Structure of PDB 8vex Chain A
Receptor sequence
>8vexA (length=625) Species:
9606
(Homo sapiens) [
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RVSSGRDLNCVPEIADTLGAVAKQGFDFLCMPVFHPRFKREFIQEPAKNR
PGPQTRSDLLLSGRDWNTLIVGKLSPWIRPDSKVEKIRRNSEAAMLQELN
FGAYLGLPAFLLPLNQEDNTNLARVLTNHIHTGHHSSMFWMRVPLVAPED
LRDDIIENAPTTHTEEYSGEEKTWMWWHNFRTLCDYSKRIAVALEIGADL
PSNHVIDRWLGEPIKAAILPTSIFLTNKKGFPVLSKMHQRLIFRLLKLEV
QFIITGTNHHSEKEFCSYLQYLEYLSQNRPPPNAYELFAKGYEDYLQSPL
QPLMDNLESQTYEVFEKDPIKYSQYQQAIYKCLLDRVPEEEKDTNVQVLM
VLGAGRGPLVNASLRAAKQADRRIKLYAVEKNPNAVVTLENWQFEEWGSQ
VTVVSSDMREWVAPEKADIIVSELLGSFADNELSPECLDGAQHFLKDDGV
SIPGEYTSFLAPISSSKLYNEVRACREKDRDPEAQFEMPYVVRLHNFHQL
SAPQPCFTFSHPNRDPMIDNNRYCTLEFPVEVNTVLHGFAGYFETVLYQD
ITLSIRPETHSPGMFSWFPILFPIKQPITVREGQTICVRFWRCSNSKKVW
YEWAVTAPVCSAIHNPTGRSYTIGL
3D structure
PDB
8vex
Discovery of TNG908: A Selective, Brain Penetrant, MTA-Cooperative PRMT5 Inhibitor That Is Synthetically Lethal with MTAP -Deleted Cancers.
Chain
A
Resolution
2.79 Å
3D
structure
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Enzymatic activity
Enzyme Commision number
2.1.1.320
: type II protein arginine methyltransferase.
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
MTA
A
P314 L315 Y324 G365 E392 K393 N394 D419 M420
P302 L303 Y312 G353 E380 K381 N382 D407 M408
BS02
A1AAR
A
Q309 S310 F327 E435 L437 E444 S578 W579 F580
Q297 S298 F315 E423 L425 E432 S566 W567 F568
Gene Ontology
Molecular Function
GO:0002039
p53 binding
GO:0003714
transcription corepressor activity
GO:0005515
protein binding
GO:0008168
methyltransferase activity
GO:0008327
methyl-CpG binding
GO:0008469
histone arginine N-methyltransferase activity
GO:0016274
protein-arginine N-methyltransferase activity
GO:0035243
protein-arginine omega-N symmetric methyltransferase activity
GO:0042054
histone methyltransferase activity
GO:0042802
identical protein binding
GO:0043021
ribonucleoprotein complex binding
GO:0044020
histone H4R3 methyltransferase activity
GO:0044877
protein-containing complex binding
GO:0046982
protein heterodimerization activity
GO:0070888
E-box binding
GO:0140938
histone H3 methyltransferase activity
Biological Process
GO:0000387
spliceosomal snRNP assembly
GO:0006325
chromatin organization
GO:0006338
chromatin remodeling
GO:0006353
DNA-templated transcription termination
GO:0006355
regulation of DNA-templated transcription
GO:0006479
protein methylation
GO:0007088
regulation of mitotic nuclear division
GO:0010468
regulation of gene expression
GO:0018216
peptidyl-arginine methylation
GO:0032259
methylation
GO:0032922
circadian regulation of gene expression
GO:0035246
peptidyl-arginine N-methylation
GO:0042118
endothelial cell activation
GO:0044027
negative regulation of gene expression via chromosomal CpG island methylation
GO:0045596
negative regulation of cell differentiation
GO:0045892
negative regulation of DNA-templated transcription
GO:0048026
positive regulation of mRNA splicing, via spliceosome
GO:0048511
rhythmic process
GO:0048714
positive regulation of oligodendrocyte differentiation
GO:0070372
regulation of ERK1 and ERK2 cascade
GO:0090161
Golgi ribbon formation
GO:0097421
liver regeneration
GO:1901796
regulation of signal transduction by p53 class mediator
GO:1904992
positive regulation of adenylate cyclase-inhibiting dopamine receptor signaling pathway
Cellular Component
GO:0000785
chromatin
GO:0005634
nucleus
GO:0005654
nucleoplasm
GO:0005694
chromosome
GO:0005737
cytoplasm
GO:0005794
Golgi apparatus
GO:0005829
cytosol
GO:0032991
protein-containing complex
GO:0034709
methylosome
GO:0035097
histone methyltransferase complex
View graph for
Molecular Function
View graph for
Biological Process
View graph for
Cellular Component
External links
PDB
RCSB:8vex
,
PDBe:8vex
,
PDBj:8vex
PDBsum
8vex
PubMed
38595098
UniProt
O14744
|ANM5_HUMAN Protein arginine N-methyltransferase 5 (Gene Name=PRMT5)
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