Information on EC 2.7.12.1 - dual-specificity kinase and Organism(s) Homo sapiens and UniProt Accession Q92630

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Homo sapiens
UNIPROT: Q92630


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


The taxonomic range for the selected organisms is: Homo sapiens

EC NUMBER
COMMENTARY hide
2.7.12.1
-
RECOMMENDED NAME
GeneOntology No.
dual-specificity kinase
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
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
-
enzyme DYRK2 is a member of the dual specificity kinase family, which can phosphorylate both Ser/Thr and Tyr substrates. At least seven DYRK family members have been identified (DYRK1A, DYRK1B, DYRK1C, DYRK2, DYRK3, DYRK4A and DYRK4B)
physiological function
-
role of DYRK2 in human cancer and as a potential oncogene. Overexpression of DYRK2 predicts a better survival in human non-small cell lung cancer, low expression level of DYRK2 correlates with poor prognosis in colorectal cancer. DYRK2 expression is significantly downregulated in colorectal cancer tissues compared with adjacent non-tumorous tissues. Enzyme DYRK2 inhibits cell invasion and migration in both HCT-116 and SW-480 cells and functions as a tumor suppressor in colorectal cancer cells. DYRK2 behaves as a proapoptotic kinase through phosphorylation of p53 at S46 which promotes its apoptotic activity. Downregulation of DYRK2 also induces a G2/M arrest. DYRK2 inhibits the proliferation, cell migration and invasion of colorectal cancer cells in vitro
evolution
enzyme DYRK4 belongs to the dual specificity tyrosine phosphorylation-regulated kinases, DYRKs, a family of conserved protein kinases that play key roles in the regulation of cell differentiation, proliferation, and survival. DYRKs contain a conserved Tyr-Xaa-Tyr motif in the activation loop. Autophosphorylation of a second tyrosine residue within the activation loop is necessary for full DYRK4 kinase activity and is a defining feature of the DYRK family. Family members DYRK1A, DYRK2, and DYRK4 differ in their target recognition sequence, and preference for an arginine residue at position P -3 is a feature of DYRK1A but not of DYRK2 and DYRK4
malfunction
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 + protein
ADP + phosphoprotein
show the reaction diagram
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 + 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 + 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 + protein
ADP + phosphoprotein
show the reaction diagram
ATP + RRARKLTATPTPLGG
ADP + phosphorylated RRARKLTATPTPLGG
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 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 + adaptor protein SH2 domain-containing leukocyte protein
ADP + phospho-[adaptor protein SH2 domain-containing leukocyte protein]
show the reaction diagram
P43405
phosphorylation of SLP-65 on several tyrosines
-
-
?
ATP + immunglobulin-alpha
ADP + phospho-[immunglobulin-alpha]
show the reaction diagram
P43405
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
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(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
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-
(5-{4-[(5-methylfuran-2-yl)amino]quinazolin-6-yl}furan-2-yl)methanol
-
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(5-{4-[methyl(3-methylthiophen-2-yl)amino]quinazolin-6-yl}furan-2-yl)methanol
-
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(5Z)-2-(2,6-dichloroanilino)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazol-4-one
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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
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-
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
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2-methyl-5-[(4-methylphenyl)amino]benzothiazole-4,7-dione
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i.e. CDK4 inhibitor III
3-(N-benzyl-N-isopropyl)amino-1-(naphthalen-2-yl)propan-1-one hydrochloride
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i.e. Jak3 inhibitor IV
3-[4-(2-phenylethyl)quinazolin-6-yl]benzonitrile
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3-[4-[2-(4-methoxyphenyl)ethyl]quinazolin-6-yl]benzonitrile
-
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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
DMSO
-
-
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
-
-
harmine
HCD160
-
82.6% inhibition at 0.01 mM
leucettamine
-
marine alkaloid, strong inhibitor
-
leucettine L-41
-
-
-
midostaurin
ML315
-
-
-
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
sorbitol
-
-
TG003
-
-
-
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 - 0.1185
ATP
additional information
additional information
-
Michaelis-Menten kinetics
