Information on EC 3.1.3.46 - fructose-2,6-bisphosphate 2-phosphatase and Organism(s) Homo sapiens and UniProt Accession Q16877

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Homo sapiens
UNIPROT: Q16877


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


The taxonomic range for the selected organisms is: Homo sapiens

EC NUMBER
COMMENTARY hide
3.1.3.46
-
RECOMMENDED NAME
GeneOntology No.
fructose-2,6-bisphosphate 2-phosphatase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
beta-D-fructose 2,6-bisphosphate + H2O = D-fructose 6-phosphate + phosphate
show the reaction diagram
FBPase performs a reaction following a classical ping pong mechanism with formation of a phosphoryl-enzyme intermediate on a histidine residue located in an Arg-His-Gly triad, catalytic site structure, overview
beta-D-fructose 2,6-bisphosphate + H2O = D-fructose 6-phosphate + phosphate
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of phosphoric ester
PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
fructose 2,6-bisphosphate biosynthesis
-
-
Fructose and mannose metabolism
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-
SYSTEMATIC NAME
IUBMB Comments
beta-D-fructose-2,6-bisphosphate 2-phosphohydrolase
The enzyme copurifies with EC 2.7.1.105 6-phosphofructo-2-kinase. (cf. EC 3.1.3.54 fructose-2,6-bisphosphate 6-phosphatase).
CAS REGISTRY NUMBER
COMMENTARY hide
81611-75-8
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
knockdown of isoform PFKFB4 reduces tumor growth, glucose uptake and beta-D-fructose 2,6-bisphosphate and increases apoptosis
physiological function
fructose-2,6-bisphosphate synthesis by 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 is required for the glycolytic response to hypoxia and tumor growth
physiological function
-
PFKFB2 has a critical role in glucose uptake and glucose-dependent lipid synthesis. Induction of de novo lipid synthesis by androgen requires the transcriptional up-regulation of HK2 and PFKFB2, and phosphorylation of PFKFB2 generated by the PI3K/Akt signalling pathway to supply the source for lipogenesis from glucose in prostate cancer cells
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
beta-D-fructose 2,6-bisphosphate + H2O
D-fructose 6-phosphate + phosphate
show the reaction diagram
beta-D-fructose 2,6-bisphosphate + H2O
D-fructose 6-phosphate + phosphate
show the reaction diagram
D-fructose 2,6-bisphosphate + H2O
D-fructose 6-phosphate + phosphate
show the reaction diagram
-
-
-
-
?
fructose 2,6-bisphosphate + H2O
?
show the reaction diagram
-
-
-
-
-
fructose 2,6-bisphosphate + H2O
fructose 6-phosphate + phosphate
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
beta-D-fructose 2,6-bisphosphate + H2O
D-fructose 6-phosphate + phosphate
show the reaction diagram
beta-D-fructose 2,6-bisphosphate + H2O
D-fructose 6-phosphate + phosphate
show the reaction diagram
D-fructose 2,6-bisphosphate + H2O
D-fructose 6-phosphate + phosphate
show the reaction diagram
-
-
-
-
?
fructose 2,6-bisphosphate + H2O
?
show the reaction diagram
-
-
-
-
-
additional information
?
-
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
dimethyloxalylglycine
inhibits the splice isozyme PFKFB-4
(2E)-2-(1,3-benzodioxol-5-ylmethylidene)butanedioic acid
-
mimics binding pattern of fructose 6-phosphate
([2-[(5-nitropyridin-2-yl)amino]phenyl]sulfanyl)acetic acid
-
mimics binding pattern of fructose 6-phosphate
1,1'-ethane-1,2-diylbis(4-acetylpyrrolidine-2,3,5-trione)
-
mimics binding pattern of fructose 6-phosphate
1-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-(2-methyl-4-nitro-1H-imidazol-1-yl)ethanol
-
mimics binding pattern of fructose 6-phosphate
1-amino-4-(2-nitro-1H-imidazol-1-yl)butan-2-ol
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mimics binding pattern of fructose 6-phosphate
2-((5-bromo-6-oxo-1-phenyl-1,6-dihydropyridazin-4-yl)amino)acetamide
-
-
2-(1,3-benzodioxol-5-ylmethyl)-3-methylbutanedioic acid
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mimics binding pattern of fructose 6-phosphate
2-(2-nitrophenoxy)-N-phenylacetamide
-
mimics binding pattern of fructose 6-phosphate
2-(3H-indol-7-ylmethyl)butanedioic acid
-
mimics binding pattern of fructose 6-phosphate
2-(5-amino-4-carbamoyl-1H-pyrazol-1-yl)ethanesulfonic acid
-
mimics binding pattern of fructose 6-phosphate
2-(5-bromo-6-oxo-1-phenyl-1,6-dihydropyridazin-4-yl)-1,2,3,4-tetrahydroisoquinoline-5-carbonitrile
-
-
2-(acetylamino)-beta-oxophenylalanine
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mimics binding pattern of fructose 6-phosphate
2-nitro-N-(pyrazin-2-ylmethyl)benzenesulfonamide
-
mimics binding pattern of fructose 6-phosphate
2-nitro-N-quinolin-3-ylbenzenesulfonamide
-
mimics binding pattern of fructose 6-phosphate
2-[(4-nitro-1H-benzimidazol-7-yl)sulfanyl]ethyl benzoate
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mimics binding pattern of fructose 6-phosphate
2-[(5-nitropyridin-2-yl)amino]ethyl 5-nitro-1H-pyrrole-2-carboxylate
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mimics binding pattern of fructose 6-phosphate
2-[(furan-2-ylmethyl)amino]-5-nitrobenzoic acid
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mimics binding pattern of fructose 6-phosphate
