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Literature summary for 2.7.1.105 extracted from
- Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer (2013), Mol. Cancer Ther., 12, 1461-1470.
Inhibitors
| 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
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | required | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| 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
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q16875 | gene/isozyme PFKFB3 | - |
Source Tissue
| 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 and Products (Substrate)
| 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
| Synonyms | Comment | Organism |
|---|---|---|
| 6-phosphofructo-2-kinase | - |
Homo sapiens |
| PFKFB3 | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 22 | - |
assay at room temperature | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 8 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
General Information
| 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 |
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