Endothelin receptor type B (EDNRB) (EDNRB)

Endothelin receptor type B (EDNRB) is a G protein-coupled receptor (GPCR) essential for vascular homeostasis, physiological development, and salt-water balance [3, 11]. It is one of two primary receptors for endothelin peptides and is prominently located on endothelial cells, where its activation triggers the release of vasodilators such as nitric oxide and prostacyclin [8, 14]. Additionally, EDNRB serves a critical role in scavenging excess circulating endothelin-1, maintaining proper vascular tone, and ensuring normal neural crest cell migration during embryonic development [3, 9, 14]. Dysregulation or genetic mutations in EDNRB are associated with Hirschsprung disease, Waardenburg syndrome, and the progression of various cancers, particularly melanoma [6, 9, 18]. In clinical practice, EDNRB is targeted by dual endothelin receptor antagonists to treat pulmonary arterial hypertension [3, 17]. Ongoing research also highlights its potential as a target for neuroregeneration and as a mechanism to overcome immune resistance in solid tumors [1, 2].

Other names

Endothelin B receptorETBET-BET-BRETBRETRBEndothelin receptor non-selective typehET-B

Antagonism of the endothelin receptor type B, typically in combination with endothelin receptor type A, to inhibit vasoconstriction and pathological vascular remodeling in conditions like pulmonary arterial hypertension; selective antagonism is also explored for its ability to increase T-cell infiltration in the tumor microenvironment and promote axonal regeneration.