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2.7.1.105: 6-phosphofructo-2-kinase

This is an abbreviated version!
For detailed information about 6-phosphofructo-2-kinase, go to the full flat file.

Word Map on EC 2.7.1.105

Reaction

ATP
+
beta-D-fructose 6-phosphate
=
ADP
 +
beta-D-fructose 2,6-bisphosphate

Synonyms

6-phosphofructo 2-kinase/fructose 2,6-bisphosphatase-2, 6-phosphofructo kinase-2/fructose diphosphatase-2 isoenzyme 3, 6-phosphofructo-2-kinase, 6-phosphofructo-2-kinase/2,6-bisphosphatase 3, 6-phosphofructo-2-kinase/fructose 2,6-bisphosphatase, 6-phosphofructo-2-kinase/fructose-2, 6-bisphosphatase, 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase, 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4, 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase-3, 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase:glucokinase complex, 6-phosphofructose 2-kinase, 6PF2K/Fru-2,6-P2ase, ATP:D-fructose-6-phosphate 2-phosphotransferase, fructose 6-phosphate 2-kinase, inducible 6-phosphofructo-2-kinase, iPFK2, kinase, 6-phosphofructo-2-(phosphorylating), OsF2KP1, OsF2KP2, Pfk-2, PFK-2/FBPase, PFK-2/FBPase-2, PFK2, PFK2/FBPase2, PFKFB, PFKFB-3, PFKFB1, PFKFB2, PFKFB3, PFKFB4, phosphofructokinase 2, phosphofructokinase-2, phosphofructokinase-2/fructose bisphosphatase-2, T-PFK2, tPFK-2, uPFK-2

ECTree

     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.1 Phosphotransferases with an alcohol group as acceptor
                2.7.1.105 6-phosphofructo-2-kinase

Inhibitors

Inhibitors on EC 2.7.1.105 - 6-phosphofructo-2-kinase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2E)-1-(pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one
-
(2E)-3-(pyridin-3-yl)-1-(pyridin-4-yl)prop-2-en-1-one
-
1-(3-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one
1-(4-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one
2,5-anhydro-D-mannitol 6-phosphate
-
-
2-((5-bromo-6-oxo-1-phenyl-1,6-dihydropyridazin-4-yl)amino)acetamide
-
2-(2-bromoacetamido)ethyl phosphate
an irreversible inhibitor of PFK-2 in several cancer cell lines
2-(5-bromo-6-oxo-1-phenyl-1,6-dihydropyridazin-4-yl)-1,2,3,4-tetrahydroisoquinoline-5-carbonitrile
-
2-hydroxy-4-[(naphthalen-1-ylsulfonyl)amino]benzoic acid
-
3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
3-phosphoglycerate
-
3H-benzo[e]indol-2-yl(pyridin-4-yl)methanone
-
4-(4-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-5-bromo-6-oxopyridazin-1(6H)-yl)benzonitrile
-
4-bromo-2-phenyl-5-(((tetrahydrofuran-2-yl)methyl)amino)pyridazin-3(2H)-one
-
4-bromo-2-phenyl-5-(2-oxa-6-azaspiro[3.3]heptan-6-yl)pyridazin-3(2H)-one
-
4-bromo-5-morpholino-2-phenylpyridazin-3(2H)-one
-
5,6,7,8-tetrahydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
-
5,6,7,8-tetrahydroxy-2-(4-hydroxyphenyl)chromen-4-one
-
-
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-2-benzyl-4-bromopyridazin-3(2H)-one
-
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-2-benzylpyridazin-3(2H)-one
-
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(3-phenylpropyl)pyridazin-3(2H)-one
-
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
-
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-(trifluoromethoxy)phenyl)-pyridazin-3(2H)-one
-
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-chlorophenyl)pyridazin-3(2H)-one
-
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(4-iodobenzyl)pyridazin-3(2H)-one
-
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-(pyrimidin-5-yl)pyridazin-3(2H)-one
-
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-phenethylpyridazin-3(2H)-one
-
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-bromo-2-phenylpyridazin-3(2H)-one
-
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-chloro-2-phenylpyridazin-3(2H)-one
-
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-ethoxy-2-phenylpyridazin-3(2H)-one
-
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-iodo-2-phenylpyridazin-3(2H)-one
-
5-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-4-isopropyl-2-phenylpyridazin-3(2H)-one
-
5-(N-(8-methoxy-4-quinolyl)amino)pentyl nitrate
-
-
5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside
AICAR, associated with phosphorylation of PFK-2 on Ser-32, phosphorylation increased of both wild-type and overexpressed PFK-2 protein in hepatocytes
7,8-dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one
-
-
7,8-dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one
-
AZ67
potent and specific PFKFB3 inhibitor
-
beta-D-fructose 2,6-bisphosphate
beta-D-fructose 6-phosphate
modeling of beta-D-fructose 6-phosphate as inhibitor
citrate
dibutyryl cAMP
slightly inhibits the complex formation between the enzyme and glucokinase
dihydroxyacetone phosphate
diphosphate
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
-
ethyl 7-hydroxy-2-oxo-2H-1-benzopyran-3-carboxylate
-
-
glucagon
glycerate 2-phosphate
Glycerol 2-phosphate
-
-
glycerol 3-phosphate
20% inhibition at 2mM
glycolate 2-phosphate
-
-
guanidine
-
inactivation, unfolding
m-periodate
-
strong, DTT protects or reverses
Mg2+
-
MgATP
MgATP
-
inhibited by, structure determination reveals substrate inhibition due to sequential binding of two MgATP molecules per subunit, the first at the usual site occupied by the nucleotide in homologous enzymes and the second at the allosteric site, making a number of direct and Mg-mediated interactions with the first, two configurations observed for the second MgATP, one of which involves interactions with Tyr-23 from the adjacent subunit in the dimer and the other making an unusual non-Watson-Crick base pairing with the adenine in the substrate ATP
MgATP2-
MgNTP
-
strain DF903, substrate inhibition, most effective: MgATP2, at low fructose concentration
N-(1-pyrenil)maleimide
-
complete loss of catalytic activity, but modified enzyme is able to bind beta-D-fructose 6-phosphate, the presence of MgATP2- completely protects the enzyme activity, the modified enzyme elutes as a monomer
N-bromoacetylethanolamine
N-bromoacetylethanolamine phosphate
-
o-phthalaldehyde
-
kinetics, DTT or substrates do not protect
PFK-15
i.e. 1-(4-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one
-
PFK-158
potent and specific inhibitor
-
phosphate
-
inhibits wild-type and mutant enzym E190Q. E190 contributs to the mechanism of phosphate inhibition in Pfk-2. E190Q mutant presents alterations in the inhibition by MgATP2- and phosphate
phosphoenolpyruvate
protein kinase A
inactivation via a 7fold increase in Km for fructose 6-phosphate without alteration of Vmax
-
pyrene maleimide
-
incorporation of 2 mol per mol of enzyme subunit, modifiying Cys-238 and Cys-295, leads to rapid inactivation, MgATP2- protects Cys295, modification of Cys238 does not abolish activity
sn-glycerol 3-phosphate
additional information
-