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Information on EC 2.7.12.1 - dual-specificity kinase and Organism(s) Homo sapiens and UniProt Accession Q9Y463

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EC Tree
IUBMB Comments
This family of enzymes can phosphorylate both Ser/Thr and Tyr residues.
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Select one or more organisms in this record: ?
This record set is specific for:
Homo sapiens
UNIPROT: Q9Y463
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea
Reaction Schemes
+
a [protein]-(L-serine/L-threonine)
=
+
a [protein]-(L-serine/L-threonine) phosphate
Synonyms
dyrk1a, dyrk2, dyrk1b, dyrk3, dual-specificity kinase, dyrk1, dual specificity kinase, dual-specificity tyrosine phosphorylation-regulated kinase 1a, dual-specificity protein kinase, dyrk1a kinase, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dual specificity tyrosine phosphorylation-regulated kinase
-
dual-specificity tyrosine phosphorylation-regulated kinase 1B
-
dual-specificity tyrosine-phosphorylation regulated kinase 1B
-
Dyrk kinase
-
biliverdin reductase
cdc2/CDC28-like protein kinase
-
Clik1
-
-
-
-
dual specificity kinase
dual specificity protein kinase TTK
-
dual specificity tyrosine phosphorylated and regulated kinase 1B
-
-
dual specificity tyrosine phosphorylation regulated kinase 1A
-
-
dual specificity tyrosine phosphorylation regulated kinase 2
-
dual specificity tyrosine phosphorylation-regulated kinase
-
dual specificity tyrosine phosphorylation-regulated kinase 3
-
dual specificity tyrosine phosphorylation-regulated kinase 4
-
dual specificity tyrosine-phosphorylation-regulated kinase 1A
-
dual specificity tyrosine-phosphorylation-regulated kinase 1A Dyrk1A
-
dual specificity tyrosine-phosphorylation-regulated kinase 1B
-
-
dual specificity tyrosine-phosphorylation-regulated kinase 2
-
dual specificity tyrosine-phosphorylation-regulated kinase 3
-
dual specificity tyrosine-phosphorylation-regulated kinase-1A
-
dual-specificity protein kinase
dual-specificity tyrosine phosphorylation-regulated kinase 1A
-
dual-specificity tyrosine phosphorylation-regulated kinase 1A Dyrk1A
-
dual-specificity tyrosine-phosphorylation regulated kinase 1A
-
dual-specificity tyrosine-phosphorylation regulated kinase 2
-
dual-specificity tyrosine-phosphorylation regulated kinase 3
-
dual-specificity tyrosine-phosphorylation-regulated kinase 2
-
-
Dyrk kinase
-
DYRK1A
Dyrk1A kinase
-
-
DYRK1B
DYRK2
erythroid kinase
-
minibrain kinase/dual-specificity tyrosine phosphorylated and regulated kinase 1A
-
-
MNB protein
-
protein kinase CLK1
-
protein kinase CLK2
-
protein kinase CLK3
-
protein kinase gene DYRK3
-
receptor serine/threonine/tyrosine kinase 1
-
-
serine/threonine/tyrosine kinase
-
-
Spleen tyrosine kinase
-
STYK1/NOK
-
-
Syk
cf. EC 2.7.10.2
additional information
-
the enzyme belongs to the insulin receptor substrate family
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
-
-
-
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
-
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 + RRRFRPASPLRGPPK
ADP + RRRFRPApSPLRGPPK
show the reaction diagram
i.e. DYRKtide
-
-
?
ATP + SR protein
ADP + ?
show the reaction diagram
enzyme is involved in the regulation of nuclear functions
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + adaptor protein SH2 domain-containing leukocyte protein
ADP + phospho-[adaptor protein SH2 domain-containing leukocyte protein]
show the reaction diagram
ATP + biotin-Ttds-TPGSRSRTPSLPT
ADP + phosphorylated biotin-Ttds-TPGSRSRTPSLPT
show the reaction diagram
i.e. peptide PEP3
-
-
?
ATP + biotin-Ttds-VGLLKLASPELER
ADP + phosphorylated biotin-Ttds-VGLLKLASPELER
show the reaction diagram
i.e. peptide PEP285
-
-
?
ATP + casein
ADP + phosphorylated casein
show the reaction diagram
-
-
-
-
?
ATP + cyclin L2
ADP + phosphorylated cyclin L2
show the reaction diagram
-
-
-
?
ATP + immunglobulin-alpha
ADP + phospho-[immunglobulin-alpha]
show the reaction diagram
ATP + insulin receptor kinase substrate 1
ADP + phosphorylated insulin receptor kinase substrate 1
show the reaction diagram
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
-
-
-
-
?
ATP + Notch-IC
ADP + phosphorylated Notch-IC
show the reaction diagram
-
-
-
?
ATP + p27
ADP + phospho-p27
show the reaction diagram
-
p27 phosphorylation at Ser10 and Thr198
-
-
?
ATP + peptide DYRKtide
ADP + phosphorylated peptide DYRKtide
show the reaction diagram
-
synthetic peptide substrate
-
-
?
ATP + PRAS40
ADP + phospho-PRAS40
show the reaction diagram
phosphorylation at Thr246
-
-
?
ATP + PRAS40
ADP + phosphorylated PRAS40
show the reaction diagram
i.e. proline rich Akt substrate 40
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + RRARKLTATPTPLGG
ADP + RRARKLTApTPTPLGG
show the reaction diagram
i.e. peptide SAPtide
-
-
?
ATP + RRRFRPASPLRGPPK
ADP + RRRFRPApSPLRGPPK
show the reaction diagram
ATP + S6K1
ADP + phospho-S6K1
show the reaction diagram
phosphorylation at Thr389
-
-
?
ATP + SF3B1 protein-L-Thr434
ADP + [SF3B1 protein]-L-Thr434 phosphate
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 + tau protein-L-Thr434
ADP + [tau protein]-L-Thr434 phosphate
show the reaction diagram
-
-
-
-
?
ATP + VSNGSPSLER
ADP + VSNGpSPSLER
show the reaction diagram
-
a p27-derived peptide, residues 6-15
-
-
?
biliverdin + ?
bilirubin + ?
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
-
-
-
?
