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Endothelin 1 (ET-1), also known as preproendothelin-1 (PPET1), is a potent vasoconstrictor peptide produced by vascular endothelial cells, [5] as well as by cells in the heart (affecting contractility) and kidney (affecting sodium handling). [6] The protein encoded by this gene – EDN1 – is proteolytically processed to release endothelin 1.
Endothelin functions through activation of two G protein-coupled receptors, endothelin A and endothelin B receptor (ETA and ETB, respectively). [2] These two subtypes of endothelin receptor are distinguished in the laboratory by the order of their affinity for the three endothelin peptides: the ETA receptor is selective for ET-1, whereas the ETB receptor has the same affinity for all three ET ...
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 blood pressure, among other functions.
Endothelin receptor type B is a G protein-coupled receptor which activates a phosphatidylinositol-calcium second messenger system. Its ligand, endothelin, consists of a family of three potent vasoactive peptides: ET 1, ET 2, and ET 3. A splice variant, named SVR, has been described; the sequence of the ETB-SVR receptor is identical to ETRB ...
Endothelial dysfunction is a result of changes in endothelial function. [20] [21] After fat accumulation and when stimulated by inflammation, endothelial cells become activated, which is characterized by the expression of molecules such as E-selectin, VCAM-1 and ICAM-1, which stimulate the adhesion of immune cells. [22]
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If you or someone you know has been sexually assaulted, please contact the National Sexual Assault Hotline at 1-800-656-HOPE (4673) or go to rainn.org. Read the original article on People.
Treatment of hypertension and hypercholesterolemia may improve endothelial function in people taking statins (HMGCoA-reductase inhibitor), and renin angiotensin system inhibitors, such as ACE inhibitors and angiotensin II receptor antagonists. [28] [29] Calcium channel blockers and selective beta 1 antagonists may also improve endothelial ...