Information on EC 2.7.11.24 - mitogen-activated protein kinase and Organism(s) Mus musculus

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The taxonomic range for the selected organisms is: Mus musculus

The enzyme appears in selected viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.11.24
-
RECOMMENDED NAME
GeneOntology No.
mitogen-activated protein kinase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + a protein = ADP + a phosphoprotein
show the reaction diagram
the kinetics of p38 MAPK follow a rapid-equilibrium random-order ternary-complex mechanism, the enzyme is highly specific for Ser-Pro or Thr-Pro motifs
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
SYSTEMATIC NAME
IUBMB Comments
ATP:protein phosphotransferase (MAPKK-activated)
Phosphorylation of specific tyrosine and threonine residues in the activation loop of this enzyme by EC 2.7.12.2, mitogen-activated protein kinase kinase (MAPKK) is necessary for enzyme activation. Once activated, the enzyme phosphorylates target substrates on serine or threonine residues followed by a proline [6]. A distinguishing feature of all MAPKs is the conserved sequence Thr-Xaa-Tyr (TXY). Mitogen-activated protein kinase (MAPK) signal transduction pathways are among the most widespread mechanisms of cellular regulation. Mammalian MAPK pathways can be recruited by a wide variety of stimuli including hormones (e.g. insulin and growth hormone), mitogens (e.g. epidermal growth factor and platelet-derived growth factor), vasoactive peptides (e.g. angiotensin-II and endothelin), inflammatory cytokines of the tumour necrosis factor (TNF) family and environmental stresses such as osmotic shock, ionizing radiation and ischaemic injury.
CAS REGISTRY NUMBER
COMMENTARY hide
142243-02-5
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
metabolism
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + activating transcription factor 2
ADP + phosphorylated activating transcription factor 2
show the reaction diagram
ATP + ATF-2
ADP + phosphorylated ATF-2
show the reaction diagram
-
substrate in kinase assay
-
-
?
ATP + ATF2
ADP + phosphorylated ATF2
show the reaction diagram
phosphorylation by p38 MAPK at threonine residues
-
-
?
ATP + ATF2DELTA109
ADP + phosphorylated ATF2DELTA109
show the reaction diagram
-
-
-
-
?
ATP + c-Jun
ADP + phosphorylated c-Jun
show the reaction diagram
-
-
-
-
?
ATP + EGF receptor peptide
ADP + phosphorylated EGF receptor peptide
show the reaction diagram
-
-
-
-
?
ATP + Elk-1
ADP + phosphorylated Elk-1
show the reaction diagram
-
an ETS family transcription factor
-
-
?
ATP + Elk1
ADP + phosphorylated Elk1
show the reaction diagram
-
recombinant GST-tagged Elk1, substrate of ERK2
-
-
?
ATP + MAPKAP-K2
ADP + phosphorylated MAPKAP-K2
show the reaction diagram
-
-
-
-
?
ATP + MAPKAP-K3
ADP + phosphorylated MAPKAP-K3
show the reaction diagram
-
-
-
-
?
ATP + MEF2
ADP + phosphorylated MEF2
show the reaction diagram
-
-
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
-
substrate of ERK2
-
-
?
ATP + Net
ADP + phosphorylated Net
show the reaction diagram
-
an ETS family transcription factor
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
-
Ser/Thr kinase
-
-
-
ATP + protein ATF2
ADP + phosphorylated protein ATF2
show the reaction diagram
-
-
-
?
ATP + Smad3
ADP + phosphorylated Smad3
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + activating transcription factor 2
ADP + phosphorylated activating transcription factor 2
show the reaction diagram
-
ATF2
-
-
?
ATP + Elk-1
ADP + phosphorylated Elk-1
show the reaction diagram
-
an ETS family transcription factor
-
-
?
ATP + MAPKAP-K2
ADP + phosphorylated MAPKAP-K2
show the reaction diagram
-
-
-
-
?
ATP + MAPKAP-K3
ADP + phosphorylated MAPKAP-K3
show the reaction diagram
-
-
-
-
?