ATP + SR protein
ADP + ?
show the reaction diagram
enzyme is involved in the regulation of nuclear functions
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + adaptor protein SH2 domain-containing leukocyte protein
ADP + phospho-[adaptor protein SH2 domain-containing leukocyte protein]
show the reaction diagram
phosphorylation of SLP-65 on several tyrosines
-
-
?
ATP + immunglobulin-alpha
ADP + phospho-[immunglobulin-alpha]
show the reaction diagram
the inhibitory residue of Ig-alpha S197 is phosphorylated in activated B cells by Syk
-
-
?
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 + p27
ADP + phospho-p27
show the reaction diagram
-
p27 phosphorylation at Ser10 and Thr198
-
-
?
ATP + PRAS40
ADP + phospho-PRAS40
show the reaction diagram
phosphorylation at Thr246
-
-
?
ATP + S6K1
ADP + phospho-S6K1
show the reaction diagram
phosphorylation at Thr389
-
-
?
ATP + SF3B1 protein-L-Thr434
ADP + [SF3B1 protein]-L-Thr434 phosphate
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 + tau protein-L-Thr434
ADP + [tau protein]-L-Thr434 phosphate
show the reaction diagram
-
-
-
-
?
biliverdin + ?
bilirubin + ?
show the reaction diagram
-
-
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-4-amine
-
2-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine
-
2-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
-
2-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
-
2-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
-
4-(1,3-benzodioxol-5-yl)-N-(3,4-dibromobenzyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-(3,5-dibromobenzyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-(4-chlorophenyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-[2-bromo-4-(trifluoromethyl)phenyl]pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-[4-(trifluoromethyl)phenyl]pyrimidin-2-amine
-
4-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
-
4-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
-
6-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)pyrimidin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
-
harmine
a plant-derived beta-carboline alkaloid, ATP-competitive
midostaurin
i.e. PKC412, a derivative of the broad-spectrum kinase inhibitor staurosporine, an alkaloid isolated from Streptomyces staurosoreus
N,4-bis(1,3-benzodioxol-5-yl)pyrimidin-2-amine
-
N-(3,4-dichlorobenzyl)-2-(1H-indazol-5-yl)pyrimidin-4-amine
-
N-(3,4-dichlorobenzyl)-4-(1H-indazol-5-yl)pyrimidin-2-amine
-
N-(3,4-dichlorobenzyl)-4-(1H-indazol-6-yl)pyrimidin-2-amine
-
N-(3,4-dichlorobenzyl)-4-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-2-amine
-
N-(3,4-dichlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
-
N-(3,4-dichlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
-
N-(4-chlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
-
N-(4-chlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
-
(1Z)-1-(3-ethyl-5-methoxy-1,3-benzothiazol-2(3H)-ylidene)propan-2-one
-
(4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione
-
82.6% inhibition at 0.01 mM
(4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-nitrobenzylidene)pyrazolidine-3,5-dione
-
76% inhibition at 0.01 mM
(4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxybenzylidene)pyrazolidine-3,5-dione
-
73% inhibition at 0.01 mM
(4Z)-1-(4-fluorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione
-
44% inhibition at 0.01 mM
(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
-
55% inhibition at 0.01 mM
(5-[4-[ethyl(thiophen-2-ylmethyl)amino]quinazolin-6-yl]furan-2-yl)methanol
-
(5-{4-[(5-methylfuran-2-yl)amino]quinazolin-6-yl}furan-2-yl)methanol
-
(5-{4-[methyl(3-methylthiophen-2-yl)amino]quinazolin-6-yl}furan-2-yl)methanol
-
(5Z)-2-(2,6-dichloroanilino)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazol-4-one
i.e. GSK-626616, the DYRK kinase inhibitor GSK-626616 affects, among others, the phosphorylation of mRNA-associated proteins and proteins downstream of mTORC1 signaling
2-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-4-amine
-
2-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine
-
2-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
-
2-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
-
2-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
-
2-methyl-5-[(4-methylphenyl)amino]benzothiazole-4,7-dione
i.e. CDK4 inhibitor III
3-(N-benzyl-N-isopropyl)amino-1-(naphthalen-2-yl)propan-1-one hydrochloride
i.e. Jak3 inhibitor IV
3-[4-(2-phenylethyl)quinazolin-6-yl]benzonitrile
-
3-[4-[2-(4-methoxyphenyl)ethyl]quinazolin-6-yl]benzonitrile
-
3-[4-[2-(4-methylphenyl)ethyl]quinazolin-6-yl]benzonitrile
-
4-(1,3-benzodioxol-5-yl)-N-(3,4-dibromobenzyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-(3,5-dibromobenzyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-(4-chlorophenyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-[2-bromo-4-(trifluoromethyl)phenyl]pyrimidin-2-amine
-
4-(1,3-benzodioxol-5-yl)-N-[4-(trifluoromethyl)phenyl]pyrimidin-2-amine
-
4-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
-
4-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
-
4-(2-phenyl)-9-hydroxypyrrolo[3,4-c]carbazole-1,3-(2H,6H)-dione
i.e. Wee1/Chk1 inhibitor
4-(6-cyclohexylmethoxy-9H-purin-2-ylamino)-N,N-diethylbenzamide
i.e. CDK2 inhibitor IV
4-[(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-3,5-dioxopyrazolidin-1-yl]benzonitrile
-
78% inhibition at 0.01 mM
5-chloro-3-(3,5-dichloro-4-hydroxybenzylidene)-1,3-dihydro-indol-2-one
i.e. HMS3229I17, a CDK2 inhibitor IV
5-[4-(thiophen-2-ylamino)quinazolin-6-yl]furan-2-carboxylic acid
-
5-{4-[(5-methylfuran-2-yl)amino]quinazolin-6-yl}furan-2-carboxylic acid
-
6-(1,3-benzodioxol-5-yl)-N-(1,3-thiazol-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(1,3-thiazol-2-ylmethyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(1H-imidazol-2-yl)-N-methylquinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(1H-imidazol-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(1H-imidazol-2-ylmethyl)-N-methylquinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(1H-imidazol-2-ylmethyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(1H-imidazol-4-ylmethyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(2,2-dimethylpropyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(2-methyl-1,3-thiazol-4-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(2-methylfuran-3-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)pyrimidin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(3-methylthiophen-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(4-methoxybenzyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(5-methylfuran-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(5-methylthiophen-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(cyclopentylmethyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(furan-2-yl)-N-methylquinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(furan-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(furan-2-ylmethyl)-N-methylquinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(furan-2-ylmethyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(furan-3-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(furan-3-ylmethyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(tetrahydro-2H-pyran-2-ylmethyl)quinazolin-4-amine
