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Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists01:18

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists

Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme (ECE). Of...
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Regulation of Angiogenesis and Blood Supply

Rapidly dividing tumors, embryos, and wounded tissues require more oxygen than usual, lowering the oxygen concentration in the blood. At low oxygen or hypoxic conditions, an oxygen-sensitive transcription factor called the hypoxia-inducible factor 1 or HIF1 is activated. HIF1 is a dimeric protein of alpha (ɑ) and beta (β) subunits.  Under optimal oxygen conditions, HIF1β is present in the nucleus while HIF1ɑ remains in the cytosol. HIF1ɑ is hydroxylated by prolyl hydroxylase and factor...
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Vascular Spasm

The vascular phase, also known as vasospasm, is the initial stage of hemostasis, crucial for preventing excessive bleeding when a blood vessel is injured. After a vessel is cut, nerves in the damaged area trigger pain and other sensory impulses. Simultaneously, the smooth muscles in the vessel wall contract, resulting in a vascular spasm. This contraction reduces the vessel's diameter at the injury site, slowing or stopping blood loss through the vessel wall. Vascular spasms typically last for...
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Related Experiment Video

Updated: Jul 1, 2026

Ultrasound Assessment of Endothelial-Dependent Flow-Mediated Vasodilation of the Brachial Artery in Clinical Research
08:42

Ultrasound Assessment of Endothelial-Dependent Flow-Mediated Vasodilation of the Brachial Artery in Clinical Research

Published on: October 22, 2014

Endothelin--role in vascular disease.

D Abraham1, M Dashwood

  • 1Department of Medicine, Centre for Rheumatology and Connective Tissue Diseases, Royal Free and University College Medical School, University College London, London, UK. d.abraham@medsch.ucl.ac.uk

Rheumatology (Oxford, England)
|September 17, 2008
PubMed
Summary

Endothelin-1 (ET-1) is a potent vasoconstrictor implicated in endothelial dysfunction and vascular disease. ET-1 receptor antagonists show promise in treating these conditions by modulating inflammatory pathways.

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Screening Assays to Characterize Novel Endothelial Regulators Involved in the Inflammatory Response
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Last Updated: Jul 1, 2026

Ultrasound Assessment of Endothelial-Dependent Flow-Mediated Vasodilation of the Brachial Artery in Clinical Research
08:42

Ultrasound Assessment of Endothelial-Dependent Flow-Mediated Vasodilation of the Brachial Artery in Clinical Research

Published on: October 22, 2014

Screening Assays to Characterize Novel Endothelial Regulators Involved in the Inflammatory Response
12:50

Screening Assays to Characterize Novel Endothelial Regulators Involved in the Inflammatory Response

Published on: September 15, 2017

Area of Science:

  • Cardiovascular Biology
  • Molecular Medicine
  • Pathophysiology

Background:

  • Endothelin-1 (ET-1) is a potent vasoconstrictor discovered two decades ago.
  • ET-1 exerts its effects via ET(A) and ET(B) receptors found on various cell types, including endothelial cells, vascular smooth muscle cells, and fibroblasts.
  • ET-1 is increasingly recognized as a critical factor in endothelial dysfunction across cardiovascular diseases, autoimmune disorders, and connective tissue diseases (CTDs).

Purpose of the Study:

  • To review the current understanding of Endothelin (ETs) roles in vascular dysfunction and disease.
  • To highlight the specific involvement of ET-1 in connective tissue diseases (CTDs).
  • To explore the therapeutic potential of ET-1 receptor antagonists.

Main Methods:

  • Literature review of existing research on ET-1 and vascular disease.
  • Analysis of the mechanisms by which ET-1 contributes to endothelial dysfunction.
  • Examination of the role of ET-1 in connective tissue diseases (CTDs).

Main Results:

  • ET-1 is a key mediator in endothelial dysfunction, leading to inflammation and cell activation.
  • Beyond vasoconstriction, ET-1 influences vessel remodeling and interacts with growth factors and cytokines.
  • ET-1 plays a significant role in the pathophysiology of various cardiovascular, autoimmune, and connective tissue diseases (CTDs).

Conclusions:

  • ET-1 receptor antagonists may effectively mitigate vascular dysfunction and disease progression.
  • These antagonists can modulate vasoconstrictor pathways, inflammatory markers, and growth factor effects.
  • Targeting ET-1 pathways offers a promising therapeutic strategy for vascular and connective tissue diseases (CTDs).