Structure of PDB 7nr8 Chain A
Receptor sequence
>7nr8A (length=346) Species:
9606
(Homo sapiens) [
Search protein sequence
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PEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFE
HQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMET
DLYKLLKTQHLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTT
CDLKICDFGLARVADPDHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSID
IWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINLKA
RNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHKRIEVEQALAH
PYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQP
3D structure
PDB
7nr8
Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
Chain
A
Resolution
1.627 Å
3D
structure
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Enzymatic activity
Enzyme Commision number
2.7.11.24
: mitogen-activated protein kinase.
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
UOE
A
Y36 V39 A52 K54 Y64 R67 Q105 M108 E109 T110 K114 D167
Y26 V29 A42 K44 Y54 R57 Q95 M98 E99 T100 K104 D157
BindingDB: IC50=3.10nM
Gene Ontology
Molecular Function
GO:0001784
phosphotyrosine residue binding
GO:0003677
DNA binding
GO:0004672
protein kinase activity
GO:0004674
protein serine/threonine kinase activity
GO:0004707
MAP kinase activity
GO:0005515
protein binding
GO:0005524
ATP binding
GO:0008353
RNA polymerase II CTD heptapeptide repeat kinase activity
GO:0016301
kinase activity
GO:0019902
phosphatase binding
GO:0042802
identical protein binding
GO:0106310
protein serine kinase activity
Biological Process
GO:0000165
MAPK cascade
GO:0006357
regulation of transcription by RNA polymerase II
GO:0006468
protein phosphorylation
GO:0006915
apoptotic process
GO:0006935
chemotaxis
GO:0006974
DNA damage response
GO:0007165
signal transduction
GO:0007166
cell surface receptor signaling pathway
GO:0007268
chemical synaptic transmission
GO:0007507
heart development
GO:0007611
learning or memory
GO:0008286
insulin receptor signaling pathway
GO:0009887
animal organ morphogenesis
GO:0010759
positive regulation of macrophage chemotaxis
GO:0010800
positive regulation of peptidyl-threonine phosphorylation
GO:0014032
neural crest cell development
GO:0014044
Schwann cell development
GO:0016310
phosphorylation
GO:0018105
peptidyl-serine phosphorylation
GO:0018107
peptidyl-threonine phosphorylation
GO:0019858
cytosine metabolic process
GO:0030278
regulation of ossification
GO:0030521
androgen receptor signaling pathway
GO:0030641
regulation of cellular pH
GO:0030878
thyroid gland development
GO:0031647
regulation of protein stability
GO:0031663
lipopolysaccharide-mediated signaling pathway
GO:0032206
positive regulation of telomere maintenance
GO:0032496
response to lipopolysaccharide
GO:0032872
regulation of stress-activated MAPK cascade
GO:0033554
cellular response to stress
GO:0033598
mammary gland epithelial cell proliferation
GO:0034198
cellular response to amino acid starvation
GO:0035094
response to nicotine
GO:0035556
intracellular signal transduction
GO:0038127
ERBB signaling pathway
GO:0038133
ERBB2-ERBB3 signaling pathway
GO:0042473
outer ear morphogenesis
GO:0042552
myelination
GO:0043330
response to exogenous dsRNA
GO:0043401
steroid hormone receptor signaling pathway
GO:0045542
positive regulation of cholesterol biosynthetic process
GO:0045596
negative regulation of cell differentiation
GO:0048009
insulin-like growth factor receptor signaling pathway
GO:0048538
thymus development
GO:0050847
progesterone receptor signaling pathway
GO:0050852
T cell receptor signaling pathway
GO:0050853
B cell receptor signaling pathway
GO:0051403
stress-activated MAPK cascade
GO:0051493
regulation of cytoskeleton organization
GO:0060020
Bergmann glial cell differentiation
GO:0060291
long-term synaptic potentiation
GO:0060324
face development
GO:0060425
lung morphogenesis
GO:0060440
trachea formation
GO:0060716
labyrinthine layer blood vessel development
GO:0061308
cardiac neural crest cell development involved in heart development
GO:0070371
ERK1 and ERK2 cascade
GO:0070849
response to epidermal growth factor
GO:0071356
cellular response to tumor necrosis factor
GO:0072584
caveolin-mediated endocytosis
GO:0090170
regulation of Golgi inheritance
GO:0120041
positive regulation of macrophage proliferation
GO:2000641
regulation of early endosome to late endosome transport
Cellular Component
GO:0005576
extracellular region
GO:0005634
nucleus
GO:0005654
nucleoplasm
GO:0005737
cytoplasm
GO:0005739
mitochondrion
GO:0005769
early endosome
GO:0005770
late endosome
GO:0005788
endoplasmic reticulum lumen
GO:0005794
Golgi apparatus
GO:0005813
centrosome
GO:0005819
spindle
GO:0005829
cytosol
GO:0005856
cytoskeleton
GO:0005886
plasma membrane
GO:0005901
caveola
GO:0005925
focal adhesion
GO:0016020
membrane
GO:0031143
pseudopodium
GO:0035578
azurophil granule lumen
GO:0045202
synapse
GO:0070161
anchoring junction
GO:0072686
mitotic spindle
GO:1904813
ficolin-1-rich granule lumen
View graph for
Molecular Function
View graph for
Biological Process
View graph for
Cellular Component
External links
PDB
RCSB:7nr8
,
PDBe:7nr8
,
PDBj:7nr8
PDBsum
7nr8
PubMed
34387469
UniProt
P28482
|MK01_HUMAN Mitogen-activated protein kinase 1 (Gene Name=MAPK1)
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