Information on EC 2.7.12.1 - dual-specificity kinase

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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea

EC NUMBER
COMMENTARY hide
2.7.12.1
-
RECOMMENDED NAME
GeneOntology No.
dual-specificity kinase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + a protein = ADP + a phosphoprotein
show the reaction diagram
-
-
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
-
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SYSTEMATIC NAME
IUBMB Comments
ATP:protein phosphotransferase (Ser/Thr- and Tyr-phosphorylating)
This family of enzymes can phosphorylate both Ser/Thr and Tyr residues.
CAS REGISTRY NUMBER
COMMENTARY hide
134549-83-0
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
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-
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Manually annotated by BRENDA team
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SwissProt
Manually annotated by BRENDA team
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-
-
Manually annotated by BRENDA team
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-
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Manually annotated by BRENDA team
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-
-
Manually annotated by BRENDA team
Methanothermobacter thermautotrophicum
-
-
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Manually annotated by BRENDA team
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-
-
Manually annotated by BRENDA team
strain CDC1551 and H37Rv
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-
Manually annotated by BRENDA team
strain CDC1551 and H37Rv
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-
Manually annotated by BRENDA team
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-
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Manually annotated by BRENDA team
strain PCC 7120
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-
Manually annotated by BRENDA team
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-
-
Manually annotated by BRENDA team
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-
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Manually annotated by BRENDA team
strain ATCC 27405
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-
Manually annotated by BRENDA team
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-
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Manually annotated by BRENDA team
Thermospora curvatum
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-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
physiological function
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 + amphiphysin I
ADP + phosphorylated amphiphysin I
show the reaction diagram
-
-
-
-
?
ATP + casein
ADP + phosphorylated casein
show the reaction diagram
-
-
-
-
?
ATP + caspase-9
ADP + phosphorylated caspase-9
show the reaction diagram
-
-
-
-
?
ATP + CREB
ADP + phosphorylated CREB
show the reaction diagram
-
-
-
-
?
ATP + cyclin L2
ADP + phosphorylated cyclin L2
show the reaction diagram
-
-
-
-
?
ATP + dynamin 1
ADP + phosphorylated dynamin 1
show the reaction diagram
-
-
-
-
?
ATP + dynamin I
ADP + phosphorylated dynamin I
show the reaction diagram
-
-
-
-
?
ATP + eIF2Bepsilon
ADP + phosphorylated eIF2Bepsilon
show the reaction diagram
-
-
-
-
?
ATP + FKHR
ADP + phosphorylated FKHR
show the reaction diagram
-
-
-
-
?
ATP + Gli1 protein
ADP + phosphorylated Gli1 protein
show the reaction diagram
-
-
-
-
?
ATP + glycogen synthase
ADP + phosphorylated glycogen synthase
show the reaction diagram
-
-
-
-
?
ATP + histone
ADP + phosphorylated histone
show the reaction diagram
-
recombinant glutathione S-transferase-Dyrk/fusion protein catalyzes histone phosphorylation on tyrosine and Ser/Thr residues
-
-
?
ATP + histone H1
ADP + phosphorylated histone H1
show the reaction diagram
-
-
-
-
?
ATP + insulin receptor kinase substrate 1
ADP + phosphorylated insulin receptor kinase substrate 1
show the reaction diagram
ATP + microtubule associated protein 1B
ADP + phosphorylated microtubule associated protein 1B
show the reaction diagram
-
DYRK1A phosphorylates the S1392 site on microtubule associated protein 1B
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
ATP + neurodegeneration-related septin 4
ADP + phosphorylated neurodegeneration-related septin 4
show the reaction diagram
-
SEPT4, also known as Pnutl2/CDCrel-2
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-
?
ATP + NFAT
ADP + phosphorylated NFAT
show the reaction diagram
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-
-
-
?
ATP + Notch protein
ADP + phosphorylated Notch protein
show the reaction diagram
-
-
-
-
?
ATP + peptide DYRKtide
ADP + phosphorylated peptide DYRKtide
show the reaction diagram
ATP + poly-(Tyr-Glu)
ADP + phospho-poly-(Tyr-Glu)
show the reaction diagram
-
tyrosine kinase substrate
-
-
?