2-[[(2Z)-2-(phenylhydrazono)acetyl]amino]benzoic acid
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mimics binding pattern of fructose 6-phosphate
2-[[2-(2,4-dinitrophenyl)hydrazino]carbonyl]benzoic acid
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mimics binding pattern of fructose 6-phosphate
3,3'-(2,4,6-trioxo-1,3,5-triazinane-1,3-diyl)dipropanoic acid
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mimics binding pattern of fructose 6-phosphate
3-(3-pyridin-2-yl-1,2,4-oxadiazol-5-yl)-N-(tetrahydrofuran-2-ylmethyl)propanamide
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mimics binding pattern of fructose 6-phosphate
3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
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3-acetylphenyl (3-acetylphenyl)acetate
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mimics binding pattern of fructose 6-phosphate
3-[(2-pyridin-2-ylhydrazino)carbonyl]pyrazine-2-carboxylic acid
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mimics binding pattern of fructose 6-phosphate
4-(4-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-5-bromo-6-oxopyridazin-1(6H)-yl)benzonitrile
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4-bromo-2-phenyl-5-(((tetrahydrofuran-2-yl)methyl)amino)pyridazin-3(2H)-one
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4-bromo-2-phenyl-5-(2-oxa-6-azaspiro[3.3]heptan-6-yl)pyridazin-3(2H)-one
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4-bromo-5-morpholino-2-phenylpyridazin-3(2H)-one
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5,6,7,8-tetrahydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
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competitive inhibitor
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-2-benzyl-4-bromopyridazin-3(2H)-one
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5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-2-benzylpyridazin-3(2H)-one
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5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(3-phenylpropyl)pyridazin-3(2H)-one
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5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-((2-(dimethylamino)ethyl)-amino)benzyl)pyridazin-3(2H)-one
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5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-(trifluoromethoxy)phenyl)-pyridazin-3(2H)-one
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5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-chlorophenyl)pyridazin-3(2H)-one
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5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-iodobenzyl)pyridazin-3(2H)-one
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5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(pyrimidin-5-yl)pyridazin-3(2H)-one
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5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-phenethylpyridazin-3(2H)-one
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5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-phenylpyridazin-3(2H)-one
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5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-chloro-2-phenylpyridazin-3(2H)-one
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5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-ethoxy-2-phenylpyridazin-3(2H)-one
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5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-iodo-2-phenylpyridazin-3(2H)-one
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5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-isopropyl-2-phenylpyridazin-3(2H)-one
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5-hydroxy-N-(4-nitro-1,3-thiazol-2-yl)-2,4-dioxopentanamide
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mimics binding pattern of fructose 6-phosphate
citrate
-
inhibits the cardiac enzyme
ethyl 1-(6-oxo-1-phenyl-5-(2-oxa-6-azaspiro[3.3]heptan-6-yl)-1,6-dihydropyridazin-4-yl)-1H-1,2,3-triazole-4-carboxylate
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fructose 6-phosphate
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noncompetetive
phosphoenolpyruvate
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-
additional information
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
Cyclic AMP dependent protein kinase
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-
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Protein kinase C
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-
-
additional information
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the hepatic enzyme expression is stimulated at transcriptional level by both insulin and glucocorticoids
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0102 - 0.204
beta-D-fructose 2,6-bisphosphate
0.0043 - 0.016
fructose 2,6-bisphosphate
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1
2-((5-bromo-6-oxo-1-phenyl-1,6-dihydropyridazin-4-yl)amino)acetamide
Homo sapiens;
-
IC50 above 1.0 mM, in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.5
2-(5-bromo-6-oxo-1-phenyl-1,6-dihydropyridazin-4-yl)-1,2,3,4-tetrahydroisoquinoline-5-carbonitrile
Homo sapiens;
-
