Human Endothelin 1 Receptor (EDNRA) CLIA Kit

Background

EDNRA is a G protein-coupled receptor (GPCR) that binds endothelin-1 (ET-1) with high affinity, playing a critical role in regulating vascular tone, cell proliferation, and cardiac function. It is predominantly expressed on vascular smooth muscle cells, where its activation by ET-1 triggers potent vasoconstriction through downstream signaling pathways, including phospholipase C (PLC), protein kinase C (PKC), and calcium mobilization. EDNRA-mediated signaling is essential for maintaining blood pressure and vascular homeostasis but contributes to pathological conditions such as hypertension, pulmonary arterial hypertension (PAH), and atherosclerosis when dysregulated. In cancer, EDNRA is overexpressed in tumors, including breast, ovarian, and prostate cancers, where it promotes cell proliferation, survival, angiogenesis, and metastasis by enhancing ET-1 signaling. EDNRA activation also contributes to cardiac hypertrophy and fibrosis in heart failure, making it a therapeutic target for cardiovascular diseases. Pharmacological antagonists of EDNRA, such as endothelin receptor antagonists (ERAs), have shown efficacy in managing PAH and reducing vascular remodeling. Overall, EDNRA plays a vital role in vascular physiology and disease, with its dysregulation driving cardiovascular pathology and tumor progression.