Endothelin 1 (ET-1), also known as preproendothelin-1 (PPET1), is a potent vasoconstrictor that in humans is encoded by the EDN1gene and produced by vascular endothelial cells. The protein encoded by this gene is proteolytically processed to release a secreted peptide termed endothelin 1. 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.
Han SG, Ko S, Lee WK, Jung ST, Yu YG (August 2017). "Determination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method". Scientific Reports. 7 (1): 7577. doi:10.1038/s41598-017-08096-6.