endotelin1

Endothelin-1 (ET-1) is a potent vasoconstrictor peptide produced by endothelial cells lining blood vessels. It plays a crucial role in regulating blood pressure and vascular tone. ET-1 is synthesized as a precursor protein that undergoes several processing steps before being released into the circulation.

Once released, ET-1 binds to two specific receptors on the surface of smooth muscle cells and other cell types: endothelin A (ETA) and endothelin B (ETB) receptors. Activation of ETA receptors primarily leads to vasoconstriction, increasing blood pressure. Activation of ETB receptors can have dual effects, causing either vasodilation or vasoconstriction depending on the receptor subtype and the cell type.

ET-1 is involved in various physiological processes, including vascular development, wound healing, and inflammation. However, its dysregulation has been implicated in several cardiovascular diseases, such as hypertension, pulmonary arterial hypertension, atherosclerosis, and heart failure. Elevated levels of ET-1 are often observed in these conditions, contributing to excessive vasoconstriction and vascular remodeling.

Therapeutic strategies targeting the ET-1 pathway have been developed to manage these diseases. Endothelin receptor antagonists (ERAs) are a class of drugs that block the action of ET-1 by binding to its receptors. These antagonists have shown efficacy in treating conditions like pulmonary arterial hypertension, where they help to reduce pulmonary vascular resistance and improve exercise capacity. Research continues to explore the multifaceted roles of ET-1 and its potential as a therapeutic target.