ATP + Pop2p
ADP + phosphorylated Pop2p
show the reaction diagram
-
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
autophosphorylated on Ser and Thr residues
-
-
?
ATP + Ser/Arg-rich splicing factors
ADP + phosphorylated Ser/Arg-rich splicing factor
show the reaction diagram
-
-
-
?
ATP + SF3B1 protein-L-Thr434
ADP + [SF3B1 protein]-L-Thr434 phosphate
show the reaction diagram
-
-
-
-
?
ATP + splicing factor 2
ADP + phosphorylated splicing factor 2
show the reaction diagram
-
-
-
-
?
ATP + splicing factor 3
ADP + phosphorylated splicing factor 3
show the reaction diagram
-
-
-
-
?
ATP + splicing factor 3B1
ADP + phosphorylated splicing factor 3B1
show the reaction diagram
-
splicing factor 3B1 is poshorylated at Thr434
-
-
?
ATP + SR protein
ADP + ?
show the reaction diagram
ATP + SR protein
ADP + hyperphosphorylated SR protein
show the reaction diagram
i.e. serine-rich and arginine-rich proteins
-
?
ATP + STAT3
ADP + phosphorylated STAT3
show the reaction diagram
-
-
-
-
?
ATP + synaptojanin I
ADP + phosphorylated synaptojanin I
show the reaction diagram
-
-
-
-
?
ATP + tau protein-L-Thr434
ADP + [tau protein]-L-Thr434 phosphate
show the reaction diagram
-
-
-
-
?
biliverdin + ?
bilirubin + ?
show the reaction diagram
-
-
-
-
?
additional information
?
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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 + amphiphysin I
ADP + phosphorylated amphiphysin I
show the reaction diagram
-
-
-
-
?
ATP + caspase-9
ADP + phosphorylated caspase-9
show the reaction diagram
-
-
-
-
?
ATP + CREB
ADP + phosphorylated CREB
show the reaction diagram
-
-
-
-
?
ATP + cyclin L2
ADP + phosphorylated cyclin L2
show the reaction diagram
-
-
-
-
?
ATP + dynamin 1
ADP + phosphorylated dynamin 1
show the reaction diagram
-
-
-
-
?
ATP + dynamin I
ADP + phosphorylated dynamin I
show the reaction diagram
-
-
-
-
?
ATP + eIF2Bepsilon
ADP + phosphorylated eIF2Bepsilon
show the reaction diagram
-
-
-
-
?
ATP + FKHR
ADP + phosphorylated FKHR
show the reaction diagram
-
-
-
-
?
ATP + Gli1 protein
ADP + phosphorylated Gli1 protein
show the reaction diagram
-
-
-
-
?
ATP + glycogen synthase
ADP + phosphorylated glycogen synthase
show the reaction diagram
-
-
-
-
?
ATP + insulin receptor kinase substrate 1
ADP + phosphorylated insulin receptor kinase substrate 1
show the reaction diagram
-
phosphorylation at serine residues, overview, the enzyme is involved in the insulin signaling pathway
-
-
?
ATP + microtubule associated protein 1B
ADP + phosphorylated microtubule associated protein 1B
show the reaction diagram
-
DYRK1A phosphorylates the S1392 site on microtubule associated protein 1B
-
-
?
ATP + neurodegeneration-related septin 4
ADP + phosphorylated neurodegeneration-related septin 4
show the reaction diagram
-
SEPT4, also known as Pnutl2/CDCrel-2
-
-
?
ATP + NFAT
ADP + phosphorylated NFAT
show the reaction diagram
-
-
-
-
?
ATP + Notch protein
ADP + phosphorylated Notch protein
show the reaction diagram
-
-
-
-
?
ATP + SF3B1 protein-L-Thr434
ADP + [SF3B1 protein]-L-Thr434 phosphate
show the reaction diagram
-
-
-
-
?
ATP + splicing factor 2
ADP + phosphorylated splicing factor 2
show the reaction diagram
-
-
-
-
?
ATP + splicing factor 3
ADP + phosphorylated splicing factor 3
show the reaction diagram
-
-
-
-
?
ATP + splicing factor 3B1
ADP + phosphorylated splicing factor 3B1
show the reaction diagram
-
splicing factor 3B1 is poshorylated at Thr434
-
-
?
