Stable Identifier
Reaction [binding]
Homo sapiens
Endothelin receptors bind endothelin
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Endothelins (EDNs) 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 EDNs can contribute to hypertension (high blood pressure). EDNs are implicated in vascular diseases of several organ systems, including the heart, general circulation and brain. There are 3 isoforms derived from the genes EDN1, EDN2 and EDN3 (Inoue et al. 1989).

EDNs bind to two receptors (Elshourbagy et al. 1993), EDNRA (Adachi et al. 1991) and EDNRB (Nakamuta et al. 1991). EDNRA is primarily located in the smooth muscle of blood vessels. EDN binding to EDNRA results in vasoconstriction and sodium retention, leading to increased blood pressure. EDNRB is primarily located on endothelial cells lining the internal walls of vasculature. EDN binding to EDNRB leads to the release of NO (nitric oxide), a powerful vasodilator.
Literature References
PubMed ID Title Journal Year
1710450 Cloning and sequence analysis of a cDNA encoding human non-selective type of endothelin receptor

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

Biochem Biophys Res Commun 1991
8440682 Molecular characterization and regulation of the human endothelin receptors

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

J Biol Chem 1993
1719979 Cloning and characterization of cDNA encoding human A-type endothelin receptor

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

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

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

Proc Natl Acad Sci U S A 1989
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