ATP + MEF2
ADP + phosphorylated MEF2
show the reaction diagram
-
-
-
-
?
ATP + Net
ADP + phosphorylated Net
show the reaction diagram
-
an ETS family transcription factor
-
-
?
ATP + Smad3
ADP + phosphorylated Smad3
show the reaction diagram
-
substrate of MAPKs, e.g. ERK2
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(E)-3-(2,4-dimethoxyphenyl)-N-(4-[3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl]pyridin-2-yl)acrylamide
-
(E)-3-(2,4-dimethoxyphenyl)-N-(4-[5-(4-fluorophenyl)-2-methanesulfinyl-3H-imidazol-4-yl]pyridin-2-yl)acrylamide
-
(E)-3-(2,4-dimethoxyphenyl)-N-(4-[5-(4-fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]pyridin-2-yl)acrylamide
-
1-(2,6-dichloro-phenyl)-5-(2,4-difluoro-phenyl)-7-piperazin-1-yl-3,4-dihydro-1H-quinazolin-2-one
highly selective for p38 isozyme alpha wild-type with IC50 of 3.2 nM, the IC50 for mutants G110A and G110D are 37 nM and 56 nM, respectively, no inhibition of JNK3, JNK2, and ERK
1-(2,6-dichloro-phenyl)-5-(2,4-difluoro-phenyl)-7-piperidin-4-yl-3,4-dihydro-1H-quinolin-2-one
highly selective for p38 isozyme alpha wild-type with IC50 of 0.74 nM, the IC50 for mutants G110A and G110D are 26 nM and 67 nM, respectively, no inhibition of JNK3, JNK2, and ERK
1-(2,6-dichloro-phenyl)-6-(2,4-difluoro-phenylsulfanyl)-7-(1,2,3,6-tetrahydro-pyridin-4-yl)-3,4-dihydro-1H-pyrido[3,2-d]pyrimidin-2-one
highly selective for p38 isozyme alpha wild-type with IC50 of 4.3 nM, the IC50 for mutants G110A and G110D are 61 nM and 160 nM, respectively, no inhibition of JNK3, JNK2, and ERK
2-(4-fluorophenyl)-3-(2-isopropylaminopyridin-4-yl)pyrido[2,3-b]pyrazine
-
-
2-(4-fluorophenyl)-3-(pyridin-4-yl)pyrido[2,3-b]pyrazine
-
-
2-(4-fluorophenyl)-3-(pyridin-4-yl)quinoxaline
-
-
2-(4-fluorophenyl)-3-pyridin-4-ylpyrido[3,4-b]pyrazine
-
-
2-(4-fluorophenyl)-6,7-dimethyl-3-pyridin-4-ylquinoxaline
-
-
2-(4-fluorophenyl)-6-methoxy-3-(pyridin-4-yl)quinoxaline
-
-
2-(4-fluorophenyl)-N-[4-(3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl)pyridin-2-yl]acetamide
-
3-(4-fluorophenyl)-2-(2-isopropylaminopyridin-4-yl)pyrido[2,3-b]pyrazine
-
-
3-(4-fluorophenyl)-2-(pyridin-4-yl)pyrido[2,3-b]pyrazine
-
-
3-(4-fluorophenyl)-2-pyridin-4-ylpyrido[3,4-b]pyrazine
-
-
3-(4-fluorophenyl)-6-methoxy-2-(pyridin-4-yl)quinoxaline
-
-
4-[3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl]-N-(1(R)-phenylethyl)pyridin-2-amine
-
4-[3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl]-N-(1(S)-phenylethyl)pyridin-2-amine
-
4-[3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl]-N-(tetrahydro-2H-pyran-4-yl)pyridin-2-amine
-
4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]-N-(1-methylethyl)pyridin-2-amine
-
-
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-(1-phenylethyl)pyridin-2-amine
-
-
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-(3-methylbutan-2-yl)pyridin-2-amine
-
-
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-isobutylpyridin-2-amine
-
-
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-isopropylpyridin-2-amine
-
-
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(1R)-1-phenylethyl]pyridin-2-amine
-
-
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(1S)-1-phenylethyl]pyridin-2-amine
-
-
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(R)-3-methylbutan-2-yl]pyridin-2-amine
-
-
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(S)-3-methylbutan-2-yl]pyridin-2-amine
-
-
4-[4-[3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-ylamine]-cyclohexanol
-
-
4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]-N-(1,2-dimethylpropyl)pyridin-2-amine
-
-
4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]-N-(1-methylethyl)pyridin-2-amine
-
-
6,7-dichloro-2-(4-fluorophenyl)-3-pyridin-4-ylquinoxaline
-
-
