Information on EC 2.7.1.149 - 1-phosphatidylinositol-5-phosphate 4-kinase and Organism(s) Homo sapiens and UniProt Accession Q8TBX8

Word Map on EC 2.7.1.149
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Specify your search results
Select one or more organisms in this record:
This record set is specific for:
Homo sapiens
UNIPROT: Q8TBX8


The taxonomic range for the selected organisms is: Homo sapiens

The enzyme appears in selected viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.1.149
-
RECOMMENDED NAME
GeneOntology No.
1-phosphatidylinositol-5-phosphate 4-kinase
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
-
-
-
Phosphorylation
-
PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
D-myo-inositol (1,4,5)-trisphosphate biosynthesis
-
-
D-myo-inositol-5-phosphate metabolism
-
-
Inositol phosphate metabolism
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:1-phosphatidyl-1D-myo-inositol-5-phosphate 4-phosphotransferase
-
CAS REGISTRY NUMBER
COMMENTARY hide
104645-76-3
-
247907-17-1
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
UniProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
-
phosphatidylinositol-5-phosphate 4-kinase type II beta knockdown inhibits E-cadherin upregulation induced by the vitamin D3 metabolite 1alpha,25(OH)2D3, while phosphatidylinositol-5-phosphate 4-kinase type II alpha does not
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 + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
show the reaction diagram
ATP + 1-phosphatidyl-1D-myo-inositol 3-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 3,4-bisphosphate
show the reaction diagram
-
poor substrate compared to 1-phosphatidyl-1D-myo-inositol 5-phosphate
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
show the reaction diagram
5' phosphorylation
-
-
r
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
show the reaction diagram
ATP + dipalmitoyl-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + dipalmitoyl-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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 + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
show the reaction diagram
ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
show the reaction diagram
P78356
5' phosphorylation
-
-
r
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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
(2E)-2-(3,4-dihydroxybenzoyl)-3-(3,4-dihydroxyphenyl)prop-2-enenitrile
-
-
(2E)-2-(3,4-dihydroxybenzoyl)-3-(4-hydroxy-3-iodo-5-methoxyphenyl)prop-2-enenitrile
-
-
(3E)-5-amino-3-[(2Z)-1-cyano-2-(3H-indol-3-ylidene)ethylidene]-2,3-dihydro-1H-pyrazole-4-carbonitrile
-
-
(3Z)-2-amino-4-(3,4,5-trihydroxyphenyl)buta-1,3-diene-1,1,3-tricarbonitrile
-
-
2,4-diamino-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
3-(trifluoromethyl)phenyl 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxylate
-
-
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-(3-phenoxyphenyl)pyrimidine-5-carboxamide
-
-
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-methyl-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[3-(2,2,2-trifluoroethoxy)phenyl]pyrimidine-5-carboxamide
-
-
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[4-methyl-3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
4-amino-2-(benzylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
4-amino-2-(dimethylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
4-amino-2-(methylsulfanyl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
4-amino-2-(piperidin-1-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
4-amino-2-hydroxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
4-amino-2-methoxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
4-amino-2-[(2,2-dimethylpropyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
4-amino-2-[(tert-butylcarbamoyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
4-amino-2-[[(1-methyl-1H-pyrazol-5-yl)methyl]amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
4-amino-N-(1,3-benzothiazol-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
-
-
4-amino-N-(1-benzothiophen-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
-
-
4-amino-N-[3-(trifluoromethyl)phenyl]-2-(3,4,4-trimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
-
-
4-amino-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
piperine
-
complete inhibition at 0.1 mM
SAR088
-
-
-
tyrphostin
-
ATP-competitive inhibitors, i.e. tyrosine phosphorylation inhibitors, of isozyme PI5P4Kalpha
tyrphostin 23
-
-
tyrphostin 47
-
-
tyrphostin AG 1478
-
-
tyrphostin AG 490
-
-
tyrphostin AG 494
-
-
tyrphostin AG 537
-
-
tyrphostin AG 555
-
-
tyrphostin AG 698
-
-
tyrphostin AG 808
-
-
additional information
-
high-throughput inhibitor screening method, counterscreen assay and ATP competition assay, overview
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.09418
ATP
isoform PI5P4Kgamma, at pH 7.4 and 22C; isoform PI5P4Kgamma, at pH 7.4 and 30C
0.00394 - 0.06705
ATP
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00000572
ATP
isoform PI5P4Kgamma, at pH 7.4 and 22C
0.000955 - 0.0105
ATP
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.014
(2E)-2-(3,4-dihydroxybenzoyl)-3-(3,4-dihydroxyphenyl)prop-2-enenitrile
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
0.002
(2E)-2-(3,4-dihydroxybenzoyl)-3-(4-hydroxy-3-iodo-5-methoxyphenyl)prop-2-enenitrile
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
0.013
(3E)-5-amino-3-[(2Z)-1-cyano-2-(3H-indol-3-ylidene)ethylidene]-2,3-dihydro-1H-pyrazole-4-carbonitrile
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
0.005
(3Z)-2-amino-4-(3,4,5-trihydroxyphenyl)buta-1,3-diene-1,1,3-tricarbonitrile
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
0.03
2,4-diamino-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
IC50 above 0.03 mM, at pH 7.4 and 26C
0.03
3-(trifluoromethyl)phenyl 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxylate
Homo sapiens
-
IC50 above 0.03 mM, at pH 7.4 and 26C
0.0054
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-(3-phenoxyphenyl)pyrimidine-5-carboxamide
Homo sapiens
-
at pH 7.4 and 26C
