General Information of Target

Target ID LDTP02105
Target Name Endothelin-1 (EDN1)
Gene Name EDN1
Gene ID 1906
Synonyms
Endothelin-1; Preproendothelin-1; PPET1) [Cleaved into: Endothelin-1; ET-1; Big endothelin-1]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDYLLMIFSLLFVACQGAPETAVLGAELSAVGENGGEKPTPSPPWRLRRSKRCSCSSLMD
KECVYFCHLDIIWVNTPEHVVPYGLGSPRSKRALENLLPTKATDRENRCQCASQKDKKCW
NFCQAGKELRAEDIMEKDWNNHKKGKDCSKLGKKCIYQQLVRGRKIRRSSEEHLRQTRSE
TMRNSVKSSFHDPKLKGKPSRERYVTHNRAHW
Target Type
Literature-reported
Target Bioclass
Other
Family
Endothelin/sarafotoxin family
Subcellular location
Secreted
Function
Endothelins are endothelium-derived vasoconstrictor peptides. Probable ligand for G-protein coupled receptors EDNRA and EDNRB which activates PTK2B, BCAR1, BCAR3 and, GTPases RAP1 and RHOA cascade in glomerular mesangial cells. Also binds the DEAR/FBXW7-AS1 receptor. Promotes mesenteric arterial wall remodeling via activation of ROCK signaling and subsequent colocalization of NFATC3 with F-actin filaments. NFATC3 then translocates to the nucleus where it subsequently promotes the transcription of the smooth muscle hypertrophy and differentiation marker ACTA2.
TTD ID
T25076
Uniprot ID
P05305
DrugMap ID
TTJR60Z
Ensemble ID
ENST00000379375.6
HGNC ID
HGNC:3176

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C155(19.70)  LDD2236  [1]

References

1 Global profiling of phosphorylation-dependent changes in cysteine reactivity. Nat Methods. 2022 Mar;19(3):341-352. doi: 10.1038/s41592-022-01398-2. Epub 2022 Feb 28.
Mass spectrometry data entry: PXD026730