Endothelin-1 receptor

Details

Name
Endothelin-1 receptor
Synonyms
  • Endothelin receptor type A
  • ET-A
  • ETA
  • ETA-R
  • ETRA
  • hET-AR
Gene Name
EDNRA
UniProtKB Entry
P25101Swiss-Prot
Organism
Humans
NCBI Taxonomy ID
9606
Amino acid sequence
>lcl|BSEQ0001040|Endothelin-1 receptor
METLCLRASFWLALVGCVISDNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLP
SNGSMHNYCPQQTKITSAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIA
SLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALS
VDRYRAVASWSRVQGIGIPLVTAIEIVSIWILSFILAIPEAIGFVMVPFEYRGEQHKTCM
LNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQ
RREVAKTVFCLVVIFALCWFPLHLSRILKKTVYNEMDKNRCELLSFLLLMDYIGINLATM
NSCINPIALYFVSKKFKNCFQSCLCCCCYQSKSLMTSVPMNGTSIQWKNHDQNNHNTDRS
SHKDSMN
Number of residues
427
Molecular Weight
48721.76
Theoretical pI
8.41
GO Classification
Processes
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway / aorta development / atrial cardiac muscle tissue development / axon extension / axonogenesis involved in innervation / blood vessel remodeling / branching involved in blood vessel morphogenesis / calcium ion transmembrane transport / canonical Wnt signaling pathway / cardiac chamber formation / cardiac neural crest cell migration involved in outflow tract morphogenesis / cell population proliferation / cellular response to follicle-stimulating hormone stimulus / cellular response to human chorionic gonadotropin stimulus / cellular response to luteinizing hormone stimulus / cellular response to oxidative stress / cranial skeletal system development / developmental pigmentation / embryonic heart tube development / embryonic skeletal system development / endothelin receptor signaling pathway involved in heart process / establishment of endothelial barrier / face development / G protein-coupled receptor signaling pathway / gene expression / glomerular endothelium development / glomerular filtration / heparin metabolic process / intracellular calcium ion homeostasis / left ventricular cardiac muscle tissue morphogenesis / meiotic cell cycle process involved in oocyte maturation / mesenchymal cell apoptotic process / middle ear morphogenesis / mitochondrion organization / mitotic cell cycle / neural crest cell fate commitment / neuromuscular process / neuron remodeling / noradrenergic neuron differentiation / norepinephrine metabolic process / pharyngeal arch artery morphogenesis / phospholipase C-activating G protein-coupled receptor signaling pathway / podocyte apoptotic process / podocyte differentiation / positive regulation of canonical NF-kappaB signal transduction / positive regulation of cation channel activity / protein kinase A signaling / protein transmembrane transport / regulation of glucose transmembrane transport / regulation of heart rate / regulation of protein localization to cell leading edge / renal albumin absorption / renal sodium ion absorption / respiratory gaseous exchange by respiratory system / response to acetylcholine / response to amphetamine / response to wounding / semaphorin-plexin signaling pathway involved in axon guidance / sodium ion homeostasis / sympathetic nervous system development / sympathetic neuron axon guidance / thyroid gland development / vascular associated smooth muscle cell development
General 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
Specific Function
endothelin receptor activity
Pfam Domain Function
Signal Regions
1-20
Transmembrane Regions
81-102 113-132 160-181 206-229 257-278 307-328 348-372
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0010366|Endothelin-1 receptor (EDNRA)
ATGGAAACCCTTTGCCTCAGGGCATCCTTTTGGCTGGCACTGGTTGGATGTGTAATCAGT
GATAATCCTGAGAGATACAGCACAAATCTAAGCAATCATGTGGATGATTTCACCACTTTT
CGTGGCACAGAGCTCAGCTTCCTGGTTACCACTCATCAACCCACTAATTTGGTCCTACCC
AGCAATGGCTCAATGCACAACTATTGCCCACAGCAGACTAAAATTACTTCAGCTTTCAAA
TACATTAACACTGTGATATCTTGTACTATTTTCATCGTGGGAATGGTGGGGAATGCAACT
CTGCTCAGGATCATTTACCAGAACAAATGTATGAGGAATGGCCCCAACGCGCTGATAGCC
AGTCTTGCCCTTGGAGACCTTATCTATGTGGTCATTGATCTCCCTATCAATGTATTTAAG
TTCTACCAAGATGTAAAGGACTGGTGGCTCTTCGGGTTCTATTTCTGTATGCCCTTGGTG
TGCACTGCGATCTTCTACACCCTCATGACTTGTGAGATGTTGAACAGAAGGAATGGCAGC
TTGAGAATTGCCCTCAGTGAACATCTTAAGCAGCGTCGAGAAGTGGCAAAAACAGTTTTC
TGCTTGGTTGTAATTTTTGCTCTTTGCTGGTTCCCTCTTCATTTAAGCCGTATATTGAAG
AAAACTGTGTATAACGAGATGGACAAGAACCGATGTGAATTACTTAGTTTCTTACTGCTC
ATGGATTACATCGGTATTAACTTGGCAACCATGAATTCATGTATAAACCCCATAGCTCTG
TATTTTGTGAGCAAGAAATTTAAAAATTGTTTCCAGTCATGCCTCTGCTGCTGCTGTTAC
CAGTCCAAAAGTCTGATGACCTCGGTCCCCATGAACGGAACAAGCATCCAGTGGAAGAAC
CACGATCAAAACAACCACAACACAGACCGGAGCAGCCATAAGGACAGCATGAACTGA
Chromosome Location
4
Locus
4q31.22-q31.23
External Identifiers
ResourceLink
UniProtKB IDP25101
UniProtKB Entry NameEDNRA_HUMAN
GenBank Protein ID238636
GenBank Gene IDS63938
GeneCard IDEDNRA
GenAtlas IDEDNRA
HGNC IDHGNC:3179
PDB ID(s)8HCQ
KEGG IDhsa:1909
IUPHAR/Guide To Pharmacology ID219
NCBI Gene ID1909
General References
  1. Adachi M, Yang YY, Furuichi Y, Miyamoto C: Cloning and characterization of cDNA encoding human A-type endothelin receptor. Biochem Biophys Res Commun. 1991 Nov 14;180(3):1265-72. [Article]
  2. Cyr C, Huebner K, Druck T, Kris R: Cloning and chromosomal localization of a human endothelin ETA receptor. Biochem Biophys Res Commun. 1991 Nov 27;181(1):184-90. [Article]
  3. Hosoda K, Nakao K, Hiroshi-Arai, Suga S, Ogawa Y, Mukoyama M, Shirakami G, Saito Y, Nakanishi S, Imura H: Cloning and expression of human endothelin-1 receptor cDNA. FEBS Lett. 1991 Aug 5;287(1-2):23-6. [Article]
  4. Arai H, Nakao K, Hosoda K, Ogawa Y, Nakagawa O, Komatsu Y, Imura H: [Molecular cloning of human endothelin receptors and their expression in vascular endothelial cells and smooth muscle cells]. Jpn Circ J. 1992;56 Suppl 5:1303-7. [Article]
  5. Elshourbagy NA, Korman DR, Wu HL, Sylvester DR, Lee JA, Nuthalaganti P, Bergsma DJ, Kumar CS, Nambi P: Molecular characterization and regulation of the human endothelin receptors. J Biol Chem. 1993 Feb 25;268(6):3873-9. [Article]
  6. Hosoda K, Nakao K, Tamura N, Arai H, Ogawa Y, Suga S, Nakanishi S, Imura H: Organization, structure, chromosomal assignment, and expression of the gene encoding the human endothelin-A receptor. J Biol Chem. 1992 Sep 15;267(26):18797-804. [Article]
  7. Hayzer DJ, Rose PM, Lynch JS, Webb ML, Kienzle BK, Liu EC, Bogosian EA, Brinson E, Runge MS: Cloning and expression of a human endothelin receptor: subtype A. Am J Med Sci. 1992 Oct;304(4):231-8. [Article]
  8. Miyamoto Y, Yoshimasa T, Arai H, Takaya K, Ogawa Y, Itoh H, Nakao K: Alternative RNA splicing of the human endothelin-A receptor generates multiple transcripts. Biochem J. 1996 Feb 1;313 ( Pt 3):795-801. [Article]
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  12. Yang H, Tabuchi H, Furuichi Y, Miyamoto C: Molecular characterization of the 5'-flanking region of human genomic ETA gene. Biochem Biophys Res Commun. 1993 Jan 29;190(2):332-9. [Article]
  13. Bourgeois C, Robert B, Rebourcet R, Mondon F, Mignot TM, Duc-Goiran P, Ferre F: 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 Sep;82(9):3116-23. [Article]
  14. Lee HJ, Chun M, Kandror KV: Tip60 and HDAC7 interact with the endothelin receptor a and may be involved in downstream signaling. J Biol Chem. 2001 May 18;276(20):16597-600. Epub 2001 Mar 21. [Article]
  15. Gordon CT, Weaver KN, Zechi-Ceide RM, Madsen EC, Tavares AL, Oufadem M, Kurihara Y, Adameyko I, Picard A, Breton S, Pierrot S, Biosse-Duplan M, Voisin N, Masson C, Bole-Feysot C, Nitschke P, Delrue MA, Lacombe D, Guion-Almeida ML, Moura PP, Garib DG, Munnich A, Ernfors P, Hufnagel RB, Hopkin RJ, Kurihara H, Saal HM, Weaver DD, Katsanis N, Lyonnet S, Golzio C, Clouthier DE, Amiel J: Mutations in the endothelin receptor type A cause mandibulofacial dysostosis with alopecia. Am J Hum Genet. 2015 Apr 2;96(4):519-31. doi: 10.1016/j.ajhg.2015.01.015. Epub 2015 Mar 12. [Article]
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Associated Data

