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Literature summary extracted from

  • Hong, B.S.; Allali-Hassani, A.; Tempel, W.; Finerty, P.J.; Mackenzie, F.; Dimov, S.; Vedadi, M.; Park, H.W.
    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.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.7.1.32 medicine the enzyme is implicated in tumorigenesis and an attractive target for anticancer chemotherapy Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.1.32 expressed in Escherichia coli BL21(DE3) cells Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.7.1.32 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
2.7.1.32 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

EC Number Protein Variants Comment Organism
2.7.1.32 F352A the mutant exhibits a higher turnover number compared to the wild type enzyme Homo sapiens
2.7.1.32 F352L the mutant exhibits a higher turnover number compared to the wild type enzyme Homo sapiens
2.7.1.32 L401A the mutant of isoform ChoKalpha1 exhibts a lower turnover number compared to the wild type enzyme Homo sapiens
2.7.1.32 L401F the mutant of isoform ChoKalpha1 exhibts a lower turnover number compared to the wild type enzyme Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.32 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]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.1.32 0.021
-
 choline isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.033
-
 choline wild type isoform ChoKbeta, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.041
-
 choline isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.086
-
 choline wild type isoform ChoKalpha2, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.102
-
 choline isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.107
-
 choline isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.18
-
 choline wild type isoform ChoKalpha1, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.4
-
 ATP isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.4
-
 ATP wild type isoform ChoKalpha2, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.4
-
 ATP wild type isoform ChoKbeta, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.55
-
 ATP isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.65
-
 ATP isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.7
-
 ATP isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.76
-
 ATP wild type isoform ChoKalpha1, pH and temperature not specified in the publication Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.1.32 Mg2+ required Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.32 Homo sapiens P35790 subunit CKalpha
-
2.7.1.32 Homo sapiens Q9Y259 subunit CKbetha
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.1.32 HisTrap column chromatography and Superdex 200 gel filtration Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.32 ATP + choline
-
 Homo sapiens ADP + phosphocholine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.1.32 CHOKalpha1 isoform Homo sapiens
2.7.1.32 ChoKalpha2 isoform Homo sapiens
2.7.1.32 ChoKbeta1 isoform Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.7.1.32 2.92
-
 choline wild type isoform ChoKbeta, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 4.58
-
 choline isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 9.5
-
 choline isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 14
-
 choline isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 47.33
-
 choline wild type isoform ChoKalpha2, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 49.5
-
 choline isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 76.83
-
 choline wild type isoform ChoKalpha1, pH and temperature not specified in the publication Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.1.32 0.00021
-
 hemicholinium-3 wild type isoform ChoKalpha1, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.00023
-
 hemicholinium-3 wild type isoform ChoKalpha2, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.00045
-
 hemicholinium-3 isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.005
-
 hemicholinium-3 isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.008
-
 hemicholinium-3 isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.016
-
 hemicholinium-3 isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication Homo sapiens
2.7.1.32 0.116
-
 hemicholinium-3 wild type isoform ChoKbeta, pH and temperature not specified in the publication Homo sapiens