Endothelin 1 (ET-1 ), also known as preproendothelin-1 (PPET1), is a potent vasoconstrictor peptide produced by vascular endothelial cells .[5] 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 [ edit ]
Preproendothelin is precursor of the peptide ET-1. Endothelial cells convert preproendothelin to proendothelin and subsequently to mature endothelin, which the cells release.[5] [6]
Clinical significance [ edit ]
Endothelin-1 receptor antagonists (Bosentan ) are used in the treatment of pulmonary hypertension .[5] Use of these antagonists prevents pulmonary arterial constriction and thus inhibits pulmonary hypertension.[5]
As of 2020, the role of endothelin-1 in affecting lipid metabolism and insulin resistance in obesity mechanisms was under clinical research .[7]
References [ edit ]
^ a b c GRCh38: Ensembl release 89: ENSG00000078401 - Ensembl , May 2017
^ a b c GRCm38: Ensembl release 89: ENSMUSG00000021367 - Ensembl , May 2017
^ "Human PubMed Reference:" . National Center for Biotechnology Information, U.S. National Library of Medicine .
^ "Mouse PubMed Reference:" . National Center for Biotechnology Information, U.S. National Library of Medicine .
^ a b c d Davenport AP, Hyndman KA, Dhaun N, Southan C, Kohan DE, Pollock JS, et al. (April 2016). "Endothelin" . Pharmacological Reviews . 68 (2): 357–418. doi :10.1124/pr.115.011833 . PMC 4815360 . PMID 26956245 .
^ Boulpaep EL, Boron WF (2009). Medical physiology: a cellular and molecular approach . Saunders/Elsevier. ISBN 978-1-4160-3115-4 .
^ Jenkins HN, Rivera-Gonzalez O, Gibert Y, Speed JS (December 2020). "Endothelin-1 in the pathophysiology of obesity and insulin resistance" . Obesity Reviews . 21 (12): e13086. doi :10.1111/obr.13086 . PMC 7669671 . PMID 32627269 .
External links [ edit ]
This article incorporates text from the United States National Library of Medicine , which is in the public domain .