7-(6-N-phenylaminohexyl)amino-2H-anthra[1,9-cd]pyrazol-6-one
-
AV-7
adenylyl-beta,gamma-methylene diphosphonic acid
-
i.e. AMP-PCP, MgAMP-PCP shows a mixed inhibition pattern in the kinase reaction, and a competitive pattern in the ATPase reaction
ADP
-
MgADP- shows an uncompetitive inhibition pattern
alsterpaullone
-
36% inhibition of MAPK2/ERK2 at 0.01 mM
AMP-PCP
-
-
BIRB796
binding structure with isozyme p38alpha
II/SP600125
inhibits SAPK/JNK; inhibits SAPK/JNK; inhibits SAPK/JNK
kenpaullone
-
30% inhibition of MAPK2/ERK2 at 0.01 mM
lignocaine
-
the enzyme inhibition by lignocine may involve voltage-sensitive sodium channels, the enzyme attenuates the induction of MAPK activation by lipopolysaccharides, overview
N-(1,2-dimethylpropyl)-4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-amine
-
-
N-(4-[3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl]pyridin-2-yl)2-phenoxypropanamide
-
N-benzyl-4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-amine
-
-
N-benzyl-4-[3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-amine
-
-
N-benzyl-4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-amine
-
-
N-sec-butyl-4-[3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl]pyridin-2-amine
-
N-sec-butyl-4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-amine
-
-
N-sec-butyl-4-[3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-amine
-
-
N-tert-butyl-4-[2-(4-fluorophenyl)pyrido[3,4-b]pyrazin-3-yl]pyridin-2-amine
-
-
N-tert-butyl-4-[3-(4-fluorophenyl)pyrido[3,4-b]pyrazin-2-yl]pyridin-2-amine
-
-
N-[4-(3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl)pyridin-2-yl]acetamide
-
purvalanol
-
74% inhibition of MAPK2/ERK2 at 0.01 mM
pyridinyl imidazole-type inhibitors
IC50 of 15-48 nM
-
roscovitine
-
19% inhibition of MAPK2/ERK2 at 0.01 mM
SB202190
SB203580
siRNA
-
-
-
skepinone-L
-
the specificity by which SCD-1 modulates the phospholipid composition and inhibits p38 MAPK signaling (among survival/stress pathways), thereby preventing endoplasmic reticulum stress (but not other SCD-1-dependent responses), suggests selective protein-lipid interactions
-
SP600125
trans-4-([4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-yl]amino)cyclohexanol
-
-
trans-4-([4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-yl]amino)cyclohexanol
-
-
U0126
-
specific inhibitor of ERK
[4-[3-methyl-2-piperidin-4-yl-5-(3-trifluoromethyl-phenyl)-3H-imidazol-4-yl]-pyrimidin-2-yl]-((S)-1-phenyl-ethyl)-amine
highly selective for p38 isozyme alpha wild-type and mutants with IC50 of 0.10-0.14 nM, IC50 for JNK2 is 680 nM, for JNK3 970 nM and for ERK 660 nM
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
EGF
-
induces phosphorylation of Smad3
-
palmitate
-
activates p38 MAPK phosphorylation and activates it
Ras
-
Ras induces phosphorylation of c-Jun by JNKs
-
TNF-alpha
-
activates p38 MAPK mediated by protein kinases MKK3, MKK4, and MKK6, overview
-
UV radiation
-
activates p38 MAPK mediated by protein kinases, overview
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.002 - 0.02
ATF2DELTA109
-
0.048 - 0.096
ATP
0.656 - 2.8
EGF receptor peptide
additional information
additional information
-
steady-state kinetics, kinetic mechanism for p38 MAP kinase alpha kinase and ATPase activities, overview
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
3.8 - 4.7
ATF2DELTA109
-
6.99 - 31.6
EGF receptor peptide
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2
ADP
-
above, pH 7.6, 27°C, recombinant p38 MAPK
0.187 - 0.242
AMP-PCP
0.000021
SB203580
-
ATPase reaction versus ATP, pH 7.6, 27°C, recombinant p38 MAPK
additional information
additional information
-
inhibition kinetics
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00252