-
-
6-(1,3-benzodioxol-5-yl)-N-(tetrahydro-2H-pyran-3-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(tetrahydrofuran-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(tetrahydrofuran-2-ylmethyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(tetrahydrofuran-3-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(tetrahydrofuran-3-ylmethyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-benzylquinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-cyclopentylquinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-ethyl-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-ethyl-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(1,3-thiazol-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(1,3-thiazol-2-ylmethyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(2-methyl-1,3-thiazol-4-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(3-methylthiophen-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(4-methyl-1,3-thiazol-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(5-methyl-1,3,4-oxadiazol-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-methyl-N-[(3-methylthiophen-2-yl)methyl]quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-methyl-N-[(4-methyl-1,3-thiazol-2-yl)methyl]quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-methyl-N-[(5-methyl-1,3,4-oxadiazol-2-yl)methyl]quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-[(2-methylfuran-3-yl)methyl]quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-[(3-methylthiophen-2-yl)methyl]quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-[(4-methyl-1,3-thiazol-2-yl)methyl]quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-[(5-methylfuran-2-yl)methyl]quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-[(5-methylthiophen-2-yl)methyl]quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-[2-(1H-imidazol-4-yl)ethyl]quinazolin-4-amine
-
6-(1,3-benzodioxol-5-yl)-N-[2-(furan-2-yl)ethyl]quinazolin-4-amine
-
6-(1-methyl-1H-indazol-6-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(1-methyl-1H-indol-5-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(1-methyl-1H-indol-5-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
6-(2,3-dihydro-1,4-benzodioxin-6-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
6-(2-chlorophenyl)-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(2-chlorophenyl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
6-(2-methylfuran-3-yl)-N-(5-methylfuran-2-yl)quinazolin-4-amine
-
6-(2-methylfuran-3-yl)-N-[(5-methylfuran-2-yl)methyl]quinazolin-4-amine
-
6-(3,4-dimethoxyphenyl)-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(3-chlorophenyl)-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(3-methoxyphenyl)-N-(4-methylbenzyl)quinazolin-4-amine
-
6-(3-methoxyphenyl)-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(3-methoxyphenyl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
6-(3-methoxyphenyl)quinazoline
-
6-(3-methylphenyl)-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(4-fluoro-1,3-benzodioxol-5-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(4-fluoro-1,3-benzodioxol-5-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
6-(4-methoxyphenyl)-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(4-methoxyphenyl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
6-(furan-2-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(furan-2-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
6-(furan-3-yl)-N-(2-methyl-1,3-thiazol-4-yl)quinazolin-4-amine
-
6-(furan-3-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
6-(furan-3-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
6-(furan-3-yl)-N-methyl-N-(3-methylthiophen-2-yl)quinazolin-4-amine
-
6-(furan-3-yl)-N-methyl-N-[(3-methylthiophen-2-yl)methyl]quinazolin-4-amine
-
6-(furan-3-yl)-N-[(2-methyl-1,3-thiazol-4-yl)methyl]quinazolin-4-amine
-
6-(pyridin-3-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
7-(1,3-benzodioxol-5-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
7-methoxy-1-methyl-9H-pyrido[3,4-b]indole
i.e. harmine
ethyl 5-(4-[[(2-methyl-1,3-thiazol-4-yl)methyl]amino]quinazolin-6-yl)furan-2-carboxylate
-
ethyl 5-(4-[[(3-methylthiophen-2-yl)methyl]amino]quinazolin-6-yl)furan-2-carboxylate
-
ethyl 5-(4-[[(5-methylfuran-2-yl)methyl]amino]quinazolin-6-yl)furan-2-carboxylate
-
ethyl 5-(4-[[2-(1H-imidazol-4-yl)ethyl]amino]quinazolin-6-yl)furan-2-carboxylate
-
ethyl 5-[4-(1H-imidazol-2-ylamino)quinazolin-6-yl]furan-2-carboxylate
-
ethyl 5-[4-(thiophen-2-ylamino)quinazolin-6-yl]furan-2-carboxylate
-
ethyl 5-[4-[(1H-imidazol-2-ylmethyl)amino]quinazolin-6-yl]furan-2-carboxylate
-
ethyl 5-[4-[ethyl(thiophen-2-ylmethyl)amino]quinazolin-6-yl]furan-2-carboxylate
-
ethyl 5-{4-[(1H-imidazol-4-ylmethyl)amino]quinazolin-6-yl}furan-2-carboxylate
-
ethyl 5-{4-[(2-methyl-1,3-thiazol-4-yl)amino]quinazolin-6-yl}furan-2-carboxylate
-
ethyl 5-{4-[(5-methylfuran-2-yl)amino]quinazolin-6-yl}furan-2-carboxylate
-
ethyl 5-{4-[methyl(3-methylthiophen-2-yl)amino]quinazolin-6-yl}furan-2-carboxylate
-
genistein
-
-
GSK-626616
i.e. (5Z)-2-(2,6-dichloroanilino)-5-[(quinoxalin-6-yl)methylidene]-1,3-thiazol-4(5H)-one, ATP competitive inhibitor
harmine
HCD160
-
82.6% inhibition at 0.01 mM
leucettamine B
marine alkaloid, strong inhibitor
leucettine L-41
-
midostaurin
i.e. PKC412, a derivative of the broad-spectrum kinase inhibitor staurosporine, an alkaloid isolated from Streptomyces staurosoreus. Enzyme binding structure analysis, overview
N,4-bis(1,3-benzodioxol-5-yl)pyrimidin-2-amine
-
N-(2,2-dimethylpropyl)-6-[5-[(ethylamino)methyl]furan-2-yl]quinazolin-4-amine
-
N-(3,4-dichlorobenzyl)-2-(1H-indazol-5-yl)pyrimidin-4-amine
-
N-(3,4-dichlorobenzyl)-4-(1H-indazol-5-yl)pyrimidin-2-amine
-
N-(3,4-dichlorobenzyl)-4-(1H-indazol-6-yl)pyrimidin-2-amine
-
N-(3,4-dichlorobenzyl)-4-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-2-amine
-
N-(3,4-dichlorobenzyl)-4-(3,4-dimethoxyphenyl)pyrimidin-2-amine
-
N-(3,4-dichlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
-
N-(3,4-dichlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
-
