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

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

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

  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000078401 – Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000021367 – Ensembl, May 2017
  3. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ 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.
  6. ^ Boulpaep EL, Boron WF (2009). Medical physiology: a cellular and molecular approach. Saunders/Elsevier. ISBN 978-1-4160-3115-4.
  7. ^ 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

This article incorporates text from the United States National Library of Medicine, which is in the public domain.