Endothelin A receptor (ETA receptor)

The Endothelin A receptor is a member of the G protein-coupled receptor superfamily, comprised of seven transmembrane α-helices. It binds endothelin-1, a potent vasoconstrictive peptide, and mediates a variety of biological effects including blood vessel contraction, cell proliferation, and anti-apoptotic signaling. ETA receptors are widely expressed in cardiovascular, renal, immune, and tumor tissues, where they are involved in the pathogenesis of hypertension, heart failure, and cancer progression. Therapeutic drugs targeting ETA (often along with ETB) are used in pulmonary arterial hypertension, kidney disease, and are being explored as adjuncts in cancer therapy to inhibit metastasis and drug resistance. Selective and dual ETA/ETB antagonists are well-characterized, with several approved for clinical use. “ET-1R” is an unofficial, imprecise abbreviation—careful distinction between ETA and ETB receptor is essential for research and clinical application.

Other names

Endothelin receptor type AEDNRAETAR

Antagonism/blockade of receptor to inhibit endothelin-1 effects; Reduction of vasoconstriction; Suppression of pathological cell proliferation and angiogenesis; Sensitization of tumor cells to chemotherapy; Reduction of proteinuria