N-(3,4-dichlorobenzyl)-6-(pyridin-3-yl)quinazolin-4-amine
-
N-(4-chlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
-
N-(4-chlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
-
N-(4-chlorobenzyl)-6-(3-methoxyphenyl)quinazolin-4-amine
-
N-(4-chlorobenzyl)-6-(pyridin-3-yl)quinazolin-4-amine
-
N-(4-methoxybenzyl)-6-(3-methoxyphenyl)quinazolin-4-amine
-
N-(4-methoxybenzyl)-6-(pyridin-3-yl)quinazolin-4-amine
-
N-(thiophen-2-yl)-6-(3,4,5-trimethoxyphenyl)quinazolin-4-amine
-
N-tert-butyl-6-{5-[(ethylamino)methyl]furan-2-yl}quinazolin-4-amine
-
RAD-001
a rapamycin derivative
-
roscovitine
-
63% inhibition at 0.01 mM
Zn2+
-
inhibits the autophosphoylation, which cannot be reversed by Mn2+ addition
[5-(4-[methyl[(3-methylthiophen-2-yl)methyl]amino]quinazolin-6-yl)furan-2-yl]methanol
-
{5-[4-(thiophen-2-ylamino)quinazolin-6-yl]furan-2-yl}methanol
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
H2O2
-
the kinase activity of biliverdin reductase is stimulated by generators of free radicals such as H2O2
sodium arsenite
-
the kinase activity of biliverdin reductase is stimulated by generators of free radicals such as sodium arsenite
additional information
autophosphorylation of a tyrosine residue within the activation loop is necessary for full DYRK4 kinase activity
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0807
ATP
pH 6.8, 22°C
0.1185
ATP
pH 6.8, 22°C
additional information
additional information
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000254
midostaurin
pH 6.8, 22°C
0.0000284
midostaurin
pH 6.8, 22°C
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
10
2-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-4-amine
Homo sapiens
above, pH and temperature not specified in the publication
8.862
2-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine
Homo sapiens
pH and temperature not specified in the publication
10
2-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
Homo sapiens
above, pH and temperature not specified in the publication
0.179
2-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.829
2-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.112
4-(1,3-benzodioxol-5-yl)-N-(3,4-dibromobenzyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.038
4-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.018
4-(1,3-benzodioxol-5-yl)-N-(3,5-dibromobenzyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.007
4-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.884
4-(1,3-benzodioxol-5-yl)-N-(4-chlorophenyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.012
4-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.137
4-(1,3-benzodioxol-5-yl)-N-[2-bromo-4-(trifluoromethyl)phenyl]pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.018
4-(1,3-benzodioxol-5-yl)-N-[4-(trifluoromethyl)phenyl]pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.093
4-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
1.156
6-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)quinazolin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.000166
harmine
Homo sapiens
pH and temperature not specified in the publication
0.000066
midostaurin
Homo sapiens
pH 6.8, 22°C
0.042
N,4-bis(1,3-benzodioxol-5-yl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.514
N-(3,4-dichlorobenzyl)-2-(1H-indazol-5-yl)pyrimidin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.125
N-(3,4-dichlorobenzyl)-4-(1H-indazol-5-yl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.599
N-(3,4-dichlorobenzyl)-4-(1H-indazol-6-yl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.055
N-(3,4-dichlorobenzyl)-4-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
10
N-(3,4-dichlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
Homo sapiens
above, pH and temperature not specified in the publication
0.411
N-(3,4-dichlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
6.782
N-(4-chlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.871
N-(4-chlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.00013
TG003
Homo sapiens
pH and temperature not specified in the publication
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
Homo sapiens
-
for autophosphorylation
0.0025
(4Z)-1-(4-fluorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione
Homo sapiens
-
for autophosphorylation
0.0012
(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
Homo sapiens
-
for autophosphorylation
3.454
2-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-4-amine
Homo sapiens
pH and temperature not specified in the publication
4.579
2-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine
Homo sapiens
pH and temperature not specified in the publication
10
2-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
Homo sapiens
above, pH and temperature not specified in the publication
0.349
2-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
Homo sapiens
pH and temperature not specified in the publication
1.434
2-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.0164
3-[4-[2-(4-methoxyphenyl)ethyl]quinazolin-6-yl]benzonitrile
Homo sapiens
pH and temperature not specified in the publication
0.0412
3-[4-[2-(4-methylphenyl)ethyl]quinazolin-6-yl]benzonitrile
Homo sapiens
pH and temperature not specified in the publication
0.018
4-(1,3-benzodioxol-5-yl)-N-(3,4-dibromobenzyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.014
4-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.009
4-(1,3-benzodioxol-5-yl)-N-(3,5-dibromobenzyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.004
4-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.273
4-(1,3-benzodioxol-5-yl)-N-(4-chlorophenyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.016
4-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.107
4-(1,3-benzodioxol-5-yl)-N-[2-bromo-4-(trifluoromethyl)phenyl]pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.01
4-(1,3-benzodioxol-5-yl)-N-[4-(trifluoromethyl)phenyl]pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.061
4-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.0006
4-[(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-3,5-dioxopyrazolidin-1-yl]benzonitrile
Homo sapiens
-
for autophosphorylation
0.282
6-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)quinazolin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.0463
6-(1,3-benzodioxol-5-yl)-N-(4-methoxybenzyl)quinazolin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.026
6-(1,3-benzodioxol-5-yl)-N-benzylquinazolin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.0654
6-(3-methoxyphenyl)-N-(4-methylbenzyl)quinazolin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.026
6-(3-methoxyphenyl)quinazoline
Homo sapiens
pH and temperature not specified in the publication
