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Details on Person Endothelins (EDNs) are 21-amino acid vasoconstricting peptid...

Class:IdSummation:9731929
_displayNameEndothelins (EDNs) are 21-amino acid vasoconstricting peptid...
_timestamp2021-05-25 09:18:48
created[InstanceEdit:9731928] Jassal, Bijay, 2021-05-25
literatureReference[LiteratureReference:9731896] Ambrisentan, an endothelin receptor type A-selective antagonist, inhibits cancer cell migration, invasion, and metastasis
[LiteratureReference:9731922] Targeted Drugs for Treatment of Pulmonary Arterial Hypertension: Past, Present, and Future Perspectives
textEndothelins (EDNs) are 21-amino acid vasoconstricting peptides produced primarily in the endothelium that play a key role in vascular homeostasis. They are potent and long-lasting vasoconstrictors. An imbalance and over-expression of EDNs can contribute to hypertension (high blood pressure). EDNs bind to two endothelin receptors, EDNRA and EDNRB. EDNRA is primarily located in the smooth muscle of blood vessels and upon EDN binding, leads to vasoconstriction and sodium retention, ultimately increasing 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.

EDNR antagonists (ERAs) are competitive antagonists of EDNs at EDNRs. ERAs selective for EDNRA are primarily indicated for pulmonary arterial hypertension (PAH) (Zheng et al. 2020). EDNRA-selective approved drugs are sitaxentan (Wu et al. 1997) and ambrisentan (Bolli et al. 2004).

Ambrisentan has been shown to inhibit cancer cell migration, invasion and metastasis in vitro, suggesting a new therapeutic application for this drug (Kappes et al. 2020).
(summation)[Reaction:9731931] EDNRA binds selective ERAs [Homo sapiens]
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