Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

Endothelin.

A P Davenport1, J J Maguire

  • 1Clinical Pharmacology Unit, University of Cambridge, Addenbrooke's Hospital, Cambridge CB2 2QQ, UK. apd10@medschl.cam.ac.uk

Handbook of Experimental Pharmacology
|September 27, 2006
PubMed
Summary
This summary is machine-generated.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

New drugs and emerging therapeutic targets in the endothelin signaling pathway and prospects for personalized precision medicine.

Physiological research·2018
Same author

Endothelin@25 - new agonists, antagonists, inhibitors and emerging research frontiers: IUPHAR Review 12.

British journal of pharmacology·2014
Same author

The Concise Guide to PHARMACOLOGY 2013/14: overview.

British journal of pharmacology·2014
Same author

Chemokine receptor CCR5: from AIDS to atherosclerosis.

British journal of pharmacology·2010
Same author

Endothelial cell-specific ETB receptor knockout: autoradiographic and histological characterisation and crucial role in the clearance of endothelin-1.

Canadian journal of physiology and pharmacology·2010
Same author

Evaluation of translocator protein quantification as a tool for characterising macrophage burden in human carotid atherosclerosis.

Atherosclerosis·2010
Same journal

Endothelial Cell Phenotypic Plasticity in Atherosclerosis.

Handbook of experimental pharmacology·2026
Same journal

Endothelial Dysfunction and Neurovascular Alterations in Autism Spectrum Disorder.

Handbook of experimental pharmacology·2026
Same journal

Molecular Mechanisms of Endothelial Shear Stress Mechanotransduction in Health and Disease.

Handbook of experimental pharmacology·2026
Same journal

Microvasculature of the Pancreatic Islets of Langerhans in Health and Diabetes.

Handbook of experimental pharmacology·2026
Same journal

Mechanisms of Actions of Physiological, Pharmacological, and Toxicological Dietary Bioactive Inorganic Boron.

Handbook of experimental pharmacology·2026
Same journal

BNCT Plus Luminescence: New Paradigm for Boron-Containing Drug Design.

Handbook of experimental pharmacology·2026
See all related articles

Endothelins (ETs) are potent vasoconstrictors. The endothelin system is implicated in cardiovascular diseases like hypertension and pulmonary arterial hypertension, with ET antagonists showing therapeutic promise.

Area of Science:

  • Biochemistry
  • Cardiovascular Physiology
  • Pharmacology

Background:

  • Endothelins (ETs) are a family of three peptides (ET-1, ET-2, ET-3) crucial in cardiovascular regulation.
  • ET-1, the primary cardiovascular isoform, is a potent vasoconstrictor synthesized via endothelin converting enzyme (ECE-1).
  • The ET system is upregulated in conditions like atherosclerosis and hypertension.

Purpose of the Study:

  • To review the synthesis, regulation, and physiological actions of endothelins.
  • To discuss the therapeutic strategies targeting the endothelin system.
  • To highlight the potential benefits of ET antagonists in cardiovascular diseases.

Main Methods:

  • Review of scientific literature on endothelin biology and pharmacology.

Related Experiment Videos

  • Analysis of the mechanisms of ET-1 synthesis and action.
  • Examination of therapeutic agents targeting the ET system, such as ECE inhibitors and receptor antagonists.

    • Main Results:

    • ET-1 is synthesized from Big ET-1 by ECE-1 and released via constitutive and regulated pathways.
    • ETs exert their effects by activating ETA and ET(B) G protein-coupled receptors.
    • ET antagonists like bosentan offer a new therapeutic approach for pulmonary arterial hypertension and potentially hypertension.

    Conclusions:

    • The endothelin system plays a significant role in maintaining vascular tone and is dysregulated in cardiovascular diseases.
    • Inhibition of ET synthesis or receptor blockade represents a viable therapeutic strategy.
    • ET antagonists, such as bosentan, have demonstrated clinical efficacy, particularly in pulmonary arterial hypertension.