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000254 - 0.0000284
midostaurin
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
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 - 10
2-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-4-amine
4.579 - 8.862
2-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine
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 - 0.349
2-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
0.829 - 1.434
2-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
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 - 0.112
4-(1,3-benzodioxol-5-yl)-N-(3,4-dibromobenzyl)pyrimidin-2-amine
0.014 - 0.038
4-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-2-amine
0.009 - 0.018
4-(1,3-benzodioxol-5-yl)-N-(3,5-dibromobenzyl)pyrimidin-2-amine
0.004 - 0.007
4-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)pyrimidin-2-amine
0.273 - 0.884
4-(1,3-benzodioxol-5-yl)-N-(4-chlorophenyl)pyrimidin-2-amine
0.012 - 0.016
4-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
0.107 - 0.137
4-(1,3-benzodioxol-5-yl)-N-[2-bromo-4-(trifluoromethyl)phenyl]pyrimidin-2-amine
0.01 - 0.018
4-(1,3-benzodioxol-5-yl)-N-[4-(trifluoromethyl)phenyl]pyrimidin-2-amine
0.061 - 0.093
4-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
0.0006
4-[(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-3,5-dioxopyrazolidin-1-yl]benzonitrile
Homo sapiens
-
for autophosphorylation
0.282 - 1.156
6-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)quinazolin-4-amine
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 - 0.000066
midostaurin
0.025 - 0.042
N,4-bis(1,3-benzodioxol-5-yl)pyrimidin-2-amine
0.514 - 2.352
N-(3,4-dichlorobenzyl)-2-(1H-indazol-5-yl)pyrimidin-4-amine
0.0129 - 0.125
N-(3,4-dichlorobenzyl)-4-(1H-indazol-5-yl)pyrimidin-2-amine
0.0169 - 0.599
N-(3,4-dichlorobenzyl)-4-(1H-indazol-6-yl)pyrimidin-2-amine
0.013 - 0.055
N-(3,4-dichlorobenzyl)-4-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-2-amine
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 - 10
N-(3,4-dichlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
0.203 - 0.411
N-(3,4-dichlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
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 - 6.782
N-(4-chlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
0.558 - 0.871
N-(4-chlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
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 - 0.00013
TG003
-
additional information
additional information
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.8
-
assay at
7
-
assay at
7.2
-
assay at
8.4
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
-
assay at room temperature
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
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
-
predominately expressed in 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
-
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
-
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
SUBUNITS
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
-
autophosphorylation
phosphoprotein
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
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
-
purified enzyme DYRK1B bound to inhibitor midostaurin, X-ray diffraction structure determination and analysis
-
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
inhibitors PKC412 and harmine elevate the melting point in buffer of the enzyme from 51°C to 53°C and 57°C, respectively
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
quantitative real-time PCR expression analysis of DYRK2 expression in colorectal carcinoma samples
-
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; the catalytic domain of DYRK1A is 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
-
green fluorescent protein fusion protein of DYRK1B is found mainly in the nucleus of transfected COS-7 cells
-
recombinant Dyrk1A-protein expressed in mammalian expression vector pcDNA3, wild-type and mutant
recombinant expression of His6-tagged Dyrk1b kinase domain, residues 78-451
-
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
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
K218M
-
site-directed mutagenesis, a kinase-deficient mutant
T198A
-
site-directed mutagenesis, the mutation reduces the enzyme activity compared to the wild-type enzyme
Y246F
site-directed mutagenesis, mutation of the autophosporylation site. The DYRK4 mutant is neither autophosphorylated nor does it display kinase activity on a synthetic substrate, the exogenous peptide substrate DYRKtide
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
diagnostics
-
enzyme DYRK2 expression is an independent prognostic factor and can be used as a prognostic biomarker of human colorectal cancer
diagnostics
drug development
-
the enzyme is a target in drug development for treatment of Alzheimer's disease
medicine