General Information

  • ID:  hor000860
  • Uniprot ID:  P05305
  • Protein name:  Big endothelin-1
  • Gene name:  EDN1
  • Organism:  Homo sapiens (Human)
  • Family:  Endothelin/sarafotoxin family
  • Source:  Human
  • Expression:  Expressed in lung, placental stem villi vessels and in cultured placental vascular smooth muscle cells.
  • Disease:  Diseases associated with EDN1 include Question Mark Ears, Isolated and Auriculocondylar Syndrome 3.
  • Comments:  NA
  • Taxonomy:  Homo (genus), Homininae (subfamily), Hominidae (family), Hominoidea (superfamily), Catarrhini (parvorder), Simiiformes (infraorder), Haplorrhini (suborder), Primates (order), Euarchontoglires (superorder), Boreoeutheria, Eutheria, Theria, Mammalia (class), Amniota, Tetrapoda, Dipnotetrapodomorpha, Sarcopterygii (superclass), Euteleostomi, Teleostomi, Gnathostomata, Vertebrata, Craniata (subphylum), Chordata (phylum), Deuterostomia, Bilateria, Eumetazoa, Metazoa (kingdom), Opisthokonta, Eukaryota (superkingdom), cellular organisms
  • GO MF:  GO:0005102 signaling receptor binding; GO:0005125 cytokine activity; GO:0005179 hormone activity; GO:0005515 protein binding; GO:0031707 endothelin A receptor binding; GO:0031708 endothelin B receptor binding; GO:0048018 receptor ligand activity
  • GO BP:  GO:0000122 negative regulation of transcription by RNA polymerase II; GO:0000165 MAPK cascade; GO:0001501 skeletal system development; GO:0001516 prostaglandin biosynthetic process; GO:0001569 branching involved in blood vessel morphogenesis; GO:0001666 response to hypoxia; GO:0001701 in utero embryonic development; GO:0001821 histamine secretion; GO:0001975 response to amphetamine; GO:0003015 heart process; GO:0003094 glomerular filtration; GO:0003100 regulation of systemic arterial blood pressure by endothelin; GO:0003253 cardiac neural crest cell migration involved in outflow tract morphogenesis; GO:0003357 noradrenergic neuron differentiation; GO:0006366 transcription by RNA polymerase II; GO:0006874 intracellular calcium ion homeostasis; GO:0006885 regulation of pH; GO:0006939 smooth muscle contraction; GO:0007005 mitochondrion organization; GO:0007166 cell surface receptor signaling pathway; GO:0007186 G protein-coupled receptor signaling pathway; GO:0007193 adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway; GO:0007200 phospholipase C-activating G protein-coupled receptor signaling pathway; GO:0007204 positive regulation of cytosolic calcium ion concentration; GO:0007205 protein kinase C-activating G protein-coupled receptor signaling pathway; GO:0007267 cell-cell signaling; GO:0007411 axon guidance; GO:0007507 heart development; GO:0007585 respiratory gaseous exchange by respiratory system; GO:0007589 body fluid secretion; GO:0008217 regulation of blood pressure; GO:0008284 positive regulation of cell population proliferation; GO:0009410 response to xenobiotic stimulus; GO:0009953 dorsal/ventral pattern formation; GO:0010193 response to ozone; GO:0010460 positive regulation of heart rate; GO:0010467 gene expression; GO:0010595 positive regulation of endothelial cell migration; GO:0010613 positive regulation of cardiac mu
  • GO CC:  GO:0005576 extracellular region; GO:0005615 extracellular space; GO:0005737 cytoplasm; GO:0030133 transport vesicle; GO:0033093 Weibel-Palade body; GO:0045178 basal part of cell; GO:0048237 rough endoplasmic reticulum lumen

Sequence Information

  • Sequence:  CSCSSLMDKECVYFCHLDIIWVNTPEHVVPYGLGSPRS
  • Length:  38(53-90)
  • Propeptide:  MDYLLMIFSLLFVACQGAPETAVLGAELSAVGENGGEKPTPSPPWRLRRSKRCSCSSLMDKECVYFCHLDIIWVNTPEHVVPYGLGSPRSKRALENLLPTKATDRENRCQCASQKDKKCWNFCQAGKELRAEDIMEKDWNNHKKGKDCSKLGKKCIYQQLVRGRKIRRSSEEHLRQTRSETMRNSVKSSFHDPKLKGKPSRERYVTHNRAHW
  • Signal peptide:  MDYLLMIFSLLFVACQG
  • Modification:  NA
  • Glycosylation:  NA
  • Mutagenesis:  NA

Activity

  • Function:  endothelium-derived vasoconstrictor peptides
  • Mechanism:  activates PTK2B, BCAR1, BCAR3 and, GTPases RAP1 and RHOA cascade in glomerular mesangial cells
  • Cross BBB:  NA
  • Target:  EDNRA, EDNRB
  • Target Unid:   P25101, P24530
  • IC50:  NA
  • EC50:  NA
  • ED50:  NA
  • Kd:  NA
  • Half life:  24 (t1/2 of hydrolysis) hours; /86400 seconds ( PubMed ID: 7529108 )

Structure

  • Disulfide bond:  1-15; 3-11
  • Structure ID:  AF-Q9HCQ7-F1(AlphaFold_DB_ID)

  • Structure: (PDB_ID-from https://www.rcsb.org/; AlphaFold_DB_ID-from https://alphafold.ebi.ac.uk/; hordbxxxxxx_AF2.pdb was predicted structure by AlphaFold2; hordbxxxxxx_ESM.pdb was predicted structure by ESMFold)
    •    AF-Q9HCQ7-F1.pdbhor000860_AF2.pdbhor000860_ESM.pdb

Physical Information

Mass: 494708 Formula: C189H286N48O56S5
Absent amino acids: AQ Common amino acids: S
pI: 5.43 Basic residues: 4
Polar residues: 15 Hydrophobic residues: 11
Hydrophobicity: 15.26 Boman Index: -3192
Half-Life / Aliphatic Index: 1.2 hour Aliphatic Index: 81.84
Instability Index: 5942.11 Extinction Coefficient cystines: 8730
Absorbance 280nm: 235.95

Literature

  • PubMed ID:  7529108
  • Title:  Proteolytic processing of big endothelin-3 by the kell blood group protein.