(E)-3-(2,4-dimethoxyphenyl)-N-(4-[3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl]pyridin-2-yl)acrylamide
Mus musculus;
P47811
-
0.000041
(E)-3-(2,4-dimethoxyphenyl)-N-(4-[5-(4-fluorophenyl)-2-methanesulfinyl-3H-imidazol-4-yl]pyridin-2-yl)acrylamide
Mus musculus;
P47811
-
0.000019
(E)-3-(2,4-dimethoxyphenyl)-N-(4-[5-(4-fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]pyridin-2-yl)acrylamide
Mus musculus;
P47811
-
0.0000043 - 0.00016
1-(2,6-dichloro-phenyl)-6-(2,4-difluoro-phenylsulfanyl)-7-(1,2,3,6-tetrahydro-pyridin-4-yl)-3,4-dihydro-1H-pyrido[3,2-d]pyrimidin-2-one
0.000333
2-(4-fluorophenyl)-3-(2-isopropylaminopyridin-4-yl)pyrido[2,3-b]pyrazine
Mus musculus;
-
-
0.00315
2-(4-fluorophenyl)-3-(pyridin-4-yl)quinoxaline
Mus musculus;
-
-
0.0037
2-(4-fluorophenyl)-6,7-dimethyl-3-pyridin-4-ylquinoxaline
Mus musculus;
-
-
0.00156
2-(4-fluorophenyl)-N-[4-(3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl)pyridin-2-yl]acetamide
Mus musculus;
P47811
-
0.000038
3-(4-fluorophenyl)-2-(2-isopropylaminopyridin-4-yl)pyrido[2,3-b]pyrazine
Mus musculus;
-
-
0.00319
3-(4-fluorophenyl)-2-(pyridin-4-yl)pyrido[2,3-b]pyrazine
Mus musculus;
-
-
0.00614
3-(4-fluorophenyl)-6-methoxy-2-(pyridin-4-yl)quinoxaline
Mus musculus;
-
-
0.00045
4-[3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl]-N-(1(R)-phenylethyl)pyridin-2-amine
Mus musculus;
P47811
-
0.000006
4-[3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl]-N-(1(S)-phenylethyl)pyridin-2-amine
Mus musculus;
P47811
-
0.00006
4-[3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl]-N-(tetrahydro-2H-pyran-4-yl)pyridin-2-amine
Mus musculus;
P47811
-
0.000238
4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]-N-(1-methylethyl)pyridin-2-amine
Mus musculus;
-
-
0.00072
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-(1-phenylethyl)pyridin-2-amine
Mus musculus;
-
-
0.000794
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-(3-methylbutan-2-yl)pyridin-2-amine
Mus musculus;
-
-
0.000642
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-isobutylpyridin-2-amine
Mus musculus;
-
-
0.000081
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-isopropylpyridin-2-amine
Mus musculus;
-
-
0.00479
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(1R)-1-phenylethyl]pyridin-2-amine
Mus musculus;
-
-
0.000431
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(1S)-1-phenylethyl]pyridin-2-amine
Mus musculus;
-
-
0.00159
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(R)-3-methylbutan-2-yl]pyridin-2-amine
Mus musculus;
-
-
0.00576
4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(S)-3-methylbutan-2-yl]pyridin-2-amine
Mus musculus;
-
-
0.000211
4-[4-[3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-ylamine]-cyclohexanol
Mus musculus;
-
-
0.00946
4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]-N-(1,2-dimethylpropyl)pyridin-2-amine
Mus musculus;
-
-
0.000412
4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]-N-(1-methylethyl)pyridin-2-amine
Mus musculus;
-
-
0.00004 - 0.00009
II/SP600125
0.00138
N-(1,2-dimethylpropyl)-4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-amine
Mus musculus;
-
-
0.00089
N-(4-[3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl]pyridin-2-yl)2-phenoxypropanamide
Mus musculus;
P47811
-
0.00153
N-benzyl-4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-amine
Mus musculus;
-
-
0.00003
N-sec-butyl-4-[3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl]pyridin-2-amine
Mus musculus;
P47811
-
0.000595
N-sec-butyl-4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-amine
Mus musculus;
-
-
0.000114
N-sec-butyl-4-[3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-amine
Mus musculus;
-
-
0.000522
N-tert-butyl-4-[2-(4-fluorophenyl)pyrido[3,4-b]pyrazin-3-yl]pyridin-2-amine
Mus musculus;