ATP + SR protein
ADP + ?
show the reaction diagram
ATP + STAT3
ADP + phosphorylated STAT3
show the reaction diagram
-
-
-
-
?
ATP + synaptojanin I
ADP + phosphorylated synaptojanin I
show the reaction diagram
-
-
-
-
?
ATP + tau protein-L-Thr434
ADP + [tau protein]-L-Thr434 phosphate
show the reaction diagram
-
-
-
-
?
biliverdin + ?
bilirubin + ?
show the reaction diagram
-
-
-
-
?
additional information
?
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COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione
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82.6% inhibition at 0.01 mM
(4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-nitrobenzylidene)pyrazolidine-3,5-dione
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76% inhibition at 0.01 mM
(4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxybenzylidene)pyrazolidine-3,5-dione
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73% inhibition at 0.01 mM
(4Z)-1-(4-fluorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione
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44% inhibition at 0.01 mM
(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
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55% inhibition at 0.01 mM
4-[(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-3,5-dioxopyrazolidin-1-yl]benzonitrile
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78% inhibition at 0.01 mM
genistein
harmine
HCD160
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82.6% inhibition at 0.01 mM
N6-Dimethylaminopurine
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unspecific inhibitor of protein kinases
roscovitine
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63% inhibition at 0.01 mM
staurosporine
tyrphostin
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competitive versus ATP, mixed inhibition versus histone H1
Zn2+
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inhibits the autophosphoylation, which cannot be reversed by Mn2+ addition
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
abscisic acid
induces the expression of isozymes DPK1-DPK3 in seedlings; induces the expression of isozymes DPK1-DPK3 in seedlings; induces the expression of isozymes DPK1-DPK3 in seedlings
H2O2
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the kinase activity of biliverdin reductase is stimulated by generators of free radicals such as H2O2
Sodium arsenite
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the kinase activity of biliverdin reductase is stimulated by generators of free radicals such as sodium arsenite
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.019 - 0.107
ATP
0.006 - 0.012
histone H1
additional information
additional information
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kinetics
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TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.26 - 14.5
ATP
3.09 - 18.4
histone H1
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000017 - 0.000426
genistein
0.000056 - 0.000694
staurosporine
0.000014 - 0.000202
tyrphostin
additional information
additional information
-
inhibition kinetics of tyrosine kinase inhibitors, recombinant His-tagged wild-type and mutant enzymes
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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0025
(4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione
Homo sapiens
-
for autophosphorylation
0.0006
(4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-nitrobenzylidene)pyrazolidine-3,5-dione
Homo sapiens
-
for autophosphorylation
0.0025
(4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxybenzylidene)pyrazolidine-3,5-dione
0.0012
(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
Homo sapiens
-
for autophosphorylation
0.0006
4-[(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-3,5-dioxopyrazolidin-1-yl]benzonitrile
Homo sapiens
-
for autophosphorylation
0.000033 - 0.001
harmine
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7
-
assay at
7.5
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assay at
8.4
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assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
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transfection analysis
Manually annotated by BRENDA team
DYRK3 expression in, ex vivo analysis of erythroid progenitor cells of DYRK3-knockout mice
Manually annotated by BRENDA team
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transfection analysis
Manually annotated by BRENDA team
co-expression experiments in
Manually annotated by BRENDA team
high expression of DPK1 in immature spikes; low expression of DPK4
Manually annotated by BRENDA team
low expression of DPK2; low expression of DPK4
Manually annotated by BRENDA team
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transfection analysis, degradation of the tumor suppressor pRb in a dose-dependent manner based on the accumulation of HPV16E7 generated by DYRK1A transfection
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
additional information
PDB
SCOP
CATH
ORGANISM
UNIPROT
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
55000
-
recombinant His-tagged wild-type enzyme, gel filtration
