Target intelligence / Profile preview

Mas receptor–endothelin type B receptor complex (MasR:ETBR)

Target
MasR:ETBR
Molecular classification
G protein-coupled receptor, Heteromeric receptor complex, Receptor
01

Overview

The Mas receptor–endothelin type B receptor complex is a functional heteromer formed by the association of the Mas receptor (MasR) and the endothelin type B receptor (ETBR) [1, 2]. This complex serves as a vital regulatory unit in the vascular endothelium, where it facilitates crosstalk between the renin-angiotensin system and the endothelin system [1]. Specifically, the interaction amplifies the signaling of angiotensin-(1-7) and promotes the vasoprotective actions of endothelin-1 through the ETBR, such as the activation of endothelial nitric oxide synthase (eNOS) and the production of nitric oxide (NO) [1, 2]. This synergy is essential for maintaining vascular homeostasis, inducing vasodilation, and preventing inflammation and vascular remodeling [1]. Dysregulation or dissociation of the MasR:ETBR complex is associated with cardiovascular pathologies, including pulmonary hypertension and endothelial dysfunction [1, 2]. Consequently, the complex is an emerging therapeutic target, with research focusing on "enhancers" that stabilize the heteromer to restore or boost its protective signaling in diseased states [1]. Pharmacological modulation of this complex offers a more nuanced approach than simple receptor antagonism, potentially avoiding the side effects associated with blocking individual receptors [1, 3].

Other names
Mas-ETB heteromerMas-ETB receptor complexMAS1-EDNRB complexMasR:ETBR interaction
02

Mechanism of action

Enhancement of receptor heteromerization to amplify vasoprotective signaling pathways, specifically eNOS activation and nitric oxide production.

03

Biological functions

Signal transductionVasodilationNitric oxide productionVascular homeostasisEndothelial function regulation
04

Disease associations

Cardiovascular diseasePulmonary hypertensionInflammationEndothelial dysfunction
05

Safety considerations

Potential for systemic hypotensionOff-target effects on individual Mas or ETB receptorsPharmacological complexity of GPCR heteromers
06

Interacting drugs

Angiotensin-(1-7)

5 more in the full profile.

07

Biomarkers

Nitric oxide (NO) levelseNOS phosphorylationVascular relaxation response

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