Endothelin receptors bind endothelin

Stable Identifier
Reaction [binding]
Homo sapiens
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Endothelins are 21-amino acid vasoconstricting peptides produced primarily in the endothelium that play a key role in vascular homeostasis. An imbalance and over-expression of endothelins can contribute to hypertension (high blood pressure). Endothelins are implicated in vascular diseases of several organ systems, including the heart, general circulation and brain. There are 3 isoforms designated ET1, ET2 and ET3 (Inoue A et al, 1989).

These bind to two receptors, designated ETA (Adachi M et al, 1991) and ETB (Nakamuta M et al, 1991). ETA receptors are primarily located in smooth muscle of blood vessels. Endothelin binding to ETA causes vasoconstriction and sodium retention, leading to increased blood pressure. ETB are primarily located on endothelial cells lining the internal walls of vasculature. Endothelin binding to ETB leads to the release of NO (nitric oxide) which is a strong vasodilator.

Literature References
PubMed ID Title Journal Year
8440682 Molecular characterization and regulation of the human endothelin receptors

Elshourbagy, NA, Korman, DR, Wu, HL, Sylvester, DR, Lee, JA, Nuthalaganti, P, Bergsma, DJ, Kumar, CS, Nambi, P

J Biol Chem 1993
1710450 Cloning and sequence analysis of a cDNA encoding human non-selective type of endothelin receptor

Nakamuta, M, Takayanagi, R, Sakai, Y, Sakamoto, S, Hagiwara, H, Mizuno, T, Saito, Y, Hirose, S, Yamamoto, M, Nawata, H

Biochem Biophys Res Commun 1991
1719979 Cloning and characterization of cDNA encoding human A-type endothelin receptor

Adachi, M, Yang, YY, Furuichi, Y, Miyamoto, C

Biochem Biophys Res Commun 1991
2649896 The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes

Inoue, A, Yanagisawa, M, Kimura, S, Kasuya, Y, Miyauchi, T, Goto, K, Masaki, T

Proc Natl Acad Sci U S A 1989
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