Endothelin-2 (EDN2)

Endothelin-2 (EDN2) is a 21-amino acid secreted peptide hormone and a member of the endothelin family, encoded by the EDN2 gene. It acts primarily as a potent vasoconstrictor and as a paracrine and autocrine signaling molecule. EDN2 exerts its biological activities by binding to two G protein-coupled receptors: the endothelin A receptor (EDNRA, also known as ETA) and the endothelin B receptor (EDNRB, or ETB), with effects that include modulation of vascular tone and promotion of smooth muscle contraction[1][2][4][5]. Uniquely, EDN2 plays a central and essential role in ovulation: it is transiently expressed in granulosa cells of the ovarian follicle immediately prior to ovulation and triggers oocyte release by inducing contraction of the follicular wall[2][5]. EDN2 has also been implicated in cardiovascular pathophysiology (notably hypertension and cardiac remodeling), cancer progression (especially via hypoxia and immune cell recruitment), and other tissue-specific processes. Current therapeutics in the endothelin pathway primarily act by antagonizing endothelin receptors, which modulate but do not specifically isolate the actions of EDN2[1][4].

Other names

Endothelin 2ET-2ET2PPET2Preproendothelin-2preproendothelin 2endothelin-2

Competitive antagonism of endothelin receptors (ETA/EDNRA, ETB/EDNRB), blocking downstream vasoconstrictive and signaling responses[1][4]. Inhibition of endothelin converting enzyme to prevent maturation of bioactive endothelins[3].