Endothelin type B receptor–Mas-related G protein-coupled receptor complex (ETBR–MasR complex) (ETBR–MasR complex)

The Endothelin type B receptor–Mas-related G protein-coupled receptor (ETBR–MasR) complex is a functional heterodimer formed by the association of the Endothelin type B receptor (EDNRB) and the Mas-related G protein-coupled receptor (MAS1) (UniProt P24530, P04201). This complex represents a crucial intersection between the endothelin system and the protective arm of the renin-angiotensin system (RAS), primarily located in the vascular endothelium and renal tissues. The interaction between these two receptors modulates their individual signaling profiles, typically enhancing vasodilatory and natriuretic pathways through the activation of nitric oxide synthase (NOS) and the subsequent release of nitric oxide (PubMed: 29438114). In cardiovascular diseases such as hypertension and preeclampsia, the synergistic signaling of the ETBR–MasR complex is often impaired, leading to increased vascular resistance and endothelial dysfunction. Therapeutic targeting of this complex involves the use of MasR agonists like Angiotensin-(1-7) or ETB-specific modulators to restore homeostatic signaling and provide cardioprotection. Understanding the specific pharmacology of this heterodimer is essential for developing selective treatments that minimize the side effects associated with broad-spectrum endothelin receptor antagonism.

Other names

ETB-Mas receptor heterodimerEDNRB-MAS1 complexEndothelin B receptor-Mas receptor complexMasR-ETBR heterodimer

The complex functions through the heterodimerization of ETBR and MasR, where activation of one receptor (e.g., MasR by Angiotensin-(1-7)) allosterically modulates the signaling of the other (e.g., ETBR), typically promoting the PI3K/Akt/eNOS pathway to increase nitric oxide production and induce vasodilation (Soares et al., 2018; Grobe et al., 2012).