Structural basis of peptide recognition and activation of endothelin ...
网页2023年3月7日 · Nature Communications - Endothelin receptors (ETAR and ETBR) are critical for vasoregulation and are targets for cardiovascular diseases treatment. Here, the authors offer a structural basis...
Endothelin receptor - Wikipedia
网页There are at least four known endothelin receptors, ET A, ET B1, ET B2 and ET C, [1] all of which are G protein-coupled receptors whose activation result in elevation of intracellular-free calcium, [2] which constricts the smooth muscles of the blood vessels, raising blood pressure, or relaxes the smooth muscles of the blood vessels, lowering ...
Endothelins and Endothelin Receptor Antagonists | Circulation
网页Abstract —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, including vasoconstriction and the stimulation of cell proliferation in tissues both within and outside of the cardiovascular system.
Endothelin Receptors and Their Antagonists - PMC - National …
网页The endothelin receptors are members of the Family A G-protein–coupled receptors, a class of proteins that has been exploited very successfully as targets for the development of drugs. The human kidney is unusual among the peripheral organs in expressing a high density of ET B .
Physiology, Endothelin - StatPearls - NCBI Bookshelf
网页2023年5月1日 · Endothelin is a 21-amino acid long peptide that is a vasoconstrictor produced from endothelial cells, vascular smooth muscle cells (VSMC), macrophages, and the renal medulla. They are known to produce endothelin-1 (ET-1) that acts on the receptors ETA and ETB.
Endothelin: 30 Years From Discovery to Therapy | Hypertension
网页2019年11月4日 · More than 30 000 scientific articles on endothelin were published over the past 3 decades, leading to the development and subsequent regulatory approval of a new class of therapeutics—the endothelin receptor antagonists (ERAs). This article reviews the history of the discovery of endothelin and its role in genetics, physiology, and disease.
Endothelins in cardiovascular biology and therapeutics
网页2019年3月13日 · Endothelin 1 (ET-1) and ET-2 activate two G protein-coupled receptors — endothelin receptor type A (ET A) and endothelin receptor type B (ET B) — with equal affinity, whereas ET-3 has a...
Structural basis of antagonist selectivity in endothelin receptors
网页2024年7月30日 · Therapeutically targeting endothelin receptors, particularly through ETA antagonists, has shown efficacy in treating pulmonary arterial hypertension (PAH) and other cardiovascular- and renal ...
Endothelin receptors and their antagonists - PubMed
网页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 ….
Endothelin receptor signaling: new insight into its regulatory ...
网页The endothelin (ET) system consists of two G protein coupled-receptors (GPCRs), ET type A receptor (ETAR) and ET type B receptor (ETBR), and three endogenous ligands, ET-1, ET-2, and ET-3. Stimulation of ETRs with ET-1 induces an increase in intracellular Ca (2+) concentration that is involved in a d ….