Structure of PDB 7m4t Chain A
Receptor sequence
>7m4tA (length=481) Species:
9606
(Homo sapiens) [
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GLKAAQKTLFPLRSIDDVVRLFAAELGREEPDLVLLSLVLGFVEHFLAVN
RVIPTNVPELTFQPSPAPDGLTYFPVADLSIIAALYARFTAQIRGAVDLS
LYPREGGVSSRELVKKVSDVIWNSLSRSYFKDRAHIQSLFSFITGTKLDS
SGVAFAVVGACQALGLRDVHLALSEDHAWVVFGPNGEQTAEVTWHGKGNE
DRRGQTVNAGVAERSWLYLKGSYMRCDRKMEVAFMVCAINPSIDLHTDSL
ELLQLQQKLLWLLYDLGHLERYPMALGNLADLEELEPTPGRPDPLTLYHK
GIASAKTYYRDEHIYPYMYLAGYHCRNRNVREALQAWADTATVIQDYNYC
REDEEIYKEFFEVANDVIPNLLKEAASLLEASALQDPECFAHLLRFYDGI
CKWEEGSPTPVLHVGWATFLVQSLGRFEGQVRQKVRIVSGTVAGTARGPV
LTFQSEKMKGMKELLVATKINSSAIKLQLTA
3D structure
PDB
7m4t
Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression.
Chain
A
Resolution
2.74 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
YQV
A
S178 E179 D180 H181 F238 C241 A242 M278 Y319 M322 Y323 C329 E363 V367
S174 E175 D176 H177 F234 C237 A238 M274 Y315 M318 Y319 C325 E359 V363
BS02
7PR
A
E366 D370
E362 D366
BS03
7PR
A
R131 W198
R127 W194
BS04
7PR
A
S246 D252
S242 D248
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:7m4t
,
PDBe:7m4t
,
PDBj:7m4t
PDBsum
7m4t
PubMed
34196551
UniProt
O00255
|MEN1_HUMAN Menin (Gene Name=MEN1)
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