Chemistry:Endothelin 1
 Generic protein structure example |
Endothelin 1 (ET-1), also known as preproendothelin-1 (PPET1), is a potent vasoconstrictor peptide produced by vascular endothelial cells.[1] 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.[1][2]
Clinical significance
Endothelin-1 receptor antagonists (Bosentan) are used in the treatment of pulmonary hypertension.[1] Use of these antagonists prevents pulmonary arterial constriction and thus inhibits pulmonary hypertension.[1]
As of 2020, the role of endothelin-1 in affecting lipid metabolism and insulin resistance in obesity mechanisms was under clinical research.[3]
References
- ↑ 1.0 1.1 1.2 1.3 "Endothelin". Pharmacological Reviews 68 (2): 357–418. April 2016. doi:10.1124/pr.115.011833. PMID 26956245.
- ↑ 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): e13086. 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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