Inhibitors | Comment | Organism | Structure |
---|---|---|---|
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | 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 | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
BxPC-3 cell | - |
Homo sapiens | - |
colon adenocarcinoma cell | - |
Homo sapiens | - |
CT26 cell | - |
Homo sapiens | - |
glioblastoma cell | - |
Homo sapiens | - |
H-522 cell | - |
Homo sapiens | - |
JURKAT cell | - |
Homo sapiens | - |
leukemia cell | - |
Homo sapiens | - |
Lewis lung carcinoma cell | - |
Homo sapiens | - |
lung adenocarcinoma cell | - |
Homo sapiens | - |
pancreatic cancer cell | - |
Homo sapiens | - |
U-87 cell | - |
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 | - |
Homo sapiens |
PFKFB3 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
22 | - |
assay at room temperature | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
8 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
General Information | Comment | Organism |
---|---|---|
physiological function | in human cancers, loss of PTEN, stabilization of HIF-1alpha and activation of Ras and AKT converge to increase the activity of a key regulator of glycolysis, 6-phosphofructo-2-kinase(PFKFB3). This enzyme synthesizes fructose 2,6-bisphosphate, which is an activator of 6-phosphofructo-1-kinase, a key step of glycolysis | Homo sapiens |