0.03
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-methyl-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
IC50 above 0.03 mM, at pH 7.4 and 26C
0.0081
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[3-(2,2,2-trifluoroethoxy)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
at pH 7.4 and 26C
0.013
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[4-methyl-3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
at pH 7.4 and 26C
0.025
4-amino-2-(benzylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
at pH 7.4 and 26C
0.03
4-amino-2-(dimethylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
IC50 above 0.03 mM, at pH 7.4 and 26C
0.03
4-amino-2-(methylsulfanyl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
IC50 above 0.03 mM, at pH 7.4 and 26C
0.03
4-amino-2-(piperidin-1-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
IC50 above 0.03 mM, at pH 7.4 and 26C
0.03
4-amino-2-hydroxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
IC50 above 0.03 mM, at pH 7.4 and 26C
0.03
4-amino-2-methoxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
IC50 above 0.03 mM, at pH 7.4 and 26C
0.008
4-amino-2-[(2,2-dimethylpropyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
at pH 7.4 and 26C
0.03
4-amino-2-[(tert-butylcarbamoyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
IC50 above 0.03 mM, at pH 7.4 and 26C
0.0041
4-amino-2-[[(1-methyl-1H-pyrazol-5-yl)methyl]amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
at pH 7.4 and 26C
0.025
4-amino-N-(1,3-benzothiazol-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
Homo sapiens
-
at pH 7.4 and 26C
0.013
4-amino-N-(1-benzothiophen-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
Homo sapiens
-
at pH 7.4 and 26C
0.03
4-amino-N-[3-(trifluoromethyl)phenyl]-2-(3,4,4-trimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
Homo sapiens
-
IC50 above 0.03 mM, at pH 7.4 and 26C
0.03
4-amino-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
-
IC50 above 0.03 mM, at pH 7.4 and 26C
0.0038
SAR088
Homo sapiens
-
at pH 7.4 and 26C
-
0.001
tyrphostin
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
0.045
tyrphostin 23
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
0.02
tyrphostin 47
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
0.1
tyrphostin AG 1478
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
0.089
tyrphostin AG 490
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
0.089
tyrphostin AG 494
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
0.032
tyrphostin AG 537
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
0.055
tyrphostin AG 555
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
0.05
tyrphostin AG 698
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
0.018
tyrphostin AG 808
Homo sapiens
-
pH 7.4, 22C, isozyme PI5P4Kalpha
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
-
assay at room temperature
30
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
DT40 cell from chicken, that expresses active PIPkin IIbetA tagged at the C-terminus of Hef, a protein component of the Fanconi anemia-related tumor-suppressor complex.
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
isoform PI5P4Kgamma
Manually annotated by BRENDA team
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
47000
-
predicted
49000
-
2 * 49000, recombinant isozyme PIP4Kbeta, SDS-PAGE, and crystal structure of isozyme PIP4Kbeta
53000
FLAG-(His6)2 tagged PIPkin IIbeta, confirmed by western blotting
97000
-
recombinant isozyme PIP4Kbeta
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
x * 47000, calculated from amino acid sequence
?
x * 47000, calculated from amino acid sequence
homodimer
-
2 * 49000, recombinant isozyme PIP4Kbeta, SDS-PAGE, and crystal structure of isozyme PIP4Kbeta
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
By using TALON metal affinity resin.
-
affinity purification of FLAG-His6 tagged proteins using TALON beads
Ni-NTA column chromatography, and gel filtration
-
recombinant GST-tagged isozymes by glutathione affinity chromatography, recombinant HA-tagged isozymes by affinity chromatography from HEK-293 cells
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
PIP5K2 genes are amplified from a whole human brain marathon-ready cDNA library using gene-specific primers. Recombinant protein is expressed from Escherichia coli harbouring PIP5K2s in pET-32a. PCR products are cloned, via incorporated HindIII and BamHI restriction sites, into appropriate plasmid vectors. HeLa, HEK 293, COS-7 and NRK cells are transiently transfected with plasmid constructs.
-
expressed in Escherichia coli BL21(DE3) cells
-
expressed in Escherichia coli BL21(DE3/pLysS) cells
-
expression of EGFP-tagged isozymes PIPKIIbeta and PIPKIIalpha in SW480-ADH cells cytosol and nucleus or cytosol, respectively
-
isozyme PIP4K IIbeta, functional expression in enzyme-deficient CHO-IR cells
-
recombinant expression of GST-tagged isozymes and of HA-tagged isozymes in HEK-293 cells
-
The last 2.6 kbp of the human PIPkin IIbeta gene and the following 3.6 kbp are cloned and inserted into a plasmid which placed a FLAG-(His6)2 double-tag, followed by a puromycin selection cassette between them. Transfection of this into DT40 cells followed by puromycin selection produces cells which have the tag attached to the C-terminus of the protein when expressed by one of the two alleles. Experiments are conducted on one clonal line derived from this procedure calling JPR3. Successful integration of the tag at the correct genomic location was confirmed by PCR analysis.
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
D280K
inactive
E300D
Site-directed mutagenesis is performed on the human Type IIbeta PIPkin cloned into pEGFP-C1 using the QuikChange mutagenesis method, to introduce an Glu300Asp amino acid substitution into the human nuclear localisation sequence producing the equivalent chicken sequence.
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
-
phosphatidylinositol-5-phosphate 4-kinase type II beta might be an effective therapeutic target for preventing of colon cancer progression