A novel potent vasoconstrictor peptide produced by vascular endothelial cells

Abstract

An endothelium-derived 21-residue vasoconstrictor peptide, endothelin, has been isolated, and shown to be one of the most potent vasoconstrictors known. Cloning and sequencing of preproendothelin complementary DNA shows that mature endothelin is generated through an unusual proteolytic processing, and regional homologies to a group of neurotoxins suggest that endothelin is an endogenous modulator of voltage-dependent ion channels. Expression of the endothelin gene is regulated by several vasoactive agents, indicating the existence of a novel cardiovascular control system.

Effect of Breed on Plasma Endothelin‐1 Concentration, Plasma Renin Activity, and Serum Cortisol Concentration in Healthy Dogs

“…Endothelin‐1 is mainly produced in vascular endothelial cells and acts locally as a potent vasoconstrictor, but it is also produced in organs such as the heart and kidney 2, 25. In dogs, increased concentrations of ET‐1 have been found in chronic kidney disease and ET‐1 has been suggested a biomarker of hypertension 6.…”

“…Decrease in blood pressure activates the sympathetic nervous system, the renin‐angiotensin‐aldosterone system (RAAS), and vasopressin, leading to vasoconstriction 1. Angiotensin II can stimulate the release of endothelin‐1 (ET‐1), a potent vasoconstrictor, from vascular endothelium, and ET‐1 can in turn stimulate the release of norepinephrine, angiotensin II, and vasopressin 2, 3. The RAAS, together with vasopressin, also stimulates sodium and fluid retention 1.…”

Identification and characterization of two isoforms of an endothelin‐converting enzyme‐1

“…Endothelins (ETs) are potent vasoconstrictive 21 amino-acid peptides originally isolated from the supernatant of cultured porcine aortic endothelial cells [1]. ETs are generated by a unique proteolytic cleavage of big endothelins (big ETs) at the Trp21-Va122 or Trp2~-Ile 22 bond catalyzed by an endothelinconverting enzyme (ECE) [2].…”

Cardioprotective effect of an endothelin receptor antagonist during ischaemia/reperfusion in the severely atherosclerotic mouse heart

“…Nitric oxide (NO) is constitutively produced in endothelial cells by endothelial NO synthase and exerts important protective effects by reducing vascular tone, inhibiting leucocyte and platelet activation and inactivating superoxide (Lu¨scher & Noll, 1995). Another endothelium-derived substance is the potent vasoconstrictor endothelin-1 (ET-1) (Yanagisawa et al, 1988). ET-1 mediates vasoconstriction by binding to the ET A and ET B receptors located on smooth muscle cells.…”