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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 ...
Widely distributed in the body, receptors for endothelin are present in blood vessels and cells of the brain, choroid plexus and peripheral nerves.When applied directly to the brain of rats in picomolar quantities as an experimental model of stroke, endothelin-1 caused severe metabolic stimulation and seizures with substantial decreases in blood flow to the same brain regions, both effects ...
Masashi Yanagisawa (柳沢 正史, Yanagisawa Masashi, born May 25, 1960) is a Japanese-American molecular biologist and physician, famous for his discovery of the hormone endothelin and the neuropeptide orexin, the absence of which is the cause of narcolepsy.
Endothelin converting enzyme 1, also known as ECE1, is an enzyme which in humans is encoded by the ECE1 gene. [5] [6] [7] Function. Endothelin-converting enzyme-1 is ...
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 ...
Endothelin-converting enzyme 1 (EC 3.4.24.71, endothelin-converting enzyme, ECE-1) is an enzyme. [1] [2] [3] This enzyme catalyses the following chemical reaction. Hydrolysis of the -Trp 21-Val- bond in big endothelin to form endothelin 1. This metalloendopeptidase belongs to the peptidase family M13.
The endothelin 1 receptor is one of the strongest known vasoconstrictors. After subarachnoidal bleedings, irritation of the blood vessels can lead to a vasospasm and thus to an ischaemia, an insufficient blood supply to brain tissue. One possible effect of this is, in turn, an ischaemic stroke.