Endothelin pathway

The endothelin pathway encompasses a family of potent vasoactive peptides (primarily endothelin-1, -2, and -3) that signal through G protein-coupled endothelin A and B receptors. Endothelin-1 is a key mediator of vasoconstriction and exerts pro-proliferative, inflammatory, and pain-promoting effects in various tissues. Dysregulation of this pathway is implicated in cardiovascular diseases such as pulmonary arterial hypertension, certain cancers (where it may promote proliferation and immune evasion), pain syndromes, and chronic kidney disease. Drugs targeting this pathway include selective and dual endothelin receptor antagonists, which have demonstrated efficacy in pulmonary arterial hypertension and are under investigation for broader disease contexts. Note: For precise molecular targeting and drug development, it is standard to reference the specific receptors (e.g., "Endothelin A receptor") or enzymes within the pathway, rather than the general term "endothelin pathway."

Other names

Endothelin systemET receptorsEndothelin axis

Antagonism of ET_A and/or ET_B receptors to inhibit vasoconstriction, proliferation, and pain signaling. Inhibition of Endothelin-converting enzyme to reduce production of active endothelins.