-
mixture of N-tert-butyl-4-[3-(4-fluorophenyl)pyrido[3,4-b]pyrazin-2-yl]pyridin-2-amine and N-tert-butyl-4-[2-(4-fluorophenyl)pyrido[3,4-b]pyrazin-3-yl]pyridin-2-amine
0.000522
N-tert-butyl-4-[3-(4-fluorophenyl)pyrido[3,4-b]pyrazin-2-yl]pyridin-2-amine
Mus musculus;
-
mixture of N-tert-butyl-4-[3-(4-fluorophenyl)pyrido[3,4-b]pyrazin-2-yl]pyridin-2-amine and N-tert-butyl-4-[2-(4-fluorophenyl)pyrido[3,4-b]pyrazin-3-yl]pyridin-2-amine
0.0003
N-[4-(3-(4-fluorophenyl)-5-isopropylisoxazol-4-yl)pyridin-2-yl]acetamide
Mus musculus;
P47811
-
0.000015 - 0.000048
pyridinyl imidazole-type inhibitors
Mus musculus;
P47811
IC50 of 15-48 nM
-
0.000025 - 0.00005
skepinone-L
Mus musculus;
-
pH 7.4, 22°C
-
0.000259
trans-4-([4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-yl]amino)cyclohexanol
Mus musculus;
-
-
0.000608
trans-4-([4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-yl]amino)cyclohexanol
Mus musculus;
-
-
0.0000001 - 0.00097
[4-[3-methyl-2-piperidin-4-yl-5-(3-trifluoromethyl-phenyl)-3H-imidazol-4-yl]-pyrimidin-2-yl]-((S)-1-phenyl-ethyl)-amine
additional information
2-(4-fluorophenyl)-3-(pyridin-4-yl)pyrido[2,3-b]pyrazine
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.4
-
assay at
7.5
-
assay at
7.6
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
21
-
assay at room temperature
22
-
assay at room temperature
27
-
assay at
additional information
-
using a relatively low induction temperature (21°C in comparison to 32°C) phosphorylation is almost completely prevented. Combining a short 5 h induction with a low expression temperature (21°C) results in highly homogeneous unphosphorylated protein
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
activated ERK2
Manually annotated by BRENDA team
splenic; splenic; splenic; splenic
Manually annotated by BRENDA team
-
p38 MAPK is expressed predominantly in nestin-positive cells in the cerebral cortex in embryonic day 10 brain
Manually annotated by BRENDA team
-
mixed glial cultures
Manually annotated by BRENDA team
-
the MAPK family enzymes have regulatory function in the myocardium
Manually annotated by BRENDA team
adrenocortical cell line; adrenocortical cell line; adrenocortical cell line, predominant expression of isozyme p38 MAPKalpha
Manually annotated by BRENDA team
additional information
-
CD4+ T cell
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
PDB
SCOP
CATH
UNIPROT
ORGANISM
Mus musculus;
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
64000
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x * 64000, recombinant p38alpha MAP kinase, SDS-PAGE
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
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x * 64000, recombinant p38alpha MAP kinase, SDS-PAGE
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
p38alpha active mutants crystallized by sitting-drop vapour-diffusion method, mutant D176A/F327L to 1.45 A resolution, crystals of the three p38alpha mutants belong to the orthorhombic space group P212121, with one molecule in the asymmetric unit
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purified p38 isozyme alpha bound to several inhibitors pyridinyl imidazole-type inhibitors, X-ray diffraction structure determination and analysis at 2.1-2.5 A resolution
purified recombinant p38alpha MAP kinase free or in complex with inhibitor SB203580, sitting or hanging drop vapour diffusion method at 16-20°C, 16 mg/ml protein in 25 mM Tris-HCl, pH 7.5, 100 mM NaCl, 10 mM MgCl2, 10 mM DTT, and 5% glycerol is mixed with reservoir solution containing 10-20% PEG 4000, 18% ethylene glycol, 0.1 M cacodylic acid, pH 6.0, at a volume ratio of 3:2, X-ray diffraction structure determination and analysis at 1.9-2.7 A resolution
