Endothelin 1

Endothelin 1 (ET-1), also known as preproendothelin-1 (PPET1), is a protein that in humans is encoded by the EDN1 gene. The protein encoded by this gene is proteolytically processed to release a secreted peptide termed endothelin 1. This peptide is a potent vasoconstrictor and is produced by vascular endothelial cells. Endothelin 1 is one of three isoforms of human endothelin.

Preproendothelin is precursor of the peptide ET-1. Endothelial cells convert preproendothelin to proendothelin and subsequently to mature endothelin, which the cells release.

Endothelin-1 receptor antagonists (Bosentan) are used in the treatment of pulmonary hypertension. Inhibition of these receptors prevents pulmonary vasculature constriction and thus decreases pulmonary vascular resistance.

References

Further reading

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

Endothelin

Endothelins are peptides that constrict blood vessels and raise blood pressure. They are normally kept in balance by other mechanisms, but when they are over-expressed, they contribute to high blood pressure (hypertension) and heart disease.

Endothelins are 21-amino acid vasoconstricting peptides produced primarily in the endothelium having a key role in vascular homeostasis. Endothelins are implicated in vascular diseases of several organ systems, including the heart, general circulation and brain.

Etymology

Endothelins derived the name from the fact that they were derived and secreted from cultured endothelial cells.

Isoforms

There are three isoforms (identified as ET-1, -2, -3) with varying regions of expression and binding to at least four known endothelin receptors, ET_A, ET_B1, ET_B2 and ET_C.

Antagonists

Earliest antagonists discovered for ET_A is BQ123, and that for ET_B is BQ788.

Examples of physiological interaction

Endothelins are the most potent vasoconstrictors known. In a healthy individual, a delicate balance between vasoconstriction and vasodilation is maintained by endothelin and other vasoconstrictors on the one hand and nitric oxide, prostacyclin and other vasodilators on the other.