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Information on EC 2.7.11.24 - mitogen-activated protein kinase

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EC Tree
IUBMB Comments
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 . 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.
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UNIPROT: P53779
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Word Map
The enzyme appears in viruses and cellular organisms
Reaction Schemes
+
a [protein]-(L-serine/L-threonine)
=
+
a [protein]-(L-serine/L-threonine) phosphate
Synonyms
mapk, p38, erk1/2, p38 mapk, mitogen-activated protein kinase, map kinase, extracellular signal-regulated kinase, p38 mitogen-activated protein kinase, p38mapk, p38 map kinase, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
c-Jun N-terminal kinase 3
-
mitogen-activated protein kinase 10
-
p493F12 kinase
-
cp38a
-
-
-
-
cp38b
-
-
-
-
CSAID binding protein
-
-
-
-
CSBP
-
-
-
-
Cytokine suppressive anti-inflammatory drug binding protein
-
-
-
-
ERK5
-
-
-
-
MAP kinase MXI2
-
-
-
-
MAP kinase p38 beta
-
-
-
-
MAP kinase p38 delta
-
-
-
-
MAP kinase p38 gamma
-
-
-
-
MAP kinase p38a
-
-
-
-
MAP kinase p38alpha
-
-
-
-
MAP kinase p38b
-
-
-
-
MAPK
-
-
-
-
mitogen-activated protein kinase
-
-
-
-
Mitogen-activated protein kinase p38 beta
-
-
-
-
Mitogen-activated protein kinase p38 delta
-
-
-
-
Mitogen-activated protein kinase p38 gamma
-
-
-
-
Mitogen-activated protein kinase p38a
-
-
-
-
Mitogen-activated protein kinase p38alpha
-
-
-
-
Mitogen-activated protein kinase p38b
-
-
-
-
p38b
-
-
-
-
SAPK2A
-
-
-
-
stress-activated protein kinase 2a
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
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
-
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 + ATF-2
ADP + phosphorylated ATF-2
show the reaction diagram
assay substrate biotinylated ATF-2
-
-
?
ATP + Bcl-2
ADP + phosphorylated Bcl-2
show the reaction diagram
-
-
-
?
ATP + c-Jun
ADP + phosphorylated c-Jun
show the reaction diagram
-
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
autophosphorylates both Thr and Tyr residues
-
-
?
ATP + protein APP
ADP + phosphorylated protein APP
show the reaction diagram
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL 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
-
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-5-carboxamide
-
3-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]benzamide
-
4-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-2-carboxamide
-
5-(acetylamino)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
5-(difluoromethyl)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
5-benzyl-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
5-bromo-N-(3-chloro-2-piperazin-1-ylphenyl)furan-2-carboxamide
-
5-bromo-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
5-bromo-N-[2-(4-prop-2-en-1-ylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]furan-2-carboxamide
-
5-bromo-N-[2-(4-prop-2-en-1-ylpiperazin-1-yl)biphenyl-3-yl]furan-2-carboxamide
-
5-bromo-N-[3-(phenylamino)-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-bromo-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-cyclopropylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-ethylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-methylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-propylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-pyridin-2-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-[4-(1-methylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-[4-(2-methylprop-2-en-1-yl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-[4-(2-phenylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-[4-(furan-2-ylmethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-[4-(trifluoroacetyl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
5-bromo-N-[3-fluoro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-methyl-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-chloro-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
5-cyano-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
6-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]pyridine-2-carboxamide
-
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-(phenylamino)furan-2-carboxamide
-
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-ethylfuran-2-carboxamide
-
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-fluorofuran-2-carboxamide
-
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methoxyfuran-2-carboxamide
-
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methylfuran-2-carboxamide
-
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-prop-1-yn-1-ylfuran-2-carboxamide
-
N-[2-(4-acetylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
-
N-[2-(4-benzylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
-
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-4-carboxamide
-
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1H-pyrrole-2-carboxamide
-
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-2-methyl-1,3-thiazole-4-carboxamide
-
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-5-cyanopyridine-2-carboxamide
-
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-6-methylpyridine-2-carboxamide
-
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]isoxazole-5-carboxamide
-
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]pyrimidine-2-carboxamide
-
tert-butyl 4-(2-[[(5-bromofuran-2-yl)carbonyl]amino]-6-chlorophenyl)piperazine-1-carboxylate
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
additional information
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00031
2-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-5-carboxamide
Homo sapiens
-
0.0064