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STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-80°C, 100 mM NaCl, 50 mM Tris-HCl buffer, pH 7.4, 10 mM DTT, 10 mM MgCl2, 5% glycerol
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Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
p38alpha active mutants, by gel filtration, on Ni2+-column
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recombinant GST-tagged p38 isozyme alpha from Escherichia coli strain BL21(DE3) by two steps of ion exchange chromatography to homogeneity, the recombinant enzyme is detagged
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recombinant His-tagged p38alpha from Escherichia coli strain BL21(DE3) by nickel affinity and anion exchange chromatography to homogeneity
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recombinant His-tagged p38alpha MAP kinase from Escherichia coli strain BL21(DE3) by nickel chelate affinity chromatohgraphy, dialysis, and ion exchange chromatography to homogeneity, the His-tag is cleaved off by thrombin
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Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expression in COS-7 cells; expression in COS-7 cells
expression of GST-tagged p38 isozyme alpha in Escherichia coli strain BL21(DE3)
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expression of His-tagged p38alpha in Escherichia coli strain BL21(DE3)
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expression of His-tagged wild-type and mutant p38 isozyme alpha
p38alpha active mutants subcloned into vector pET-28a and expressed in Rosetta strain of Escherichia coli
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p38alpha MAP kinase expression in Escherichia coli strain BL21(DE3) as His-tagged protein with a thrombin cleavage site
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quantitative RT-PCR enzyme expression analysis
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recombinant expression of GST-tagged enzyme
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ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
D176A
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active p38alpha mutant, crystals do not appear spontaneously, cross-seeding approaches using crystals of mutant D176A+F327L as the source of microseeds results in crystals suitable for X-ray analysis
D176A/F327L
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most active p38alpha mutant, improvement of crystallization assays, obtained with abolishing phosporylation completely by reducing both the temperature and duration of induction and by significantly shortening the N-terminal hexahistidine spacer, facilitating the growth of well diffracting crystals
D176A/F327S
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active p38alpha mutant, crystals do not appear spontaneously, cross-seeding approaches using crystals of mutant D176A+F327L as the source of microseeds results in crystals suitable for X-ray analysis
G110A
site-directed mutagenesis of isozyme alpha, the mutant shows a slightly decreased Km value for ATP, but unaltered activity compared to the wild-type enzyme, decreased sensitivity for inhibitors compared to the wild-type enzyme
G110D
site-directed mutagenesis of isozyme alpha, the mutant shows a decreased Km value for ATP, but unaltered activity compared to the wild-type enzyme, decreased sensitivity for inhibitors compared to the wild-type enzyme
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
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MAPKs are targets for drug development
medicine
pharmacology
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MAPKs are targets for inhibitors and pharmacological drug development