Endothelin 1 Explained

Endothelin 1 (ET-1), also known as preproendothelin-1 (PPET1), is a potent vasoconstrictor peptide produced by vascular endothelial cells,[1] as well as by cells in the heart (affecting contractility) and kidney (affecting sodium handling).[2] 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] [3]

Clinical significance

Patients with salt-sensitive hypertension have higher plasma ET-1. 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.[4]

Notes and References

  1. Davenport AP, Hyndman KA, Dhaun N, Southan C, Kohan DE, Pollock JS, Pollock DM, Webb DJ, Maguire JJ . 6 . Endothelin . Pharmacological Reviews . 68 . 2 . 357–418 . April 2016 . 26956245 . 4815360 . 10.1124/pr.115.011833 .
  2. Jankowich M, Choudhary G . Endothelin-1 levels and cardiovascular events . . 30 . 1 . 1-8 . 2020 . 10.1016/j.tcm.2019.01.007 . 30765295.
  3. Book: Boulpaep EL, Boron WF . Medical physiology: a cellular and molecular approach . Saunders/Elsevier . 2009 . 978-1-4160-3115-4 .
  4. Jenkins HN, Rivera-Gonzalez O, Gibert Y, Speed JS . Endothelin-1 in the pathophysiology of obesity and insulin resistance . Obesity Reviews . 21 . 12 . e13086 . December 2020 . 32627269 . 7669671 . 10.1111/obr.13086 .