Endothelin receptor type A (ET-A) (ET-A)

The endothelin receptor type A (ET-A) is a G protein-coupled receptor primarily located on vascular smooth muscle cells, where it mediates the potent vasoconstrictive effects of endothelin-1 (ET-1) (UniProt, P25101). Upon activation, ET-A triggers intracellular signaling pathways, including the phospholipase C pathway, which leads to prolonged contraction of blood vessels and promotes cellular proliferation and fibrosis (PubMed, PMID: 21937751). This receptor plays a critical role in maintaining vascular tone and blood pressure, but its overactivation is linked to various pathological conditions, most notably pulmonary arterial hypertension (PAH) and chronic kidney disease (StatPearls, NBK544315). In the context of disease, ET-A signaling contributes to vascular remodeling, increased peripheral resistance, and cardiac hypertrophy (NIH, Gene ID: 1909). Consequently, ET-A has become a significant therapeutic target, with several endothelin receptor antagonists (ERAs) developed to treat PAH by inducing vasodilation and inhibiting structural changes in the vasculature (PubChem, CID: 110635). Beyond cardiovascular health, ET-A is also investigated for its role in cancer progression, particularly in prostate and ovarian cancers, and for its potential in providing renal protection in diabetic nephropathy (Wikipedia, Endothelin receptor A).

Other names

EDNRAETA receptorEndothelin A receptorhETAEndothelin-1 receptor

Antagonism of the endothelin receptor type A to prevent the binding of endothelin-1, thereby inhibiting vasoconstriction and cellular proliferation (StatPearls, NBK544315).