Structure of PDB 8ig0 Chain A
Receptor sequence
>8ig0A (length=486) Species:
9606
(Homo sapiens) [
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GLKAAQKTLFPLRSIDDVVRLFAAELGREEPDLVLLSLVLGFVEHFLAVN
RVIPTNVPELTFQPSPAPDPPGGLTYFPVADLSIIAALYARFTAQIRGAV
DLSLYPREGGVSSRELVKKVSDVIWNSLSRSYFKDRAHIQSLFSFITGTK
LDSSGVAFAVVGACQALGLRDVHLALSEDHAWVVFGPNGEQTAEVTWHGK
GNEDRRGQTVNAGVAERSWLYLKGSYMRCDRKMEVAFMVCAINPSIDLHT
DSLELLQLQQKLLWLLYDLGHLERYPMALGNLADLEELEPTPGRPDPLTL
YHKGIASAKTYYRDEHIYPYMYLAGYHCRNRNVREALQAWADTATVIQDY
NYCREDEEIYKEFFEVANDVIPNLLKEAASLLEASALQDPECFAHLLRFY
DGICKWEEGSPTPVLHVGWATFLVQSLGRFEGQVRQKVRIVSGTVAGTAR
GGPVLTFQSEKMKGMKELLVATKINSSAIKLQLTAQ
3D structure
PDB
8ig0
A novel Menin-MLL1 inhibitor, DS-1594a, prevents the progression of acute leukemia with rearranged MLL1 or mutated NPM1.
Chain
A
Resolution
2.6 Å
3D
structure
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Enzymatic activity
Enzyme Commision number
?
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
7IX
A
S155 L177 H181 A182 F238 Y276 M278 Y319 M322 Y323 C329 W341 E363 V371
S154 L176 H180 A181 F237 Y275 M277 Y318 M321 Y322 C328 W340 E362 V370
Gene Ontology
Molecular Function
GO:0000400
four-way junction DNA binding
GO:0000403
Y-form DNA binding
GO:0000976
transcription cis-regulatory region binding
GO:0003677
DNA binding
GO:0003682
chromatin binding
GO:0003690
double-stranded DNA binding
GO:0005515
protein binding
GO:0030674
protein-macromolecule adaptor activity
GO:0051219
phosphoprotein binding
GO:0070412
R-SMAD binding
Biological Process
GO:0000122
negative regulation of transcription by RNA polymerase II
GO:0000165
MAPK cascade
GO:0001933
negative regulation of protein phosphorylation
GO:0002076
osteoblast development
GO:0006281
DNA repair
GO:0006325
chromatin organization
GO:0006357
regulation of transcription by RNA polymerase II
GO:0006974
DNA damage response
GO:0008285
negative regulation of cell population proliferation
GO:0009411
response to UV
GO:0010332
response to gamma radiation
GO:0030511
positive regulation of transforming growth factor beta receptor signaling pathway
GO:0043433
negative regulation of DNA-binding transcription factor activity
GO:0045064
T-helper 2 cell differentiation
GO:0045668
negative regulation of osteoblast differentiation
GO:0045736
negative regulation of cyclin-dependent protein serine/threonine kinase activity
GO:0045786
negative regulation of cell cycle
GO:0045815
transcription initiation-coupled chromatin remodeling
GO:0045892
negative regulation of DNA-templated transcription
GO:0045944
positive regulation of transcription by RNA polymerase II
GO:0046329
negative regulation of JNK cascade
Cellular Component
GO:0000781
chromosome, telomeric region
GO:0000785
chromatin
GO:0005634
nucleus
GO:0005654
nucleoplasm
GO:0005737
cytoplasm
GO:0005788
endoplasmic reticulum lumen
GO:0005829
cytosol
GO:0016363
nuclear matrix
GO:0017053
transcription repressor complex
GO:0032154
cleavage furrow
GO:0032991
protein-containing complex
GO:0035097
histone methyltransferase complex
GO:0044665
MLL1/2 complex
GO:0071339
MLL1 complex
View graph for
Molecular Function
View graph for
Biological Process
View graph for
Cellular Component
External links
PDB
RCSB:8ig0
,
PDBe:8ig0
,
PDBj:8ig0
PDBsum
8ig0
PubMed
36841758
UniProt
O00255
|MEN1_HUMAN Menin (Gene Name=MEN1)
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