0.000033 - 0.001
harmine
0.00004
leucettine L-41
Homo sapiens
pH and temperature not specified in the publication
0.000059
midostaurin
Homo sapiens
pH 6.8, 22°C
0.025
N,4-bis(1,3-benzodioxol-5-yl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
2.352
N-(3,4-dichlorobenzyl)-2-(1H-indazol-5-yl)pyrimidin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.0129
N-(3,4-dichlorobenzyl)-4-(1H-indazol-5-yl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.0169
N-(3,4-dichlorobenzyl)-4-(1H-indazol-6-yl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.013
N-(3,4-dichlorobenzyl)-4-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
10
N-(3,4-dichlorobenzyl)-4-(3,4-dimethoxyphenyl)pyrimidin-2-amine
Homo sapiens
above, pH and temperature not specified in the publication
4.654
N-(3,4-dichlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.203
N-(3,4-dichlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.0412
N-(3,4-dichlorobenzyl)-6-(pyridin-3-yl)quinazolin-4-amine
Homo sapiens
pH and temperature not specified in the publication
6.361
N-(4-chlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.558
N-(4-chlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.0207
N-(4-chlorobenzyl)-6-(3-methoxyphenyl)quinazolin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.0292
N-(4-chlorobenzyl)-6-(pyridin-3-yl)quinazolin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.026
N-(4-methoxybenzyl)-6-(3-methoxyphenyl)quinazolin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.0328
N-(4-methoxybenzyl)-6-(pyridin-3-yl)quinazolin-4-amine
Homo sapiens
pH and temperature not specified in the publication
0.000012
TG003
Homo sapiens
pH and temperature not specified in the publication
additional information
additional information
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.2
assay at
8.4
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
assay at room temperature
22
assay at room temperature
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
predominately expressed in muscle and testis
Manually annotated by BRENDA team
predominately expressed in muscle and testis
Manually annotated by BRENDA team
transfection analysis
Manually annotated by BRENDA team
most malignant tumors assessed express TTK mRNA, as well, all rapidly proliferating cell lines tested express TTK mRNA
Manually annotated by BRENDA team
DYRK2 level is lower in primary or metastatic colorectal carcinoma compared to adjacent normal colon tissue or non-metastatic colorectal carcinoma, respectively. DYRK2 expression analysis of in 181 archived colorectal carcinoma samples, overview
Manually annotated by BRENDA team
human brain microvascular endothelial cells
Manually annotated by BRENDA team
DYRK3 is initially identified as an erythroid kinase (REDK), as the gene is expressed preferentially in erythroid cells
Manually annotated by BRENDA team
levels of TTK protein are significantly elevated in neoplastic tissues from a cohort of liver cancer patients, when compared with adjacent hepatic tissues
Manually annotated by BRENDA team
levels of TTK protein are significantly elevated in neoplastic tissues from a cohort of liver cancer patients, when compared with adjacent hepatic tissues
Manually annotated by BRENDA team
bone marrow monocyte
Manually annotated by BRENDA team
transfection analysis
Manually annotated by BRENDA team
strong overexpression of dual specificity kinase TTK
Manually annotated by BRENDA team
-
retinal pigmented epithelial cells
Manually annotated by BRENDA team
co-expression experiments in
Manually annotated by BRENDA team
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
one of several splice variants of DYRK4, the long isoform, contains a nuclear localization signal in its extended N-terminus that mediates its interaction with importin alpha3 and alpha5 and that is capable of targeting a heterologous protein to the nucleus. The nucleocytoplasmic mobility of this variant differs from that of a shorter isoform
Manually annotated by BRENDA team
additional information
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
malfunction
physiological function
additional information
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
DYR1B_HUMAN
629
0
69198
Swiss-Prot
other Location (Reliability: 4)
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
Dyrk1A contains a nuclear targeting signal sequence, a protein kinase domain, a PEST domain (protein domain that is enriched in proline (P), glutamic acid (E), serine (S), and threonine (T) residues), 13 consecutive histidine residues (His repeats) and a serine/threonine rich segment (S/T). The PEST region is located in the C terminus of the catalytic domain. A stretch of 13 histidines located between 607 and 619 amino acid residues follows subsequently a segment of 14 serine/threonine residues
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
purified enzyme DYRK1B bound to inhibitor midostaurin, X-ray diffraction structure determination and analysis
purified enzyme DYRK1A bound to inhibitor midostaurin, sitting drop vapour diffusion method, mixing of 200 nl of 7-10 mg/ml protein in 50 mM MOPS, pH 6.8, 50 mM KCl, 2 mM 2-mercaptoethanol, with 200 nl of precipitant solution containing 10-16% PEG 3350, 0.1 M potassium thiocyanate, 0.1 M KCl (or 0.1 M NaCl or 0.1 M LiCl), for co-crystallization with the inhibitor midostaurin, protein is mixed in a 1:1 ratio with the inhibitor in crystallization solution, containing 100 mM potassium thiocyanate, 50-100 mM LiCl (or NaCl or KCl), and 10-16% PEG 3350, to give a final drop size of 0.004 ml, by hanging drop vapour diffusion method, 5-7 days at room temperature, X-ray diffraction structure determination and analysis at 2.6 A resolution
structure of the mature form in complex with inhibitor harmine, to 1.9 A resolution. The phosphorylation of residue S350 increases the stability of DYRK3 and enhances its kinase activity. The N-terminal autophosphorylation accessory domain stabilizes the DYRK3 protein, followed by autophosphorylation of the tyrosine of the activation loop, which is important for kinase activity
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
K188R
K218M
site-directed mutagenesis, a kinase-deficient mutant
K238M
loss of kinase activity
S350A
50% of wild-type activity, melting temperature decreases by almost 5 degrees compared to wild-type
S350D
80% of wild-type activity, melting temperature is similar to wild-type
S350E
90% of wild-type activity, melting temperature decreases by 2 degrees compared to wild-type
T198A
-
site-directed mutagenesis, the mutation reduces the enzyme activity compared to the wild-type enzyme
Y246F
