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Target intelligence / Profile preview
Endothelin Receptor Type A (ETA)
- Target
- ETA
- Molecular classification
- G protein-coupled receptor
01
Overview
Endothelin receptor type A (ETA/EDNRA) is a G protein-coupled receptor that primarily binds endothelin-1, a potent vasoconstrictor peptide. Activation leads to vasoconstriction, sodium retention, and increased blood pressure. Overactivation contributes to hypertension, heart failure, renal failure, atherosclerosis, and cancer. ETA antagonists are under investigation for pulmonary arterial hypertension, chronic kidney disease, heart failure, and certain cancers.
- Other names
- ET-AETA-RETARETRAEDNRA
02
Mechanism of action
ETA antagonists block the binding of endothelin-1 to the ETA receptor, preventing vasoconstriction, cell proliferation, and other downstream effects.
03
Biological functions
VasoconstrictionCell ProliferationSodium RetentionBlood Pressure ControlSignal transduction
04
Disease associations
HypertensionHeart failureRenal failureGlomerulosclerosisAtherosclerosisRestenosisVascular remodelingFibrosisChronic kidney diseaseCardiovascular diseaseCancer
05
Safety considerations
ETA antagonists may cause hypotension.
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