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. EDNRA is primarily located in the smooth muscle of blood vessels. EDNs binding to EDNRA result in vasoconstriction and sodium retention, leading to increased blood pressure. EDNRB is primarily located on endothelial cells lining the internal walls of vasculature. Conversely, EDNs binding to EDNRB leads to vasodilation due to the release of NO (nitric oxide), a powerful vasodilator.
Lee, JA, Kumar, CS, Sylvester, DR, Elshourbagy, NA, Nambi, P, Wu, HL, Bergsma, DJ, Nuthalaganti, P, Korman, DR
Yang, YY, Furuichi, Y, Adachi, M, Miyamoto, C
Yanagisawa, M, Goto, K, Masaki, T, Miyauchi, T, Kasuya, Y, Kimura, S, Inoue, A
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