Cloned (Comment) | Organism |
---|---|
gene PFKFB3, recombinant expression of GST-tagged isozyme PFKFB3 in Escherichia coli strain BL21(DE3) | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2E)-1-(pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one | - |
Homo sapiens | |
(2E)-3-(pyridin-3-yl)-1-(pyridin-4-yl)prop-2-en-1-one | - |
Homo sapiens | |
2-((5-bromo-6-oxo-1-phenyl-1,6-dihydropyridazin-4-yl)amino)acetamide | - |
Homo sapiens | |
2-(5-bromo-6-oxo-1-phenyl-1,6-dihydropyridazin-4-yl)-1,2,3,4-tetrahydroisoquinoline-5-carbonitrile | - |
Homo sapiens | |
2-hydroxy-4-[(naphthalen-1-ylsulfonyl)amino]benzoic acid | - |
Homo sapiens | |
3H-benzo[e]indol-2-yl(pyridin-4-yl)methanone | - |
Homo sapiens | |
4-(4-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-5-bromo-6-oxopyridazin-1(6H)-yl)benzonitrile | - |
Homo sapiens | |
4-bromo-2-phenyl-5-(((tetrahydrofuran-2-yl)methyl)amino)pyridazin-3(2H)-one | - |
Homo sapiens | |
4-bromo-2-phenyl-5-(2-oxa-6-azaspiro[3.3]heptan-6-yl)pyridazin-3(2H)-one | - |
Homo sapiens | |
4-bromo-5-morpholino-2-phenylpyridazin-3(2H)-one | - |
Homo sapiens | |
5,6,7,8-tetrahydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one | - |
Homo sapiens | |
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-2-benzyl-4-bromopyridazin-3(2H)-one | - |
Homo sapiens | |
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-2-benzylpyridazin-3(2H)-one | - |
Homo sapiens | |
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(3-phenylpropyl)pyridazin-3(2H)-one | - |
Homo sapiens | |
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 | |
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-(trifluoromethoxy)phenyl)-pyridazin-3(2H)-one | - |
Homo sapiens | |
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-chlorophenyl)pyridazin-3(2H)-one | - |
Homo sapiens | |
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-iodobenzyl)pyridazin-3(2H)-one | - |
Homo sapiens | |
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(pyrimidin-5-yl)pyridazin-3(2H)-one | - |
Homo sapiens | |
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-phenethylpyridazin-3(2H)-one | - |
Homo sapiens | |
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-phenylpyridazin-3(2H)-one | - |
Homo sapiens | |
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-chloro-2-phenylpyridazin-3(2H)-one | - |
Homo sapiens | |
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-ethoxy-2-phenylpyridazin-3(2H)-one | - |
Homo sapiens | |
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-iodo-2-phenylpyridazin-3(2H)-one | - |
Homo sapiens | |
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-isopropyl-2-phenylpyridazin-3(2H)-one | - |
Homo sapiens | |
7,8-dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one | - |
Homo sapiens | |
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 | |
additional information | enzyme structure-activity relationships, screening of a small-molecule library, and design and synthesis of 5-triazolo-2-arylpyridazinone analogus inhibitors, molecular docking using the X-ray structure for human PFKFB3, PDB ID 2AXN, overview | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + beta-D-fructose 6-phosphate | Homo sapiens | - |
ADP + beta-D-fructose 2,6-bisphosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q16875 | gene/isozyme PFKFB3 | - |
Purification (Comment) | Organism |
---|---|
recombinant GST-tagged isozyme PFKFB3 from Escherichia coli strain BL21(DE3) by glutathione affinity chromatography | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + beta-D-fructose 6-phosphate | - |
Homo sapiens | ADP + beta-D-fructose 2,6-bisphosphate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
6-phosphofructo-2-kinase/2,6-bisphosphatase 3 | - |
Homo sapiens |
PFKFB3 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
30 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0026 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-phenethylpyridazin-3(2H)-one | |
0.0034 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-2-benzyl-4-bromopyridazin-3(2H)-one | |
0.007 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-chlorophenyl)pyridazin-3(2H)-one | |
0.0074 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-phenylpyridazin-3(2H)-one | |
0.0084 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 4-(4-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-5-bromo-6-oxopyridazin-1(6H)-yl)benzonitrile | |
0.0087 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-iodobenzyl)pyridazin-3(2H)-one | |
0.0091 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-(trifluoromethoxy)phenyl)-pyridazin-3(2H)-one | |
0.0096 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(pyrimidin-5-yl)pyridazin-3(2H)-one | |
0.011 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(3-phenylpropyl)pyridazin-3(2H)-one | |
0.013 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-iodo-2-phenylpyridazin-3(2H)-one | |
0.026 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-chloro-2-phenylpyridazin-3(2H)-one | |
0.026 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | (2E)-3-(pyridin-3-yl)-1-(pyridin-4-yl)prop-2-en-1-one | |
0.027 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 2-hydroxy-4-[(naphthalen-1-ylsulfonyl)amino]benzoic acid | |
0.055 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 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 | |
0.5 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 2-(5-bromo-6-oxo-1-phenyl-1,6-dihydropyridazin-4-yl)-1,2,3,4-tetrahydroisoquinoline-5-carbonitrile | |
0.5 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-isopropyl-2-phenylpyridazin-3(2H)-one | |
0.5 | - |
pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 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 | |
1 | - |
above, pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 4-bromo-5-morpholino-2-phenylpyridazin-3(2H)-one | |
1 | - |
above, pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 4-bromo-2-phenyl-5-(2-oxa-6-azaspiro[3.3]heptan-6-yl)pyridazin-3(2H)-one | |
1 | - |
above, pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 2-((5-bromo-6-oxo-1-phenyl-1,6-dihydropyridazin-4-yl)amino)acetamide | |
1 | - |
above, pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 4-bromo-2-phenyl-5-(((tetrahydrofuran-2-yl)methyl)amino)pyridazin-3(2H)-one | |
1 | - |
above, pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-ethoxy-2-phenylpyridazin-3(2H)-one | |
1 | - |
above, pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 3H-benzo[e]indol-2-yl(pyridin-4-yl)methanone | |
10 | - |
above, pH 7.5, 30°C, recombinant GST-tagged enzyme | Homo sapiens | 5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-2-benzylpyridazin-3(2H)-one |
General Information | Comment | Organism |
---|---|---|
metabolism | cancer cells use control of PFKFB3 of the important glycolytic pathway to generate ATP | Homo sapiens |