IC50 above 0.5 mM,in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.026
3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
Homo sapiens;
-
in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.0084
4-(4-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-5-bromo-6-oxopyridazin-1(6H)-yl)benzonitrile
Homo sapiens;
-
in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
1
4-bromo-2-phenyl-5-(((tetrahydrofuran-2-yl)methyl)amino)pyridazin-3(2H)-one
Homo sapiens;
-
IC50 above 1.0 mM, in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
1
4-bromo-2-phenyl-5-(2-oxa-6-azaspiro[3.3]heptan-6-yl)pyridazin-3(2H)-one
Homo sapiens;
-
IC50 above 1.0 mM, in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
1
4-bromo-5-morpholino-2-phenylpyridazin-3(2H)-one
Homo sapiens;
-
IC50 above 1.0 mM,in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.0034
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-2-benzyl-4-bromopyridazin-3(2H)-one
Homo sapiens;
-
in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
10
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-2-benzylpyridazin-3(2H)-one
Homo sapiens;
-
IC50 above 10 mM, in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.011
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(3-phenylpropyl)pyridazin-3(2H)-one
Homo sapiens;
-
in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.5
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-((2-(dimethylamino)ethyl)-amino)benzyl)pyridazin-3(2H)-one
Homo sapiens;
-
IC50 above 0.5 mM, in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.0091
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-(trifluoromethoxy)phenyl)-pyridazin-3(2H)-one
Homo sapiens;
-
in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.007
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-chlorophenyl)pyridazin-3(2H)-one
Homo sapiens;
-
in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.0087
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-iodobenzyl)pyridazin-3(2H)-one
Homo sapiens;
-
in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.0096
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(pyrimidin-5-yl)pyridazin-3(2H)-one
Homo sapiens;
-
in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.0026
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-phenethylpyridazin-3(2H)-one
Homo sapiens;
-
in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.0074
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-phenylpyridazin-3(2H)-one
Homo sapiens;
-
in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.0262
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-chloro-2-phenylpyridazin-3(2H)-one
Homo sapiens;
-
in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
1
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-ethoxy-2-phenylpyridazin-3(2H)-one
Homo sapiens;
-
IC50 above 1.0 mM, in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.013
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-iodo-2-phenylpyridazin-3(2H)-one
Homo sapiens;
-
in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.5
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-isopropyl-2-phenylpyridazin-3(2H)-one
Homo sapiens;
-
IC50 above 0.5 mM, in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
0.055
ethyl 1-(6-oxo-1-phenyl-5-(2-oxa-6-azaspiro[3.3]heptan-6-yl)-1,6-dihydropyridazin-4-yl)-1H-1,2,3-triazole-4-carboxylate
Homo sapiens;
-
in 40 mM Tris pH 7.5, 20 mM MgCl2, 0.1 mg/ml bovine serum albumin, at 30C
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.5
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
melanoma cell line, minor splice isozyme PFKFB-4, major isozyme is PFKFB-3, isozyme PFKFB-4 is overexpressed in hypoxic conditions
Manually annotated by BRENDA team
minor splice isozyme PFKFB-4, major isozyme is PFKFB-3
Manually annotated by BRENDA team
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inducible expression of isozyme PFKFB3, visceral fat cell
Manually annotated by BRENDA team
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overexpression of isozyme PFKFB-4 in breast and colon malignant tumors compared to non-malignant tissue, overexpression of isozyme PFKFB-4 is correlated with enhanced expression of isozyme PFKFB-3, hypoxia-inducible factor 1alpha, dependent glucose transporter 1, and vascular endothelial growth factor VEGF, overview
Manually annotated by BRENDA team
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overexpression of isozyme PFKFB-4 in breast and colon malignant tumors compared to non-malignant tissue, overexpression of isozyme PFKFB-4 is correlated with enhanced expression of isozyme PFKFB-3, hypoxia-inducible factor 1alpha, dependent glucose transporter 1, and vascular endothelial growth factor VEGF, overview
Manually annotated by BRENDA team
isoform pattern
Manually annotated by BRENDA team
isozyme PFKFB4
Manually annotated by BRENDA team
additional information
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
12000
-
gel filtration
54000
-
x * 54000, there are 2 isoforms of 54000 and 58000 Da, SDS-PAGE
58000
-
x * 58000, there are 2 isoforms of 54000 and 58000 Da, SDS-PAGE
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
homodimeric bifunctional enzyme
?
