Endothelin-1 (ET-1)

Endothelin-1 is a 21-amino-acid peptide and the most prominent isoform of the endothelin family, produced primarily by vascular endothelial cells but also found in heart, kidney, and nervous tissues[3][8]. It is one of the body's most potent endogenous vasoconstrictors, acting through two G protein-coupled receptors (endothelin receptor A and B) to regulate vascular tone, cell proliferation, inflammation, and fibrosis[1][7][5][8]. Beyond its classic cardiovascular effects, endothelin-1 participates in immune modulation, platelet aggregation, and tissue remodeling, and contributes to the pathogenesis of cardiovascular diseases, cancer, chronic kidney disease, infectious diseases, and other conditions[1][2][4]. Endothelin-1-targeted therapies—including several endothelin receptor antagonists—are approved for pulmonary arterial hypertension and under investigation for cancer, renal, and other diseases; however, use of such drugs is accompanied by significant safety considerations, notably edema, hepatotoxicity, and teratogenicity[4][6][8].

Other names

Preproendothelin-1PPET1EDN1

Endothelin receptor antagonism (blockade of ETA and/or ETB G protein-coupled receptors), inhibition of vasoconstriction, decreased cell proliferation and fibrosis, and improvement in hemodynamics and reduction in disease progression.