Structure of PDB 4ai8 Chain A

Receptor sequence
>4ai8A (length=339) Species: 9606 (Homo sapiens) [Search protein sequence]
SGSGEPREEAGALGPAWDESQLRSYSFPTRPIPRLSQSDPRAEELIENEE
PVVLTDTNLVYPALKWDLEYLQENIGNGDFSVYSASTHKFLYYDEKKMAN
FQNFKPRSNREEMKFHEFVEKLQDIQQRGGEERLYLQQTLNDTVGRKIVM
DFLGFNWNWINKQQGKRGWGQLTSNLLLIGMEGNVTPAHYDEQQNFFAQI
KGYKRCILFPPDQFECLYPYPVHHPCDRQSQVDFDNPDYERFPNFQNVVG
YETVVGPGDVLYIPMYWWHHIESLLNGGITITVNFWYKGAPTPKRIEYPL
KAHQKVAIMRNIEKMLGEALGNPQEVGPLLNTMIKGRYN
3D structure
PDB4ai8 Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.
ChainA
Resolution2.4 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 1.14.11.30: hypoxia-inducible factor-asparagine dioxygenase.
1.14.11.n4: ankyrin-repeat-histidine dioxagenase.
Interaction with ligand
Site
#
Ligand Ligand
chain
Binding residues on receptor
(original residue number in PDB)
Binding residues on receptor
(residue number reindexed from 1)
Binding affinity
BS01 DZA A Y145 T196 H199 D201 N205 F207 K214 H279 Y135 T186 H189 D191 N195 F197 K204 H269 MOAD: ic50>100uM
PDBbind-CN: -logKd/Ki=4.00,IC50>100uM
BindingDB: IC50=>100000nM
BS02 ZN A H199 D201 H279 H189 D191 H269
Gene Ontology
Molecular Function
GO:0003714 transcription corepressor activity
GO:0005112 Notch binding
GO:0005515 protein binding
GO:0008198 ferrous iron binding
GO:0008270 zinc ion binding
GO:0019826 oxygen sensor activity
GO:0031406 carboxylic acid binding
GO:0036139 peptidyl-histidine dioxygenase activity
GO:0036140 [protein]-asparagine 3-dioxygenase activity
GO:0042803 protein homodimerization activity
GO:0046872 metal ion binding
GO:0051059 NF-kappaB binding
GO:0051213 dioxygenase activity
GO:0062101 peptidyl-aspartic acid 3-dioxygenase activity
GO:0071532 ankyrin repeat binding
Biological Process
GO:0045663 positive regulation of myoblast differentiation
GO:0045746 negative regulation of Notch signaling pathway
GO:0045892 negative regulation of DNA-templated transcription
GO:2001214 positive regulation of vasculogenesis
Cellular Component
GO:0005634 nucleus
GO:0005654 nucleoplasm
GO:0005737 cytoplasm
GO:0005829 cytosol
GO:0048471 perinuclear region of cytoplasm

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Molecular Function

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Biological Process

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Cellular Component
External links
PDB RCSB:4ai8, PDBe:4ai8, PDBj:4ai8
PDBsum4ai8
PubMed22724510
UniProtQ9NWT6|HIF1N_HUMAN Hypoxia-inducible factor 1-alpha inhibitor (Gene Name=HIF1AN)

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