Cloned (Comment) | Organism |
---|---|
expression of His6-tagged isozymes in Escherichia coli | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
4-amino-2-methylnaphthalen-1-ol | i.e. vitamin K5, shows a significantly stronger potency to inhibit isozyme PKM2 than to inhibit isozymes PKM1 and PKL | Homo sapiens | |
menadione | i.e. vitamin K3, shows a significantly stronger potency to inhibit isozyme PKM2 than to inhibit isozymes PKM1 and PKL | Homo sapiens | |
additional information | D-fructose 1,6-bisphosphate diminishes the inhibitory effects of vitamin K derivatives. No inhibition of isozyme PKM2 by vitamin K1 and vitamin K2 | Homo sapiens | |
N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrrole | a PKM2 inhibitor | Homo sapiens | |
shikonin | a PKM2 inhibitor | 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 + pyruvate | Homo sapiens | - |
ADP + phosphoenolpyruvate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
recombinant His6-tagged isozymes from Escherichia coli by nickel affinity chromatgraphy | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
HeLa cell | Hela cells express PKM2 but not PKM1 or PKL | Homo sapiens | - |
liver | isozyme PKL | Homo sapiens | - |
additional information | isozyme PKM1 is expressed in most adult tissues | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + pyruvate | - |
Homo sapiens | ADP + phosphoenolpyruvate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
PKL | - |
Homo sapiens |
PKM1 | - |
Homo sapiens |
PKM2 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.028 | - |
pH 7.5, 25°C, recombinant His6-tagged isozyme PKM2, in absence of D-fructose 1,6-bisphosphate | Homo sapiens | 4-amino-2-methylnaphthalen-1-ol | |
0.045 | - |
pH 7.5, 25°C, recombinant His6-tagged isozyme PKM2, in presence of D-fructose 1,6-bisphosphate | Homo sapiens | 4-amino-2-methylnaphthalen-1-ol | |
0.0593 | - |
pH 7.5, 25°C, recombinant His6-tagged isozyme PKM2, in absence of D-fructose 1,6-bisphosphate | Homo sapiens | N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrrole | |
0.0775 | - |
pH 7.5, 25°C, recombinant His6-tagged isozyme PKM2, in presence of D-fructose 1,6-bisphosphate | Homo sapiens | N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrrole | |
0.12 | - |
pH 7.5, 25°C, recombinant His6-tagged isozyme PKL, in absence of D-fructose 1,6-bisphosphate | Homo sapiens | 4-amino-2-methylnaphthalen-1-ol | |
0.15 | - |
pH 7.5, 25°C, recombinant His6-tagged isozyme PKM2, in absence of D-fructose 1,6-bisphosphate | Homo sapiens | menadione | |
0.191 | - |
pH 7.5, 25°C, recombinant His6-tagged isozyme PKM1, in absence of D-fructose 1,6-bisphosphate | Homo sapiens | 4-amino-2-methylnaphthalen-1-ol | |
0.381 | - |
pH 7.5, 25°C, recombinant His6-tagged isozyme PKM2, in presence of D-fructose 1,6-bisphosphate | Homo sapiens | menadione | |
0.837 | - |
pH 7.5, 25°C, recombinant His6-tagged isozyme PKL, in absence of D-fructose 1,6-bisphosphate | Homo sapiens | menadione | |
3.407 | - |
pH 7.5, 25°C, recombinant His6-tagged isozyme PKM1, in absence of D-fructose 1,6-bisphosphate | Homo sapiens | menadione |
General Information | Comment | Organism |
---|---|---|
malfunction | consequence of PKM2 inhibition is a reduced glycolytic flux, which can be reflected by the rates of cellular glucose consumption and lactate production | Homo sapiens |
physiological function | pyruvate kinase isozyme PKM2 is a rate-limiting enzyme of aerobic glycolysis in cancer cells and plays important roles in cancer metabolism and growth. Vitamin K3/vitamin K5-enhanced toxicity of doxorubicin is associated with pyruvate kinase activity | Homo sapiens |