site-directed mutagenesis, mutation of the autophosphorylation site. The DYRK4 mutant is neither autophosphorylated nor does it display kinase activity on a synthetic substrate, the exogenous peptide substrate DYRKtide
additional information
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
41.8
melting temperature, mutant S350A
44.3
melting temperature, mutant S350E
46.5
melting temperature, wild-type
46.8
melting temperature, mutant S350D
additional information
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
gel filtration
gel filtration, SDS-PAGE
glutathione-Sepharose column chromatography
-
native enzyme partially from both vector and E7 expressing cells by subcellular fractionation
-
recombinant GST-fusion protein from Escherichia coli strain DH5alpha by glutathione affinity chromatography
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
green fluorescent protein fusion protein of DYRK1B is found mainly in the nucleus of transfected COS-7 cells
recombinant expression of His6-tagged Dyrk1b kinase domain, residues 78-451
DNA and amino acid sequence determination and analysis, the enzyme occurs in several splicing variants, expression in human fibroblast 3T3-L1 cell line
-
expressed in Escherichia coli BL21(DE3) cells
-
expressed in Escherichia coli BL21(DE3) codon plus RIL, plasmid pcDNA3.1
expressed in Mus musculus
-
expression in Escherichia coli strain DH5alpha as GST-fusion protein, expression in 293A cells
-
gene DYRK3, recombinant expression of GST-tagged wild-type and mutant enzymes
gene DYRK4, DNA and amino acid sequence determination and analysis, splicing variants analysis and comparison to the murine splicing variants, expression analysis, overview. Recombinant expression of GST-tagged enzyme in Escherichia coli strain BL21(DE3)pLysS and in insect cells
gene TTK, quantitative real time reverse transcription PCR enzyme expression analysis
quantitative real-time PCR expression analysis of DYRK2 expression in colorectal carcinoma samples
recombinant Dyrk1A-protein expressed in mammalian expression vector pcDNA3, wild-type and mutant
the catalytic domain of DYRK1A is expressed in Escherichia coli BL21(DE3) cells
-
the dyrk1a gene is located in the Down syndrome critical region (DSCR) on chromosome 21 and full or partial trisomy of DSCR in Down syndrome (DS) leads to overexpression of DYRK1A, recombinant expression of His6-tagged Dyrk1a kinase domain, residues 126-490
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
the enzyme is upregulated in cells expressing the high-risk human papillomavirus E7 oncogene, which promotes S-phase entry of host cells from quiescent state in the presence of elevated cell cycle inhibitor p27Kip1
-
there are higher levels of full-length DYRK1A in the brains of patients with Down syndrome when compared to control brains
-
TTK kinase is upregulated in pancreatic cancer
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
diagnostics
drug development
the enzyme is a target in drug development for treatment of Alzheimer's disease
medicine
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Lee, K.; Du, C.; Horn, M.; Rabinow, L.
Activity and autophosphorylation of LAMMER protein kinases
J. Biol. Chem.
271
27299-27303
1996
Saccharomyces cerevisiae (P32350), Homo sapiens (P49760), Drosophila melanogaster (P49762)
Manually annotated by BRENDA team
Xia, J.; Yang, X.; Ruan, Q.; Pan, Q.; Liu, C.; Xie, W.; Deng, H.
Molecular cloning and characterization of novel protein kinase gene DYRK3
Zhonghua Yi Xue Yi Chuan Xue Za Zhi
15
327-332
1998
Homo sapiens (O43781), Homo sapiens
Manually annotated by BRENDA team
Becker, W.; Weber, Y.; Wetzel, K.; Eirmbter, K.; Tejedor, F.J.; Joost, H.G.
Sequence characteristics, subcellular localization, and substrate specificity of DYRK-related kinases, a novel family of dual specificity protein kinases
J. Biol. Chem.
273
25893-25902
1998
Homo sapiens (O43781), Homo sapiens (Q92630), Rattus norvegicus (Q63470)
Manually annotated by BRENDA team
Hanes, J.; von der Kammer, H.; Klaudiny, J.; Scheit, K.H.
Characterization by cDNA cloning of two new human protein kinases. Evidence by sequence comparison of a new family of mammalian protein kinases
J. Mol. Biol.
244
665-672
1994
Mus musculus (P22518), Homo sapiens (P49759), Homo sapiens (P49760), Homo sapiens (P49761)
Manually annotated by BRENDA team
Johnson, K.W.; Smith, K.A.
Molecular cloning of a novel human cdc2/CDC28-like protein kinase
J. Biol. Chem.
266
3402-3407
1991
Homo sapiens (P49759), Homo sapiens
Manually annotated by BRENDA team
Winfield, S.L.; Tayebi, N.; Martin, B.M.; Ginns, E.I.; Sidransky, E.
Identification of three additional genes contiguous to the glucocerebrosidase locus on chromosome 1q21: implications for Gaucher disease
Genome Res.
7
1020-1026
1997
Homo sapiens (P49760)
Manually annotated by BRENDA team
Guimera, J.; Casas, C.; Estivill, X.; Pritchard, M.
Human minibrain homologue (MNBH/DYRK1): characterization, alternative splicing, differential tissue expression, and overexpression in Down syndrome
Genomics
57
407-418
1999
Homo sapiens (Q13627), Homo sapiens
Manually annotated by BRENDA team
Dahmane, N.; Ghezala, G.A.; Gosset, P.; Chamoun, Z.; et al.
Transcriptional map of the 2.5-Mb CBR-ERG region of chromosome 21 involved in Down syndrome
Genomics
48
12-23
1998
Homo sapiens (Q13627)
Manually annotated by BRENDA team
Song, W.J.; Sternberg, L.R.; Kasten-Sportes, C.; et al.
Isolation of human and murine homologues of the Drosophila minibrain gene: human homologue maps to 21q22.2 in the Down syndrome "critical region"
Genomics
38
331-339
1996
Homo sapiens (Q13627), Homo sapiens, Mus musculus (Q61214), Mus musculus
Manually annotated by BRENDA team
Shindoh, N.; Kudoh, J.; Maeda, H.; Yamaki, A.; Minoshima, S.; Shimizu, Y.; Shimizu, N.
Cloning of a human homolog of the Drosophila minibrain/rat Dyrk gene from "the Down syndrome critical region" of chromosome 21
Biochem. Biophys. Res. Commun.
225
92-99
1996
Homo sapiens (Q13627), Homo sapiens
Manually annotated by BRENDA team
Guimera, J.; Casas, C.; Pucharcos, C.; et al.
A human homologue of Drosophila minibrain (MNB) is expressed in the neuronal regions affected in Down syndrome and maps to the critical region
Hum. Mol. Genet.
5
1305-1310
1996
Homo sapiens (Q13627)
Manually annotated by BRENDA team
Leder, S.; Weber, Y.; Altafaj, X.; Estivill, X.; Joost, H.G.; Becker, W.
Cloning and characterization of DYRK1B, a novel member of the DYRK family of protein kinases
Biochem. Biophys. Res. Commun.
254
474-479
1999
Homo sapiens (Q9Y463), Homo sapiens
Manually annotated by BRENDA team
Mills, G.B.; Schmandt, R.; McGill, M.; Amendola, A.; Hill, M.; Jacobs, K.; May, C.; Rodricks, A.M.; Campbell, S.; Hogg, D.