Bio-Entities
Bio-EntityType
Endothelin-1 receptor (Humans)protein
primary
Drug Relations
DrugDrug groupPharmacological action?TypeActionsDetails
Bosentanapproved, investigationalyestargetantagonistDetails
DarusentaninvestigationalyestargetantagonistDetails
Sparsentanapproved, investigationalyestargetantagonistDetails
SPP 301investigationalunknowntargetDetails
Actelion-1investigationalunknowntargetDetails
Ambrisentanapproved, investigationalyestargetantagonistDetails
AtrasentaninvestigationalyestargetantagonistDetails
TezosentaninvestigationalunknowntargetDetails
2-HYDROXY-3,5-DIIODOBENZOIC ACIDexperimentalyestargetinhibitorDetails
Sitaxentanapproved, investigational, withdrawnyestargetantagonistDetails
MacitentanapprovedyestargetantagonistDetails
Acetylsalicylic acidapproved, vet_approvedunknowntargetinhibitorDetails
ClazosentaninvestigationalyestargetantagonistDetails
EnrasentaninvestigationalyestargetmodulatorDetails
Aprocitentanapproved, investigationalyestargetantagonistDetails
ZibotentaninvestigationalyestargetantagonistDetails
TBC-3711investigationalyestargetantagonistDetails
BQ-123investigationalyestargetantagonistDetails