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Endothelin-1 in Health and Disease.

Katherine M R M Banecki1, Kim A Dora1

  • 1Department of Pharmacology, University of Oxford, Mansfield Road, Oxford OX1 3QT, UK.

International Journal of Molecular Sciences
|July 29, 2023
PubMed
Summary

Endothelin-1 (ET-1), a potent peptide, impacts physiology and pathology. Targeting ET-1 offers potential for treating cardiovascular diseases, COVID-19, and chronic pain, though therapeutic development is ongoing.

Keywords:
cardiovascular diseaseendothelin-1endotheliumreleasestoragevasculature

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Area of Science:

  • Biochemistry
  • Physiology
  • Pathology

Background:

  • Endothelin-1 (ET-1) is a potent vasoconstrictor peptide with significant physiological and pathological roles.
  • Recent research highlights ET-1's contribution to various diseases, leading to the development of ET receptor antagonists.
  • Despite approved treatments for pulmonary arterial hypertension, broader therapeutic success targeting the ET-1 pathway remains limited.

Purpose of the Study:

  • To summarize current knowledge on ET-1 synthesis, storage, and release.
  • To review the role of ET-1 in diseases such as cardiovascular diseases, COVID-19, and chronic pain.
  • To identify potential new therapeutic avenues by exploring ET-1 pathway modulation.

Main Methods:

  • Literature review of ET-1 synthesis, storage, and release mechanisms.
  • Analysis of ET-1's involvement in diverse pathological conditions.
  • Examination of existing and potential therapeutic strategies targeting the ET-1 pathway.

Main Results:

  • ET-1 plays a critical role in both normal physiological functions and disease pathogenesis.
  • ET-1 is implicated in cardiovascular diseases, COVID-19, and chronic pain.
  • Research into ET-1 synthesis and release pathways, beyond cell cultures, is needed for therapeutic advancement.

Conclusions:

  • Targeting the ET-1 pathway holds significant therapeutic potential for a range of diseases.
  • Developing novel strategies focused on ET-1 synthesis and release could overcome limitations of current antagonists.
  • Further research in ex vivo and in vivo models is crucial for translating ET-1 pathway discoveries into effective treatments.