Expression of TTK, a novel human protein kinase, is associated with cell proliferation
J. Biol. Chem.
267
16000-16006
1992
Homo sapiens (P33981)
Manually annotated by BRENDA team
Hanks, S.K.; Quinn, A.M.
Protein kinase catalytic domain sequence database: identification of conserved features of primary structure and classification of family members
Methods Enzymol.
200
38-62
1991
Homo sapiens (P33981)
Manually annotated by BRENDA team
Leder, S.; Czajkowska, H.; Maenz, B.; De Graaf, K.; Barthel, A.; Joost, H.G.; Becker, W.
Alternative splicing variants of dual specificity tyrosine phosphorylated and regulated kinase 1B exhibit distinct patterns of expression and functional properties
Biochem. J.
372
881-888
2003
Homo sapiens, Mus musculus (Q9Z188), Mus musculus
Manually annotated by BRENDA team
Lerner-Marmarosh, N.; Shen, J.; Torno, M.D.; Kravets, A.; Hu, Z.; Maines, M.D.
Human biliverdin reductase: A member of the insulin receptor substrate family with serine/threonine/tyrosine kinase activity
Proc. Natl. Acad. Sci. USA
102
7109-7114
2005
Homo sapiens
Manually annotated by BRENDA team
Liu, F.; Liang, Z.; Wegiel, J.; Hwang, Y.W.; Iqbal, K.; Grundke-Iqbal, I.; Ramakrishna, N.; Gong, C.X.
Overexpression of Dyrk1A contributes to neurofibrillary degeneration in Down syndrome
FASEB J.
22
3224-3233
2008
Homo sapiens (Q13627)
Manually annotated by BRENDA team
Liang, Y.J.; Chang, H.S.; Wang, C.Y.; Yu, W.C.
DYRK1A stabilizes HPV16E7 oncoprotein through phosphorylation of the threonine 5 and threonine 7 residues
Int. J. Biochem. Cell Biol.
40
2431-2441
2008
Homo sapiens (Q13627)
Manually annotated by BRENDA team
Shi, J.; Zhang, T.; Zhou, C.; Chohan, M.O.; Gu, X.; Wegiel, J.; Zhou, J.; Hwang, Y.W.; Iqbal, K.; Grundke-Iqbal, I.; Gong, C.X.; Liu, F.
Increased dosage of Dyrk1A alters alternative splicing factor (ASF)-regulated alternative splicing of tau in Down syndrome
J. Biol. Chem.
283
28660-28669
2008
Homo sapiens (Q13627), Homo sapiens
Manually annotated by BRENDA team
Ryoo, S.R.; Cho, H.J.; Lee, H.W.; Jeong, H.K.; Radnaabazar, C.; Kim, Y.S.; Kim, M.J.; Son, M.Y.; Seo, H.; Chung, S.H.; Song, W.J.
Dual-specificity tyrosine(Y)-phosphorylation regulated kinase 1A-mediated phosphorylation of amyloid precursor protein: evidence for a functional link between Down syndrome and Alzheimers disease
J. Neurochem.
104
1333-1344
2008
Homo sapiens (Q13627), Homo sapiens
Manually annotated by BRENDA team
Kapitulnik, J.; Maines, M.D.
Pleiotropic functions of biliverdin reductase: cellular signaling and generation of cytoprotective and cytotoxic bilirubin
Trends Pharmacol. Sci.
30
129-137
2009
Homo sapiens
Manually annotated by BRENDA team
Wegiel, J.; Dowjat, K.; Kaczmarski, W.; Kuchna, I.; Nowicki, K.; Frackowiak, J.; Mazur Kolecka, B.; Wegiel, J.; Silverman, W.P.; Reisberg, B.; Deleon, M.; Wisniewski, T.; Gong, C.X.; Liu, F.; Adayev, T.; Chen-Hwang, M.C.; Hwang, Y.W.
The role of overexpressed DYRK1A protein in the early onset of neurofibrillary degeneration in Down syndrome
Acta Neuropathol.
116
391-407
2008
Homo sapiens
Manually annotated by BRENDA team
Koo, K.A.; Kim, N.D.; Chon, Y.S.; Jung, M.S.; Lee, B.J.; Kim, J.H.; Song, W.J.
QSAR analysis of pyrazolidine-3,5-diones derivatives as Dyrk1A inhibitors
Bioorg. Med. Chem. Lett.
19
2324-2328
2009
Homo sapiens
Manually annotated by BRENDA team
Goeckler, N.; Jofre, G.; Papadopoulos, C.; Soppa, U.; Tejedor, F.J.; Becker, W.
Harmine specifically inhibits protein kinase DYRK1A and interferes with neurite formation
FEBS J.
276
6324-6337
2009
Homo sapiens
Manually annotated by BRENDA team
Yamashita, S.; Chujo, M.; Tokuishi, K.; Anami, K.; Miyawaki, M.; Yamamoto, S.; Kawahara, K.
Expression of dual-specificity tyrosine-(Y)-phosphorylation-regulated kinase 2 (DYRK2) can be a favorable prognostic marker in pulmonary adenocarcinoma
J. Thorac. Cardiovasc. Surg.
138
1303-1308
2009
Homo sapiens
Manually annotated by BRENDA team
Kimbro, K.S.; Duschene, K.; Willard, M.; Moore, J.; Freeman, S.
A novel gene STYK1/NOK is upregulated in estrogen receptor-alpha negative estrogen receptor-beta positive breast cancer cells following estrogen treatment
Mol. Biol. Rep.
35
23-27
2008
Homo sapiens
Manually annotated by BRENDA team
Alexeeva, M.; Aberg, E.; Engh, R.A.; Rothweiler, U.
The structure of a dual-specificity tyrosine phosphorylation-regulated kinase 1A-PKC412 complex reveals disulfide-bridge formation with the anomalous catalytic loop HRD(HCD) cysteine
Acta Crystallogr. Sect. D
71
1207-1215
2015
Homo sapiens (Q13627), Homo sapiens (Q9Y463)
Manually annotated by BRENDA team
Coombs, T.; Tanega, C.; Shen, M.; Wang, J.; Auld, D.; Gerritz, S.; Schoenen, F.; Thomas, C.; Aube, J.
Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: Development of chemical probe ML315
Bioorg. Med. Chem. Lett.
