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(2E)-1-(pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one
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(2E)-3-(pyridin-3-yl)-1-(pyridin-4-yl)prop-2-en-1-one
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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
-
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2-((5-bromo-6-oxo-1-phenyl-1,6-dihydropyridazin-4-yl)amino)acetamide
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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
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2-hydroxy-4-[(naphthalen-1-ylsulfonyl)amino]benzoic acid
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3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
3H-benzo[e]indol-2-yl(pyridin-4-yl)methanone
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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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5,6,7,8-tetrahydroxy-2-(4-hydroxyphenyl)chromen-4-one
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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-(N-(8-methoxy-4-quinolyl)amino)pentyl nitrate
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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
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7,8-dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one
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AZ67
potent and specific PFKFB3 inhibitor
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beta-D-fructose 2,6-bisphosphate
beta-D-fructose 6-phosphate
modeling of beta-D-fructose 6-phosphate as inhibitor
dibutyryl cAMP
slightly inhibits the complex formation between the enzyme and glucokinase
dihydroxyacetone phosphate
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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ethyl 7-hydroxy-2-oxo-2H-1-benzopyran-3-carboxylate
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glycerol 3-phosphate
20% inhibition at 2mM
glycolate 2-phosphate
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guanidine
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inactivation, unfolding
m-periodate
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strong, DTT protects or reverses
MgATP
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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
MgNTP
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strain DF903, substrate inhibition, most effective: MgATP2, at low fructose concentration
N-(1-pyrenil)maleimide
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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
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o-phthalaldehyde
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kinetics, DTT or substrates do not protect
PFK-15
i.e. 1-(4-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one
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PFK-158
potent and specific inhibitor
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phosphate
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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
protein kinase A
inactivation via a 7fold increase in Km for fructose 6-phosphate without alteration of Vmax
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pyrene maleimide
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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
1-(3-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one
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1-(3-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one
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1-(4-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one
the inhibitor causes a rapid induction of apoptosis in transformed cells, has adequate pharmacokinetic properties, suppresses the glucose uptake and growth of Lewis lung carcinomas in syngeneic mice and yields anti-tumor effects in three human xenograft models of cancer in athymic mice that are comparable to FDA-approved chemotherapeutic agents
1-(4-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one
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3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
(3PO), small-molecule inhibitor, mixed inhibition mechanism, both competitive and uncompetitive inhibition, suppresses glycolytic flux and is cytostatic to neoplastic cells, inhibits activity of recombinantly expressed PFKFB3
3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
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3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
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3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
the PFKFB3 inhibitor, 3PO, increases p27 protein in Lewis lung carcinoma cells in vitro and in vivo
3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
3PO, a weak competitive inhibitor of PFKFB3, reduces the glucose metabolism and proliferation of cancer cells
3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
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ADP
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AMP
not
ATP
not
ATP
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at low concentrations of Mg2+ and fructose 6-phosphate
beta-D-fructose 2,6-bisphosphate
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product inhibition
beta-D-fructose 2,6-bisphosphate
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kinetics
beta-D-fructose 2,6-bisphosphate
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citrate
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weak
citrate
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heart enzyme is more sensitive than liver enzyme
citrate
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at physiological concentrations
citrate
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skeletal muscle enzyme is more sensitive than liver enzyme
citrate
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heart enzyme is more sensitive than liver enzyme
citrate
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skeletal muscle enzyme is more sensitive than liver enzyme
citrate
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phosphorylation enhances sensitivity
citrate
60% inhibition at 1 mM
dihydroxyacetone phosphate
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dihydroxyacetone phosphate
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weak
dihydroxyacetone phosphate
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diphosphate
not phosphate
diphosphate
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not phosphate
diphosphate
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not phosphate
diphosphate
not phosphate
glucagon
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the native and the recombinant wild-type and mutant enzymes are phosphorylated after incubation with glucagon inactivating the enzyme
glucagon
phosphorylation of PFK2 on Ser-32 in liver
glycerate 2-phosphate
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glycerate 2-phosphate
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MgATP2-
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allosteric inhibition, important regulation of in vivo carbohydrate metabolism under gluconeogenic conditions
MgATP2-
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E190Q mutant presents alterations in the inhibition by MgATP2- and phosphate
MgATP2-
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allosteric inhibition
N-bromoacetylethanolamine
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repetitive administration affects inhibition of glycolysis and lipid metabolism, causing suppression of body weight gain
N-bromoacetylethanolamine
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specific active site-directed inactivator of enzyme, in vitro and in vivo
phosphoenolpyruvate
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phosphoenolpyruvate
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weak
phosphoenolpyruvate
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not
phosphoenolpyruvate
HBP1 and HBP2, the bifunctional enzyme is regulated via inhibition by phosphoenolpyruvate, uncompetitive against ATP, noncompetitive against beta-D-fructose 6-phosphate
phosphoenolpyruvate
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strong
phosphoenolpyruvate
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kinetics
phosphoenolpyruvate
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mixed-type inhibitory effect, phosphorylation enhances sensitivity
sn-glycerol 3-phosphate
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sn-glycerol 3-phosphate
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heart enzyme is less sensitive than liver
sn-glycerol 3-phosphate
