Structure of PDB 2gtm Chain A
Receptor sequence
>2gtmA (length=341) Species:
10090
(Mus musculus) [
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RPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGHRVAVKK
LSRPFQSIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYL
VTHLMGADLNNIVKLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLA
VNEDCELKILDFGLARHTDDYVATRWYRAPEIMLNWMHYNQTVDIWSVGC
IMAELLTGRTLFPGTDHIDQLKLILRLVGTPGAELLKKISSESARNYIQS
LAQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAAQALAHAYFAQY
HDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPP
3D structure
PDB
2gtm
The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production.
Chain
A
Resolution
1.9 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB)
D150 K152 N155 D168 T185
Catalytic site (residue number reindexed from 1)
D143 K145 N148 D161 T174
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
LID
A
V30 A51 K53 L75 T106 H107 L108 M109 G110 A111 L167 G170 L171
V26 A47 K49 L71 T102 H103 L104 M105 G106 A107 L160 G163 L164
MOAD
: ic50=542nM
Gene Ontology
Molecular Function
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:0016301
kinase activity
GO:0019899
enzyme binding
GO:0019903
protein phosphatase binding
GO:0048273
mitogen-activated protein kinase p38 binding
GO:0051525
NFAT protein binding
GO:0106310
protein serine kinase activity
Biological Process
GO:0000077
DNA damage checkpoint signaling
GO:0000165
MAPK cascade
GO:0000902
cell morphogenesis
GO:0001502
cartilage condensation
GO:0001525
angiogenesis
GO:0001649
osteoblast differentiation
GO:0001890
placenta development
GO:0002021
response to dietary excess
GO:0002062
chondrocyte differentiation
GO:0006006
glucose metabolic process
GO:0006355
regulation of DNA-templated transcription
GO:0006357
regulation of transcription by RNA polymerase II
GO:0006366
transcription by RNA polymerase II
GO:0006468
protein phosphorylation
GO:0006915
apoptotic process
GO:0006974
DNA damage response
GO:0007178
cell surface receptor protein serine/threonine kinase signaling pathway
GO:0007519
skeletal muscle tissue development
GO:0010628
positive regulation of gene expression
GO:0010831
positive regulation of myotube differentiation
GO:0016310
phosphorylation
GO:0018105
peptidyl-serine phosphorylation
GO:0019395
fatty acid oxidation
GO:0030278
regulation of ossification
GO:0030316
osteoclast differentiation
GO:0031098
stress-activated protein kinase signaling cascade
GO:0031281
positive regulation of cyclase activity
GO:0031663
lipopolysaccharide-mediated signaling pathway
GO:0032495
response to muramyl dipeptide
GO:0032496
response to lipopolysaccharide
GO:0032735
positive regulation of interleukin-12 production
GO:0032868
response to insulin
GO:0035331
negative regulation of hippo signaling
GO:0035556
intracellular signal transduction
GO:0035924
cellular response to vascular endothelial growth factor stimulus
GO:0035994
response to muscle stretch
GO:0038066
p38MAPK cascade
GO:0042307
positive regulation of protein import into nucleus
GO:0042770
signal transduction in response to DNA damage
GO:0045648
positive regulation of erythrocyte differentiation
GO:0045663
positive regulation of myoblast differentiation
GO:0045944
positive regulation of transcription by RNA polymerase II
GO:0046323
D-glucose import
GO:0046326
positive regulation of D-glucose import
GO:0048010
vascular endothelial growth factor receptor signaling pathway
GO:0048863
stem cell differentiation
GO:0051146
striated muscle cell differentiation
GO:0051403
stress-activated MAPK cascade
GO:0060045
positive regulation of cardiac muscle cell proliferation
GO:0060348
bone development
GO:0071222
cellular response to lipopolysaccharide
GO:0071223
cellular response to lipoteichoic acid
GO:0071356
cellular response to tumor necrosis factor
GO:0071479
cellular response to ionizing radiation
GO:0071493
cellular response to UV-B
GO:0090090
negative regulation of canonical Wnt signaling pathway
GO:0090336
positive regulation of brown fat cell differentiation
GO:0090400
stress-induced premature senescence
GO:0098586
cellular response to virus
GO:0099179
regulation of synaptic membrane adhesion
GO:1900015
regulation of cytokine production involved in inflammatory response
GO:1901741
positive regulation of myoblast fusion
GO:2000379
positive regulation of reactive oxygen species metabolic process
Cellular Component
GO:0000922
spindle pole
GO:0005634
nucleus
GO:0005654
nucleoplasm
GO:0005737
cytoplasm
GO:0005739
mitochondrion
GO:0005829
cytosol
GO:0016607
nuclear speck
GO:0098978
glutamatergic synapse
View graph for
Molecular Function
View graph for
Biological Process
View graph for
Cellular Component
External links
PDB
RCSB:2gtm
,
PDBe:2gtm
,
PDBj:2gtm
PDBsum
2gtm
PubMed
16750367
UniProt
P47811
|MK14_MOUSE Mitogen-activated protein kinase 14 (Gene Name=Mapk14)
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