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x * 54000, there are 2 isoforms of 54000 and 58000 Da, SDS-PAGE; x * 58000, there are 2 isoforms of 54000 and 58000 Da, SDS-PAGE
monomer
-
1* 36600 and 1* 35600 which seems a degradation product of the larger subunit, SDS-PAGE
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
by the sitting-drop, vapor-diffusion method, crystals of PFKFB D-fructose 6-phosphate complex in the presence of the nonreactive ATP-analogue AMPPCP beta,gamma-methyleneadenosine 5-triphosphate and crystals the inhibitory complex of PFKFB ADP and phosphoenolpyruvate
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crystal structure of the liver enzyme
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in complex with D-fructose 6-phosphate, diphosphate, or AlF4, sitting drop vapor diffusion method, using 100 mM Tris-HCl, pH 7.5, 20-25% (w/v) ethylene glycol, 200-400 mM tartaric acid, 5% (v/v) glycerol, and 12% (w/v) polyethylene glycol 4000
purified recombinant inducible isozyme PFKFB3, 8 mg/ml protein in 20 mM Tris-HCl, pH 8.0, 10 mM sodium phosphate, 0.05 mM EDTA, 5 mM 2-mercaptoethanol, 0.2 mM ADP, 5% glycerol, and 0.2 mM fructose-6-phosphate, sitting drop vapour diffusion method in presence or absence of fructose-2,6-bisphosphate, the protein sample is mixed with an equal volume of mother liquor containing 50 mM Tris-HCl, pH 7.5, 20-25% ethylene glycol, 12% dioxane, 5% glycerol, and 12% PEG 4000, 2-3 weeks, removal of free phosphate from crystals prior to X-ray diffraction structure determination and analysis at 2.1 A resolution; sitting-drop vapor diffusion of the 1:1 mixture of the protein sample with mother liquor of 50 mM Tris-HCl, pH 7.5, 20.35% ethylene glycol, 12% dioxane, 5% glycerol, and 12% polyethylene glycol 4000. Crystals in a size of 0.2 * 0.2 * 0.05 mm grow in 2-3 weeks. Determination of structure at 2.1 A resolution
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
glutathione Sepharose 4 column chromatography
-
Ni-NTA affinity column chromatography
recombinant His-tagged inducible isozyme PFKFB3 from Escherichia coli strain BL21(DE3) by nickel affinity chromatography, after which the tag is cleaved off by thrombin, followed by anion exchange chromatography, to homogeneity
recombinant His6-tagged bifunctional 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase from Escherichia coli strain BL21(DE3) pLysS by nickel affinity chromatography and anion exchange chromatography with triethylammonium bicarbonate as eluant
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using Ni-NTA affinity columns
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Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
gene PFKFB4, DNA and amino acid sequence determination, expression analysis in DB-1 melanoma cells
genes PFKFB1-4, chromosomal localization of tissue-specific isozymes, phylogenetic analysis, overview, transcriptional control of isozymes, overview
expressed in Escherichia coli BL21(DE3) cells
expression in Escherichia coli
-
expression of His-tagged inducible isozyme PFKFB3 in Escherichia coli strain BL21(DE3)
expression of His6-tagged bifunctional 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase in Escherichia coli strain BL21(DE3) pLysS
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genes PFKFB1-4, chromosomal localization of tissue-specific isozymes, phylogenetic analysis, overview, transcriptional control of isozymes, overview
KDO-phosphatase knockout, enzyme is encoded by 4 genes, PFKFB1-4, PFKFB3 is activated by mitogenic, inflammatory and hypoxic stimuli
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overexpression in Escherichia coli as His6-tagged fusion protein
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
the enzyme isoform PFKFB4 is about 3fold overexpressed in lung adenocarcinoma compared to normal lung tissue. PFKFB4 mRNA and protein expression are also increased by hypoxia
androgen stimulates glycolysis for de novo lipid synthesis by increasing the activities of hexokinase 2 and 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 2, up-regulation of PFKFB2 expression in LNCaP cells is mediated by the direct binding of ligand-activated androgen receptor to the PFKFB2 promoter. Expression of PFKFB2 gene is increased 3.0fold by treatment with methyltrienolone, i.e. R1881, a synthetic androgen
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the enzyme is induced in hypoxia and upregulated as a consequence of the transcriptional changes orchestrated by the androgen receptor in prostate cancer cells
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the protein levels are markedly elevated in high-grade astrocytomas relative to low-grade astrocytomas and corresponding non-neoplastic brain tissue, whereas no significant increase of PFKFB3 mRNA is observed in high-grade astrocytomas
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ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
A44G
-
site directed mutagenesis
A44V
-
site directed mutagenesis
K168A
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site directed mutagenesis
K168N
-
site directed mutagenesis
K168R
-
site directed mutagenesis
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
pharmacological disruption of the PFKFB4 kinase domain may have clinical utility for the treatment of human cancers
medicine
pharmacology
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a pharmacophore map is generated and validated to identify inhibitors of the F6PFBPase complex