Details of the Target

General Information of Target

Target ID LDTP12732
Target Name Hypoxia-inducible factor 1-alpha inhibitor (HIF1AN)
Gene Name HIF1AN
Gene ID 55662
Synonyms
FIH1; Hypoxia-inducible factor 1-alpha inhibitor; EC 1.14.11.30; EC 1.14.11.n4; Factor inhibiting HIF-1; FIH-1; Hypoxia-inducible factor asparagine hydroxylase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MELVAGCYEQVLFGFAVHPEPEACGDHEQWTLVADFTHHAHTASLSAVAVNSRFVVTGSK
DETIHIYDMKKKIEHGALVHHSGTITCLKFYGNRHLISGAEDGLICIWDAKKWECLKSIK
AHKGQVTFLSIHPSGKLALSVGTDKTLRTWNLVEGRSAFIKNIKQNAHIVEWSPRGEQYV
VIIQNKIDIYQLDTASISGTITNEKRISSVKFLSESVLAVAGDEEVIRFFDCDSLVCLCE
FKAHENRVKDMFSFEIPEHHVIVSASSDGFIKMWKLKQDKKVPPSLLCEINTNARLTCLG
VWLDKVADMKESLPPAAEPSPVSKEQSKIGKKEPGDTVHKEEKRSKPNTKKRGLTGDSKK
ATKESGLISTKKRKMVEMLEKKRKKKKIKTMQ
Target Bioclass
Enzyme
Subcellular location
Nucleus
Function
Hydroxylates HIF-1 alpha at 'Asn-803' in the C-terminal transactivation domain (CAD). Functions as an oxygen sensor and, under normoxic conditions, the hydroxylation prevents interaction of HIF-1 with transcriptional coactivators including Cbp/p300-interacting transactivator. Involved in transcriptional repression through interaction with HIF1A, VHL and histone deacetylases. Hydroxylates specific Asn residues within ankyrin repeat domains (ARD) of NFKB1, NFKBIA, NOTCH1, ASB4, PPP1R12A and several other ARD-containing proteins. Also hydroxylates Asp and His residues within ARDs of ANK1 and TNKS2, respectively. Negatively regulates NOTCH1 activity, accelerating myogenic differentiation. Positively regulates ASB4 activity, promoting vascular differentiation.
Uniprot ID
Q9NWT6
Ensemble ID
ENST00000299163.7
HGNC ID
HGNC:17113
ChEMBL ID
CHEMBL5909

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
IA-alkyne
 Probe Info  		N.A.  LDD0165  [1]
PAL-AfBPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C197
 Probe Info  		22.16  LDD1873  [2]
C228
 Probe Info  		19.84  LDD1901  [2]
C367
 Probe Info  		5.31  LDD2028  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Poly [ADP-ribose] polymerase tankyrase-1 (TNKS) ARTD/PARP family O95271
Poly [ADP-ribose] polymerase tankyrase-2 (TNKS2) ARTD/PARP family Q9H2K2
Ubiquitin thioesterase OTUB1 (OTUB1) Peptidase C65 family Q96FW1
Ankyrin repeat and protein kinase domain-containing protein 1 (ANKK1) TKL Ser/Thr protein kinase family Q8NFD2
Integrin-linked protein kinase (ILK) TKL Ser/Thr protein kinase family Q13418
Receptor-interacting serine/threonine-protein kinase 4 (RIPK4) TKL Ser/Thr protein kinase family P57078
Transcription factor
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
NF-kappa-B inhibitor alpha (NFKBIA) NF-kappa-B inhibitor family P25963
Hypoxia-inducible factor 1-alpha (HIF1A) . Q16665
Nuclear factor NF-kappa-B p105 subunit (NFKB1) . P19838
Other
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ankyrin repeat and SOCS box protein 9 (ASB9) Ankyrin SOCS box (ASB) family Q96DX5
Protein fem-1 homolog B (FEM1B) Fem-1 family Q9UK73
26S proteasome non-ATPase regulatory subunit 10 (PSMD10) . O75832
Amyloid-beta A4 precursor protein-binding family A member 3 (APBA3) . O96018
Ankyrin repeat domain-containing protein 37 (ANKRD37) . Q7Z713
Ankyrin repeat domain-containing protein 49 (ANKRD49) . Q8WVL7
Uveal autoantigen with coiled-coil domains and ankyrin repeats (UACA) . Q9BZF9

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
D-tartaric Acid Small molecular drug DB01694
N-(Carboxycarbonyl)-d-phenylalanine . DB08263

References

1 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
2 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587