub, MH
core +1 more source
The current endothelin receptor classification: Time for reconsideration? [PDF]
The possible involvement of endothelins in a variety of diseases has attracted the attention of many pharmacologists in search of a novel therapeutic approach.
Bax, W.A. (Willem)+1 more
core +2 more sources
Endothelin and the ischaemic heart [PDF]
Soon after its identification as a powerful vasoconstrictor peptide, endothelin (ET-1) was implicated as a detrimental agent involved in determining the outcome of myocardial ischaemia and reperfusion.
Kane, K.A., McCabe, C., Wainwright, C.L.
core +1 more source
Clinical trials with endothelin receptor antagonists: What went wrong and where can we improve? [PDF]
In the early 1990s, within three years of cloning of endothelin receptors, orally active endothelin receptor antagonists (ERAs) were tested in humans and the first clinical trial of ERA therapy in humans was published in 1995.
Barton, Matthias+4 more
core +1 more source