3-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]benzamide
Homo sapiens
-
0.0018
4-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-2-carboxamide
Homo sapiens
-
0.011
5-(acetylamino)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
Homo sapiens
-
0.00035
5-(difluoromethyl)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
Homo sapiens
-
0.0048
5-benzyl-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
Homo sapiens
-
0.0099
5-bromo-N-(3-chloro-2-piperazin-1-ylphenyl)furan-2-carboxamide
Homo sapiens
-
0.00006
5-bromo-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
Homo sapiens
-
0.02
5-bromo-N-[2-(4-prop-2-en-1-ylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]furan-2-carboxamide
Homo sapiens
larger than 0.020
0.02
5-bromo-N-[2-(4-prop-2-en-1-ylpiperazin-1-yl)biphenyl-3-yl]furan-2-carboxamide
Homo sapiens
larger than 0.020
0.02
5-bromo-N-[3-(phenylamino)-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
Homo sapiens
larger than 0.020
0.02
5-bromo-N-[3-bromo-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
Homo sapiens
larger than 0.020
0.00096
5-bromo-N-[3-chloro-2-(4-cyclopropylpiperazin-1-yl)phenyl]furan-2-carboxamide
Homo sapiens
-
0.0011
5-bromo-N-[3-chloro-2-(4-ethylpiperazin-1-yl)phenyl]furan-2-carboxamide
Homo sapiens
-
0.0012
5-bromo-N-[3-chloro-2-(4-methylpiperazin-1-yl)phenyl]furan-2-carboxamide
Homo sapiens
-
0.00033
5-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
Homo sapiens
-
0.00016
5-bromo-N-[3-chloro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
Homo sapiens
-
0.0009
5-bromo-N-[3-chloro-2-(4-propylpiperazin-1-yl)phenyl]furan-2-carboxamide
Homo sapiens
-
0.001
5-bromo-N-[3-chloro-2-(4-pyridin-2-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
Homo sapiens
-
0.0022
5-bromo-N-[3-chloro-2-[4-(1-methylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
Homo sapiens
-
0.00054
5-bromo-N-[3-chloro-2-[4-(2-methylprop-2-en-1-yl)piperazin-1-yl]phenyl]furan-2-carboxamide
Homo sapiens
-
0.0014
5-bromo-N-[3-chloro-2-[4-(2-phenylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
Homo sapiens
-
0.00025
5-bromo-N-[3-chloro-2-[4-(furan-2-ylmethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
Homo sapiens
-
0.02
5-bromo-N-[3-chloro-2-[4-(trifluoroacetyl)piperazin-1-yl]phenyl]furan-2-carboxamide
Homo sapiens
larger than 0.020
0.00029
5-bromo-N-[3-fluoro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
Homo sapiens
-
0.0002
5-bromo-N-[3-methyl-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
Homo sapiens
-
0.00008
5-chloro-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
Homo sapiens
-
0.00021
5-cyano-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
Homo sapiens
-
0.002
6-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]pyridine-2-carboxamide
Homo sapiens
-
0.02
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-(phenylamino)furan-2-carboxamide
Homo sapiens
larger than 0.020
0.001
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-ethylfuran-2-carboxamide
Homo sapiens
-
0.00041
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-fluorofuran-2-carboxamide
Homo sapiens
-
0.00062
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methoxyfuran-2-carboxamide
Homo sapiens
-
0.00053
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methylfuran-2-carboxamide
Homo sapiens
-
0.00011
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-prop-1-yn-1-ylfuran-2-carboxamide
Homo sapiens
-
0.00081
N-[2-(4-acetylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
Homo sapiens
-
0.0011
N-[2-(4-benzylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
Homo sapiens
-
0.0023
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-4-carboxamide
Homo sapiens
-
0.0089
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1H-pyrrole-2-carboxamide
Homo sapiens
-
0.0058
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-2-methyl-1,3-thiazole-4-carboxamide
Homo sapiens
-
0.02
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-5-cyanopyridine-2-carboxamide
Homo sapiens
larger than 0.020
0.002
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-6-methylpyridine-2-carboxamide
Homo sapiens
-
0.005
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]isoxazole-5-carboxamide
Homo sapiens
-
0.02
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]pyrimidine-2-carboxamide
Homo sapiens
larger than 0.020
0.02
tert-butyl 4-(2-[[(5-bromofuran-2-yl)carbonyl]amino]-6-chlorophenyl)piperazine-1-carboxylate
Homo sapiens
larger than 0.020
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
JNK3 has been shown to mediate neuronal apoptosis
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
MK10_HUMAN
464
0
52585
Swiss-Prot
other Location (Reliability: 2)
PDB
SCOP
CATH
UNIPROT
ORGANISM
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
JNK3 may be a promising target for the treatment of neurodegenerative diseases such as Parkinsons disease, Alzheimers disease and other CNS disorders
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Gupta, S.; Barrett, T.; Whitmarsh, A.J.; Cavanagh, J.; Sluss, H.K.; Derijard, B.; Davis, R.J.
Selective interaction of JNK protein kinase isoforms with transcription factors
EMBO J.
15
2760-2770
1996
Homo sapiens (P45983), Homo sapiens (P45984), Homo sapiens (P53779), Homo sapiens
Manually annotated by BRENDA team
Mohit, A.A.; Martin, J.H.; Miller, C.A.
P493F12 kinase: a novel MAP kinase expressed in a subset of neurons in the human nervous system
Neuron
14
67-78
1995
Homo sapiens (P53779), Homo sapiens
Manually annotated by BRENDA team
Shin, Y.; Chen, W.; Habel, J.; Duckett, D.; Ling, Y.Y.; Koenig, M.; He, Y.; Vojkovsky, T.; LoGrasso, P.; Kamenecka, T.M.
Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors
Bioorg. Med. Chem. Lett.
19
3344-3347
2009
Homo sapiens, Homo sapiens (P53779)
Manually annotated by BRENDA team