Endothelin-1 receptor
Also known as: EDNRA, ETA, ETRA
Function
Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3.
Classification
- Family (Pfam)
- PF00001 7tm_1
- InterPro
- Endthln_rcpt, ETA_rcpt, GPCR_endothelin_rcpt, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM
- Functional cluster
- MFS & Drug-Efflux Transporters
Experimental structures · PDB · 5
A predicted model is available from AlphaFold.
Gene Ontology · 73
- GO:0005886 plasma membrane
- GO:0004962 endothelin receptor activity
- GO:0004435 phosphatidylinositol-4,5-bisphosphate phospholipase C activity
- GO:0007190 activation of adenylate cyclase activity
- GO:0035904 aorta development
- GO:0014824 artery smooth muscle contraction
- GO:0003228 atrial cardiac muscle tissue development
- GO:0048675 axon extension
- GO:0060385 axonogenesis involved in innervation
- GO:0001974 blood vessel remodeling
- GO:0001569 branching involved in blood vessel morphogenesis
- GO:0070588 calcium ion transmembrane transport
- GO:0141156 cAMP/PKA signal transduction
- GO:0060070 canonical Wnt signaling pathway
- GO:0003207 cardiac chamber formation
- GO:0003253 cardiac neural crest cell migration involved in outflow tract morphogenesis
- GO:0008283 cell population proliferation
- GO:0071372 cellular response to follicle-stimulating hormone stimulus
- GO:0044751 cellular response to human chorionic gonadotropin stimulus
- GO:0071373 cellular response to luteinizing hormone stimulus
- GO:0034599 cellular response to oxidative stress
- GO:0097237 cellular response to toxic substance
- GO:1904888 cranial skeletal system development
- GO:0048066 developmental pigmentation
- GO:0035050 embryonic heart tube development
- GO:0048706 embryonic skeletal system development
- GO:0086100 endothelin receptor signaling pathway
- GO:0048484 enteric nervous system development
- GO:0061028 establishment of endothelial barrier
- GO:0060324 face development
- GO:0007186 G protein-coupled receptor signaling pathway
- GO:0010467 gene expression
- GO:0072011 glomerular endothelium development
- GO:0003094 glomerular filtration
- GO:0003015 heart process
- GO:0030202 heparin proteoglycan metabolic process
- GO:0006874 intracellular calcium ion homeostasis
- GO:0003220 left ventricular cardiac muscle tissue morphogenesis
- GO:1903537 meiotic cell cycle process involved in oocyte maturation
- GO:0097152 mesenchymal cell apoptotic process
- GO:0042474 middle ear morphogenesis
- GO:0007005 mitochondrion organization
- GO:0000278 mitotic cell cycle
- GO:0014034 neural crest cell fate commitment
- GO:0050905 neuromuscular process
- GO:0016322 neuron remodeling
- GO:0003357 noradrenergic neuron differentiation
- GO:0042415 norepinephrine metabolic process
- GO:0061626 pharyngeal arch artery morphogenesis
- GO:0007200 phospholipase C-activating G protein-coupled receptor signaling pathway
- GO:1903210 podocyte apoptotic process
- GO:0072112 podocyte differentiation
- GO:2001259 positive regulation of cation channel activity
- GO:0007204 positive regulation of cytosolic calcium ion concentration
- GO:0071806 protein transmembrane transport
- GO:0008217 regulation of blood pressure
- GO:0002027 regulation of heart rate
- GO:1905871 regulation of protein localization to cell leading edge
- GO:0097018 renal albumin absorption
- GO:0070294 renal sodium ion absorption
- GO:0007585 respiratory gaseous exchange by respiratory system
- GO:1905144 response to acetylcholine
- GO:0001975 response to amphetamine
- GO:0009611 response to wounding
- GO:0071526 semaphorin-plexin signaling pathway
- GO:0007165 signal transduction
- GO:0006939 smooth muscle contraction
- GO:0055078 sodium ion homeostasis
- GO:0048485 sympathetic nervous system development
- GO:0097492 sympathetic neuron axon guidance
- GO:0030878 thyroid gland development
- GO:0097084 vascular associated smooth muscle cell development
- GO:0042310 vasoconstriction
Disease associations
- mandibulofacial dysostosis with alopecia MONDO:0014608
Drugs targeting this protein · 16
- CLAZOSENTAN antagonist
- AMBRISENTAN antagonist
- ZIBOTENTAN antagonist
- MACITENTAN antagonist
- SITAXENTAN SODIUM antagonist
- ATRASENTAN HYDROCHLORIDE antagonist
- NEBENTAN antagonist
- APROCITENTAN antagonist
- DARUSENTAN antagonist
- SITAXENTAN antagonist
- BQ-123 antagonist
- AVOSENTAN antagonist
- ENRASENTAN antagonist
- SPARSENTAN antagonist
- TEZOSENTAN antagonist
- BOSENTAN antagonist
Related proteins · sequence + function similarity
- Endothelin-1 receptor 1.00
- Endothelin-1 receptor 1.00
- Endothelin-1 receptor 1.00
- Endothelin-1 receptor 1.00
- Endothelin-1 receptor 0.99
- Endothelin-1 receptor 0.99
- Endothelin receptor type B 0.91
- Endothelin receptor type B 0.90
- Endothelin receptor type B 0.90
- Endothelin receptor type B 0.90
- Endothelin receptor type B 0.90
- Endothelin receptor type B 0.89
Co-cited proteins · studied together in the literature
- Endothelin receptor type B 3 shared papers
- Histone deacetylase 7 1 shared papers
- Endothelin-2 1 shared papers
- Endothelin-1 1 shared papers
- Endothelin-3 1 shared papers
- Histone acetyltransferase KAT5 1 shared papers
Literature · 16 cited papers
- Mutations in the endothelin receptor type A cause mandibulofacial dysostosis with alopecia. Am. J. Hum. Genet. · 2015
- The consensus coding sequences of human breast and colorectal cancers. Science · 2006
- Generation and annotation of the DNA sequences of human chromosomes 2 and 4. Nature · 2005
- The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
- Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat. Genet. · 2004
- Tip60 and HDAC7 interact with the endothelin receptor a and may be involved in downstream signaling. J. Biol. Chem. · 2001
- Endothelin-1 and ETA receptor expression in vascular smooth muscle cells from human placenta: a new ETA receptor messenger ribonucleic acid is generated by alternative splicing of exon 3. J. Clin. Endocrinol. Metab. · 1997
- Alternative RNA splicing of the human endothelin-A receptor generates multiple transcripts. Biochem. J. · 1996
- Molecular characterization and regulation of the human endothelin receptors. J. Biol. Chem. · 1993
- Molecular characterization of the 5'-flanking region of human genomic ETA gene. Biochem. Biophys. Res. Commun. · 1993
- Cloning and characterization of cDNA encoding human A-type endothelin receptor. Biochem. Biophys. Res. Commun. · 1991
- Cloning and chromosomal localization of a human endothelin ETA receptor. Biochem. Biophys. Res. Commun. · 1991
- … and 4 more in the literature graph
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