23
3654-3661
2013
Homo sapiens (Q13627), Homo sapiens (Q9Y463)
Manually annotated by BRENDA team
Kaistha, B.P.; Honstein, T.; Mueller, V.; Bielak, S.; Sauer, M.; Kreider, R.; Fassan, M.; Scarpa, A.; Schmees, C.; Volkmer, H.; Gress, T.M.; Buchholz, M.
Key role of dual specificity kinase TTK in proliferation and survival of pancreatic cancer cells
Br. J. Cancer
111
1780-1787
2014
Homo sapiens (P33981), Homo sapiens
Manually annotated by BRENDA team
Wippich, F.; Bodenmiller, B.; Trajkovska, M.G.; Wanka, S.; Aebersold, R.; Pelkmans, L.
Dual specificity kinase DYRK3 couples stress granule condensation/dissolution to mTORC1 signaling
Cell
152
791-805
2013
Homo sapiens (O43781)
Manually annotated by BRENDA team
Leal, F.D.; da Silva Lima, C.H.; de Alencastro, R.B.; Castro, H.C.; Rodrigues, C.R.; Albuquerque, M.G.
Hologram QSAR models of a series of 6-arylquinazolin-4-amine inhibitors of a new Alzheimers disease target: dual specificity tyrosine-phosphorylation-regulated kinase-1A enzyme
Int. J. Mol. Sci.
16
5235-5253
2015
Homo sapiens (Q13627)
Manually annotated by BRENDA team
Qian, W.; Jin, N.; Shi, J.; Yin, X.; Jin, X.; Wang, S.; Cao, M.; Iqbal, K.; Gong, C.X.; Liu, F.
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (Dyrk1A) enhances tau expression
J. Alzheimers Dis.
37
529-538
2013
Homo sapiens (Q13627)
Manually annotated by BRENDA team
Huang, S.-H.; Long, M.; Wu, C.-H.; Kwon-Chung, K.J.; Chang, Y.C.; Chi, F.; Lee, S.; Jong, A.
Invasion of Cryptococcus neoformans into human brain microvascular endothelial cells is mediated through the lipid rafts-endocytic pathway via the dual specificity tyrosine phosphorylation-regulated kinase 3 (DYRK3)
J. Biol. Chem.
286
34761-34769
2011
Homo sapiens (O43781), Homo sapiens
Manually annotated by BRENDA team
Papadopoulos, C.; Arato, K.; Lilienthal, E.; Zerweck, J.; Schutkowski, M.; Chatain, N.; Mueller-Newen, G.; Becker, W.; de la Luna, S
Splice variants of the dual specificity tyrosine phosphorylation-regulated kinase 4 (DYRK4) differ in their subcellular localization and catalytic activity
J. Biol. Chem.
286
5494-5505
2011
Mus musculus (Q8BI55), Homo sapiens (Q9NR20)
Manually annotated by BRENDA team
Pan, Y.; Wang, Y.; Bryant, S.H.
Pharmacophore and 3D-QSAR characterization of 6-arylquinazolin-4-amines as Cdc2-like kinase 4 (Clk4) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (Dyrk1A) inhibitors
J. Chem. Inf. Model.
53
938-947
2013
Homo sapiens (Q13627)
Manually annotated by BRENDA team
Zhou, N.; Yuan, S.; Wang, R.; Zhang, W.; Chen, J.J.
Role of dual specificity tyrosine-phosphorylation-regulated kinase 1B (Dyrk1B) in S-phase entry of HPV E7 expressing cells from quiescence
Oncotarget
6
30745-30761
2015
Homo sapiens
Manually annotated by BRENDA team
Yan, H.; Hu, K.; Wu, W.; Li, Y.; Tian, H.; Chu, Z.; Koeffler, H.P.; Yin, D.
Low expression of DYRK2 (dual specificity tyrosine phosphorylation regulated kinase 2) correlates with poor prognosis in colorectal cancer
PLoS ONE
11
e0159954
2016
Homo sapiens (Q92630), Homo sapiens
Manually annotated by BRENDA team
Heizmann, B; Reth, M.; Infantino, S.
Syk is a dual-specificity kinase that self-regulates the signal output from the B-cell antigen receptor
Proc. Natl. Acad. Sci. USA
107
18563-18568
2010
Homo sapiens (P43405)
Manually annotated by BRENDA team
Miao, R.; Wu, Y.; Zhang, H.; Zhou, H.; Sun, X.; Csizmadia, E.; He, L.; Zhao, Y.; Jiang, C.; Miksad, R.A.; Ghaziani, T.; Robson, S.C.; Zhao, H.
Utility of the dual-specificity protein kinase TTK as a therapeutic target for intrahepatic spread of liver cancer
Sci. Rep.
6
33121
2016
Homo sapiens (P33981), Homo sapiens
Manually annotated by BRENDA team
Morrugares, R.; Correa-Saez, A.; Moreno, R.; Garrido-Rodriguez, M.; Munoz, E.; de la Vega, L.; Calzado, M.A.
Phosphorylation-dependent regulation of the NOTCH1 intracellular domain by dual-specificity tyrosine-regulated kinase 2
Cell. Mol. Life Sci.
77
2621-2639
2020
Homo sapiens (Q92630)
Manually annotated by BRENDA team
Guterman-Ram, G.; Pesic, M.; Orenbuch, A.; Czeiger, T.; Aflalo, A.; Levaot, N.
Dual-specificity tyrosine phosphorylation-regulated kinase 2 regulates osteoclast fusion in a cell heterotypic manner
J. Cell. Physiol.
233
617-629
2018
Homo sapiens (Q92630)
Manually annotated by BRENDA team
Kim, K.; Cha, J.S.; Cho, Y.S.; Kim, H.; Chang, N.; Kim, H.J.; Cho, H.S.
Crystal structure of human dual-specificity tyrosine-regulated kinase 3 reveals new structural features and insights into its auto-phosphorylation
J. Mol. Biol.
430
1521-1530
2018
Homo sapiens (O43781), Homo sapiens
Manually annotated by BRENDA team
Kisaka, J.; Ratner, L.; Kyei, G.
The dual-specificity kinase DYRK1A modulates the levels of cyclin L2 to control HIV replication in macrophages
J. Virol.
94
e01583
2020
Homo sapiens (Q13627), Homo sapiens
Manually annotated by BRENDA team