Endothelin-1 receptor

Details

Name
Endothelin-1 receptor
Synonyms
  • Endothelin A receptor
  • ET-A
  • ETA
  • ETA-R
  • ETRA
  • hET-AR
Gene Name
EDNRA
Organism
Humans
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
Functions
endothelin receptor activity / phosphatidylinositol phospholipase C activity
Processes
activation of adenylate cyclase activity / activation of phospholipase C activity / artery smooth muscle contraction / cell proliferation / endothelin receptor signaling pathway / enteric nervous system development / G-protein coupled receptor signaling pathway / glucose transport / head development / heart development / in utero embryonic development / negative regulation of cAMP biosynthetic process / neural crest cell development / patterning of blood vessels / positive regulation of cytosolic calcium ion concentration / regulation of blood pressure / respiratory gaseous exchange / response to hypoxia / signal transduction / smooth muscle contraction / vasoconstriction
Components
cytosol / integral component of plasma membrane / plasma membrane
General Function
Phosphatidylinositol phospholipase c activity
Specific 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.
Pfam Domain Function
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
4q31.23
External Identifiers
ResourceLink
UniProtKB IDP25101
UniProtKB Entry NameEDNRA_HUMAN
GenBank Protein ID238636
GenBank Gene IDS63938
GenAtlas IDEDNRA
HGNC IDHGNC:3179
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. [PubMed:1719979]
  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. [PubMed:1659806]
  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. [PubMed:1652463]
  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. [PubMed:1291713]
  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. [PubMed:8440682]
  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. [PubMed:1326535]
  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. [PubMed:1415318]
  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. [PubMed:8611157]
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Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB00559Bosentanapproved, investigationalyesantagonistDetails
DB04883DarusentaninvestigationalunknownDetails
DB12548SparsentaninvestigationalunknownDetails
DB05290SPP 301investigationalunknownDetails
DB05367Actelion-1investigationalunknownDetails
DB06403Ambrisentanapproved, investigationalyesantagonistDetails
DB06199AtrasentaninvestigationalunknownDetails
DB06558TezosentaninvestigationalunknownDetails
DB046742-HYDROXY-3,5-DIIODOBENZOIC ACIDexperimentalunknownDetails
DB06268Sitaxentanapproved, investigational, withdrawnyesantagonistDetails
DB08932MacitentanapprovedyesantagonistDetails
DB00945Acetylsalicylic acidapproved, vet_approvedunknowninhibitorDetails
DB06677ClazosentaninvestigationalunknownDetails
DB06460EnrasentaninvestigationalunknownDetails