Application | Comment | Organism |
---|---|---|
medicine | clinical development of PFKFB3 inhibitors as chemotherapeutic agents | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
subcloned into the pET-30b(+) vector, expression in BL21 (DE3) Escherichia coli | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
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 | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.097 | - |
beta-D-fructose 6-phosphate | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + beta-D-fructose 6-phosphate | Homo sapiens | PFKFB3 is a potent stimulator of glycolysis, up-regulated by inflammatory and hypoxic stimuli | ADP + beta-D-fructose 2,6-bisphosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q16875 | - |
- |
Purification (Comment) | Organism |
---|---|
gel filtration, recombinant protein | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
JURKAT cell | engineered to overexpress PFKFB3, inhibitor studies on recombinant PFKFB3 activity in | Homo sapiens | - |
leukemia cell | constitutively expressed in | Homo sapiens | - |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
0.277 | - |
specific PFK-2 activity of the recombinant PFKFB3 protein determined by measurement of fructose 2,6-bisphosphate | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + beta-D-fructose 6-phosphate | PFKFB3 is a potent stimulator of glycolysis, up-regulated by inflammatory and hypoxic stimuli | Homo sapiens | ADP + beta-D-fructose 2,6-bisphosphate | - |
? | |
ATP + beta-D-fructose 6-phosphate | PFKFB3 is a potent stimulator of glycolysis, up-regulated by inflammatory and hypoxic stimuli, role in the progression of cancerous cells, antiproliferative effects during inhibitor incubation determined | Homo sapiens | ADP + beta-D-fructose 2,6-bisphosphate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
PFKFB3 | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.025 | - |
3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one | inhibition of recombinant PFKFB3 protein, no inhibition of purified PFK-1 activity | Homo sapiens |