Chemistry:Endothelin 1
 Generic protein structure example |
Endothelin 1 (ET-1), also known as preproendothelin-1 (PPET1), is the most potent vasoconstrictor produced by the human body.[1] It is a peptide produced by vascular endothelial cells,[2] as well as by cells in the heart (affecting contractility) and kidney (affecting sodium handling).[3] The protein encoded by this gene – EDN1 – is proteolytically processed to release endothelin 1. Endothelin 1 is one of three isoforms of human endothelin.
Sources
Preproendothelin is precursor of the peptide ET-1. Endothelial cells convert preproendothelin to proendothelin and subsequently to mature endothelin, which the cells release.[2][4]
Clinical significance
Patients with salt-sensitive hypertension have higher plasma ET-1.[3] Endothelin-1 receptor antagonists (Bosentan) are used in the treatment of pulmonary hypertension.[2] Use of these antagonists prevents pulmonary arterial constriction and thus inhibits pulmonary hypertension.[2]
As of 2020, the role of endothelin-1 in affecting lipid metabolism and insulin resistance in obesity mechanisms was under clinical research.[5]
References
- ↑ Dhaun, Neeraj; Webb, David J. (August 2019). "Endothelins in cardiovascular biology and therapeutics" (in en). Nature Reviews Cardiology 16 (8): 491–502. doi:10.1038/s41569-019-0176-3. ISSN 1759-5010. https://www.nature.com/articles/s41569-019-0176-3.
- ↑ 2.0 2.1 2.2 2.3 "Endothelin". Pharmacological Reviews 68 (2): 357–418. April 2016. doi:10.1124/pr.115.011833. PMID 26956245.
- ↑ 3.0 3.1 "Endothelin-1 levels and cardiovascular events". Trends in Cardiovascular Medicine 30 (1): 1-8. 2020. doi:10.1016/j.tcm.2019.01.007. PMID 30765295.
- ↑ Medical physiology: a cellular and molecular approach. Saunders/Elsevier. 2009. ISBN 978-1-4160-3115-4.
- ↑ "Endothelin-1 in the pathophysiology of obesity and insulin resistance". Obesity Reviews 21 (12). December 2020. doi:10.1111/obr.13086. PMID 32627269.
External links
- Overview of all the structural information available in the PDB for UniProt: P05305 (Endothelin-1) at the PDBe-KB.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
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