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Literature summary for 2.7.1.32 extracted from
- Crystal structures of human choline kinase isoforms in complex with hemicholinium-3: single amino acid near the active site influences inhibitor sensitivity (2010), J. Biol. Chem., 285, 16330-16340.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | the enzyme is implicated in tumorigenesis and an attractive target for anticancer chemotherapy | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in Escherichia coli BL21(DE3) cells | Homo sapiens |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| isoform ChoKalpha1 in complex with hemicholinium-3 and ADP, sitting drop vapor diffusion method, using 0.1 M HEPES (pH 7.5), 25% (w/v) polyethylene glycol 3350, and 0.2 M lithium sulfate | Homo sapiens |
| isoform ChoKbeta in complex with hemicholinium-3 and ADP, sitting drop vapor diffusion method, using 0.1 M sodium cacodylate (pH 6.5), 30% polyethylene glycol 4000, and 0.2 M ammonium sulfate | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| F352A | the mutant exhibits a higher turnover number compared to the wild type enzyme | Homo sapiens |
| F352L | the mutant exhibits a higher turnover number compared to the wild type enzyme | Homo sapiens |
| L401A | the mutant of isoform ChoKalpha1 exhibts a lower turnover number compared to the wild type enzyme | Homo sapiens |
| L401F | the mutant of isoform ChoKalpha1 exhibts a lower turnover number compared to the wild type enzyme | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| hemicholinium-3 | competitive inhibitor, the inhibitory effect of hemicholinium-3 is about 500times higher toward the ChoKalpha isoforms than ChoKbeta isoform; competitive inhibitor, the inhibitory effect of hemicholinium-3 is about 500times higher toward the ChoKalpha isoforms than ChoKbeta isoform | Homo sapiens |  |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.021 | - |
choline | isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication | Homo sapiens | |
| 0.033 | - |
choline | wild type isoform ChoKbeta, pH and temperature not specified in the publication | Homo sapiens | |
| 0.041 | - |
choline | isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication | Homo sapiens | |
| 0.086 | - |
choline | wild type isoform ChoKalpha2, pH and temperature not specified in the publication | Homo sapiens | |
| 0.102 | - |
choline | isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication | Homo sapiens | |
| 0.107 | - |
choline | isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication | Homo sapiens | |
| 0.18 | - |
choline | wild type isoform ChoKalpha1, pH and temperature not specified in the publication | Homo sapiens | |
| 0.4 | - |
ATP | isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication | Homo sapiens | |
| 0.4 | - |
ATP | wild type isoform ChoKalpha2, pH and temperature not specified in the publication | Homo sapiens | |
| 0.4 | - |
ATP | wild type isoform ChoKbeta, pH and temperature not specified in the publication | Homo sapiens | |
| 0.55 | - |
ATP | isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication | Homo sapiens | |
| 0.65 | - |
ATP | isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication | Homo sapiens | |
| 0.7 | - |
ATP | isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication | Homo sapiens | |
| 0.76 | - |
ATP | wild type isoform ChoKalpha1, pH and temperature not specified in the publication | Homo sapiens | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | required | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P35790 | subunit CKalpha | - |
| Homo sapiens | Q9Y259 | subunit CKbetha | - |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| HisTrap column chromatography and Superdex 200 gel filtration | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + choline | - |
Homo sapiens | ADP + phosphocholine | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| CHOKalpha1 | isoform | Homo sapiens |
| ChoKalpha2 | isoform | Homo sapiens |
| ChoKbeta1 | isoform | Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 2.92 | - |
choline | wild type isoform ChoKbeta, pH and temperature not specified in the publication | Homo sapiens | |
| 4.58 | - |
choline | isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication | Homo sapiens | |
| 9.5 | - |
choline | isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication | Homo sapiens | |
| 14 | - |
choline | isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication | Homo sapiens | |
| 47.33 | - |
choline | wild type isoform ChoKalpha2, pH and temperature not specified in the publication | Homo sapiens | |
| 49.5 | - |
choline | isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication | Homo sapiens | |
| 76.83 | - |
choline | wild type isoform ChoKalpha1, pH and temperature not specified in the publication | Homo sapiens | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00021 | - |
hemicholinium-3 | wild type isoform ChoKalpha1, pH and temperature not specified in the publication | Homo sapiens | |
| 0.00023 | - |
hemicholinium-3 | wild type isoform ChoKalpha2, pH and temperature not specified in the publication | Homo sapiens | |
| 0.00045 | - |
hemicholinium-3 | isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication | Homo sapiens | |
| 0.005 | - |
hemicholinium-3 | isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication | Homo sapiens | |
| 0.008 | - |
hemicholinium-3 | isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication | Homo sapiens | |
| 0.016 | - |
hemicholinium-3 | isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication | Homo sapiens | |
| 0.116 | - |
hemicholinium-3 | wild type isoform ChoKbeta, pH and temperature not specified in the publication | Homo sapiens | |
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