90000
-
SDS-PAGE
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
x * 65000, splicing variant 1, SDS-PAGE, x * 70000, splicing variant 2, SDS-PAGE, x * 75000, splicing variant 3 from skeletal muscle, SDS-PAGE
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
phosphoprotein
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.5 - 7.4
-
the kinase is resistant to high salt and Triton X-100 extraction at pH 6.5. At pH 7.4, the kinase becomes soluble to some extent after treatment with Triton X-100 and 1.0 M NaCl
702352
ORGANIC SOLVENT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Triton X-100
-
the kinase is resistant to high salt and Triton X-100 extraction at pH 6.5. At pH 7.4, the kinase becomes soluble to some extent after treatment with Triton X-100 and 1.0 M NaCl
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
gel filtration
-
gel filtration, SDS-PAGE
-
glutathione-Sepharose column chromatography
-
hydroxylapatite column chromatography
-
recombinant GST-fusion protein from Escherichia coli strain DH5alpha by glutathione affinity chromatography
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recombinant His-tagged wild-type and mutant enzymes from Escherichia coli strain BL21(DE3) by nickel affinity chromatography
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
DNA and amino acid sequence determination and analysis, the enzyme occurs in several splicing variants, analysis overview, expression in murine hypothalamic GT1-7 cell line, expression of splicing variants in COS_7 cells and in Escherichia coli
DNA and amino acid sequence determination and analysis, the enzyme occurs in several splicing variants, expression in human fibroblast 3T3-L1 cell line
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EGFP-tagged DYRK1A is expressed in HEK-293 cell
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expressed in Escherichia coli BL21(DE3) cells; the catalytic domain of DYRK1A is expressed in Escherichia coli BL21(DE3) cells
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expressed in Escherichia coli BL21(DE3) codon plus RIL, plasmid pcDNA3.1
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expressed in Mus musculus
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expression in Escherichia coli strain DH5alpha as GST-fusion protein, expression in 293A cells
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expression of His-tagged wild-type and mutant enzymes in Escherichia coli strain BL21(DE3)
-
fusion protein of DYRK1A accumulates in the nucleus of transfected COS-7 and HEK293 cells, expression in Escherichia coli
-
genomic clones of DYRK3 isolated from a 129svJ Lambda phage library, transgenic mice generated, DYRK3 gene deletion in E14 ES cells using a floxed PGKneo targeting vector, targeted cells injected into C57BL/6J blastocysts, transgenic pA2gata1-DYRK3 mice prepared using an Myc epitope-tagged mDYRK3 cDNA within a pA2gata1 vector
green fluorescent protein fusion protein of DYRK1B is found mainly in the nucleus of transfected COS-7 cells
isozyme DPK1, DNA and amino acid sequence determination and analysis, gene mapping, expression analysis under stress conditions; isozyme DPK2, DNA and amino acid sequence determination and analysis, gene mapping, expression analysis under stress conditions; isozyme DPK3, DNA and amino acid sequence determination and analysis, gene mapping, expression analysis under stress conditions; isozyme DPK4, DNA and amino acid sequence determination and analysis, gene mapping, expression analysis under stress conditions
overexpression of His-tagged wild-type and mutant enzymes in Escherichia coli strain BL21(DE3)
-
phylogenetic tree of kinases derived from the kinase core sequence, overview, overexpression as GST-fusion protein under control of the galactose-inducible GAL1 promotor in Escherichia coli, determination of 5'-end sequences
-
recombinant Dyrk1A-protein expressed in mammalian expression vector pcDNA3, wild-type and mutant
sequence analysis for enzyme domain determination
single-copy gene, DNA and amino acid sequence determination and analysis, comparison of subdomain sequences with those of Arabidopsis thaliana
transfected into NIH-3T3 cells; wild-type and mutant DNA fragments of DYRK1A, vectors pCMV-Tag2B, pRK5, pCITE4, pGEX-5X-1, pCDNA3-HA
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
Dyrk1A expression can be enhanced by treatment with beta-amyloid or overexpression of the transcription factor E2F1, Dyrk1A activity can be increased by binding of 14-3-3 protein
-
Dyrk1A expression can be reressed by the AP4- geminin complex
-
there are higher levels of full-length DYRK1A in the brains of patients with Down syndrome when compared to control brains
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
K160R
-
site-directed mutagenesis, inactive mutant enzyme
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
analysis
-
development of a protein chip consisting of a silicone elastomer microwell array with recombinant enzyme covalently attached to the wells via a 3-glycidoxypropyltrimethoxysilane crosslinker for large scale activity assay, overview
medicine
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