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i.e. alpha-glycerol phosphate
sn-glycerol 3-phosphate
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not
sn-glycerol 3-phosphate
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heart enzyme is less sensitive than liver
sn-glycerol 3-phosphate
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not
sn-glycerol 3-phosphate
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sn-glycerol 3-phosphate
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stimulates phosphatase activity
sn-glycerol 3-phosphate
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heart enzyme is less sensitive than liver
sn-glycerol 3-phosphate
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sn-glycerol 3-phosphate
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heart enzyme is less sensitive than liver; liver enzyme
sn-glycerol 3-phosphate
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75% decrease in activity of liver enzyme but not hepatoma cells
sn-glycerol 3-phosphate
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most potent inhibitor of phosphorylated liver enzyme, phosphorylation enhances sensitivity
sn-glycerol 3-phosphate
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most potent inhibitor of phosphorylated liver enzyme, phosphorylation enhances sensitivity; skeletal muscle enzyme is not sensitive to inhibition
sn-glycerol 3-phosphate
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sn-glycerol 3-phosphate
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additional information
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no inhibition by protein kinase C; phosphorylation by cAMP-dependent protein kinase, but no inhibition
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme; rat liver enzyme is inhibited by phosphorylation by cAMP-dependent protein kinase, but not rat skeletal muscle, bovine and rat heart enzyme
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additional information
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no inhibition by protein kinase C; phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme; rat liver enzyme is inhibited by phosphorylation by cAMP-dependent protein kinase but not rat kidney, testis and skeletal muscle enzyme and bovine and rat heart enzyme
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme
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additional information
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-
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additional information
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no inhibition by protein kinase C; phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme
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additional information
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not: ITP, GTP, UTP, CTP, strain DF905; phosphorylation by cAMP-dependent protein kinase causes inactivation
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme
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additional information
phosphorylation site: Ser-32
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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
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additional information
synthesis and screening of 3PO inhibitor derivatives for inhibitory potency against isozyme PFKFB3, overview. 1-(4-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one displays improved pharmacokinetic properties relative to 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
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additional information
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synthesis and screening of 3PO inhibitor derivatives for inhibitory potency against isozyme PFKFB3, overview. 1-(4-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one displays improved pharmacokinetic properties relative to 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
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additional information
not inhibited by up to 0.75 mM 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
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additional information
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no inhibition by phosphorylation with Ca2+/calmodulin dependent protein kinase; no inhibition by protein kinase C
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme
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additional information
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phosphorylation at lower pH-values; phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme
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additional information
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phosphorylation site: Ser-32
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme; phosphorylation of foetal liver enzyme by protein kinase C, but no effect on adult liver cells
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additional information
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not: cAMP or protein kinase alone; phosphorylation at pH 6.6, not at pH 8; phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme; phosphorylation by cAMP-dependent protein kinase of liver enzyme, not of skeletal muscle enzyme, since the phosphorylation site target Ser-32 of the liver isozyme is replaced by Ala in the muscle isozyme
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme; rat liver enzyme is inhibited by phosphorylation by cAMP-dependent protein kinase, but not rat skeletal muscle, bovine and rat heart enzyme
-
additional information
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no inhibition by protein kinase C; phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme; rat liver enzyme is inhibited by phosphorylation by cAMP-dependent protein kinase but not rat kidney, testis and skeletal muscle enzyme and bovine and rat heart enzyme
-
additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme; phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme, not of heart and skeletal muscle enzyme
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additional information
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loss of phosphorylation-dependent reduction of enzyme by deletion of the N-terminal residues of enzyme. The deletion of 7 N-terminal amino acids causes a 75% decrease in activity; phosphorylation site: Ser-32
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme
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additional information
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phosphorylation by cAMP-dependent protein kinase causes 35% inactivation of isozyme L of adipose tissue, not isozyme M
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additional information
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kinetic of phosphorylation by cAMP-dependent protein kinase
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additional information
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phosphorylation by cAMP-dependent protein kinase causes 80% decrease in activity of the liver cells but not of hepatoma cells; phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme; phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme, not of kidney, testis and heart enzyme
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additional information
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the islet enzyme lacks protein kinase A and C phosphorylation sites
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additional information
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phosphorylation by cAMP-dependent protein kinase, but no inhibition
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additional information
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no inhibition by lactate, glyceraldehyde 3-phosphate, beta-D-fructose 1,6-bisphosphate
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additional information
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phosphorylation by cAMP-dependent protein kinase causes inactivation of liver enzyme, not skeletal muscle enzyme
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additional information
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-
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additional information
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-
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additional information
enzyme is not affected by protein kinase C
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additional information
enzyme is not affected by protein kinase C
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additional information
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enzyme is not affected by protein kinase C
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