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Endothelin Converting Enzymes and Endothelin Receptor Localisation in Human Tissues

  • Chapter
Endothelin and Its Inhibitors

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 152))

Abstract

ET-1 is the principal isoform of endothelin in the human cardiovascular system. ET-1 is continuously released from vascular endothelial cells, to produce intense vasoconstriction of the underlying smooth muscle and so maintain endogenous vascular tone. ET-l released from other epithelial cells situated at the interface between biological compartments may have a range of actions in humans as well as functioning as a neuropeptide in the brain. Overexpression of ET-l has been implicated in a number of pathophysiological conditions such as coronary artery disease (see Chaps. 12–19). Two strategies have emerged to block undesirable actions of ET-l in diseased tissue: receptor antagonists and inhibitors of the enzymes responsible for ET-l synthesis. Given the wide distribution and emerging multifunctional role of the peptide, determining the anatomical localisation of endothelin converting enzymes (ECE) is important in understanding the mechanism of production of ET and identification of the receptor sub-type interacting with the released peptide.

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Authors
  1. A. P. Davenport
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  2. F. D. Russell
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Editors and Affiliations

  1. Department of Cardiac, Vascular and Inflammation Research, The William Harvey Research Institute St. Barthomew’s and the Royal London School of Medicine and Dentistry, Charterhouse Square, London, EC1M 6BQ, UK

    Timothy D. Warner Ph.D

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Davenport, A.P., Russell, F.D. (2001). Endothelin Converting Enzymes and Endothelin Receptor Localisation in Human Tissues. In: Warner, T.D. (eds) Endothelin and Its Inhibitors. Handbook of Experimental Pharmacology, vol 152. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-56899-2_8

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  • DOI: https://doi.org/10.1007/978-3-642-56899-2_8

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