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Literature summary for 2.7.1.32 extracted from
- Choline kinase: an important target for cancer (2006), Curr. Med. Chem., 13, 1169-1186.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | target in anti-cancer therapy | Homo sapiens |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
- |
Saccharomyces cerevisiae |
- |
Schizosaccharomyces pombe |
- |
Caenorhabditis elegans |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| D255A | complete loss of activity | Homo sapiens |
| E125A | 2-25% catalytic efficiency compared to the wild type enzyme | Homo sapiens |
| E125A | modest change in kcat/Km with a marked decrease in the affinity for Ca2+ and a significant increase in Km for Mg2+ | Homo sapiens |
| E255A | almost complete loss of activity | Homo sapiens |
| E303A | 10fold decrease in activity | Homo sapiens |
| E320A | 26fold higher Km for ATP | Homo sapiens |
| N255A | complete loss of activity | Homo sapiens |
| R111A | 2-25% catalytic efficiency compared to the wild type enzyme | Homo sapiens |
| S86A | 2-25% catalytic efficiency compared to the wild type enzyme | Homo sapiens |
| W387A | 2-25% catalytic efficiency compared to the wild type enzyme | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 4'-bispyridyl-5,5'-perfluoroalkyl-2,2'-bisoxazol | - |
Homo sapiens | |
| 5'-dithio-bis-(2-nitrobenzoic acid) | modest inhibitory activity | Homo sapiens |  |
| choline | - |
Homo sapiens | |
| cyclophane | - |
Homo sapiens | |
| hemicholinium | - |
Homo sapiens | |
| hemicholinium-3 | weak inhibitor, IC50: 0.057 mM | Homo sapiens | |
| N-ethylmaleimide | modest inhibitory activity | Homo sapiens | |
| N-[2-bromocinnamyl(amino)ethyl]-5-isoquinoline sulfonamide | - |
Homo sapiens | |
| piperazine | modest inhibitory activity | Homo sapiens | |
| purinyl-6-histamine | modest inhibitory activity | Homo sapiens | |
| Quinacrine | indirect inhibitor | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytosol | - |
Mus musculus | 5829 | - |
| cytosol | - |
Homo sapiens | 5829 | - |
| cytosol | - |
Rattus norvegicus | 5829 | - |
| cytosol | - |
Saccharomyces cerevisiae | 5829 | - |
| cytosol | - |
Schizosaccharomyces pombe | 5829 | - |
| cytosol | - |
Caenorhabditis elegans | 5829 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Ca2+ | required | Mus musculus | |
| Ca2+ | required | Homo sapiens | |
| Ca2+ | required | Rattus norvegicus | |
| Ca2+ | required | Saccharomyces cerevisiae | |
| Ca2+ | required | Schizosaccharomyces pombe | |
| Ca2+ | required | Caenorhabditis elegans | |
| Mg2+ | required | Mus musculus | |
| Mg2+ | required | Homo sapiens | |
| Mg2+ | required | Rattus norvegicus | |
| Mg2+ | required | Saccharomyces cerevisiae | |
| Mg2+ | required | Schizosaccharomyces pombe | |
| Mg2+ | required | Caenorhabditis elegans | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 12750 | - |
4 * 12750 | Rattus norvegicus |
| 13000 | - |
4 * 13000 | Mus musculus |
| 42000 | - |
- |
Caenorhabditis elegans |
| 51000 | - |
- |
Rattus norvegicus |
| 52000 | - |
- |
Mus musculus |
| 52000 | - |
CHKA | Homo sapiens |
| 52000 | - |
1 * 52000 | Schizosaccharomyces pombe |
| 66000 | - |
1 * 66000 | Saccharomyces cerevisiae |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Caenorhabditis elegans | - |
- |
- |
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
| Rattus norvegicus | - |
- |
- |
| Saccharomyces cerevisiae | - |
- |
- |
| Schizosaccharomyces pombe | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| brain | - |
Rattus norvegicus | - |
| breast | - |
Homo sapiens | - |
| colon | - |
Homo sapiens | - |
| kidney | - |
Rattus norvegicus | - |
| liver | - |
Rattus norvegicus | - |
| lung | - |
Homo sapiens | - |
| lung | - |
Rattus norvegicus | - |
| lymphoma cell | - |
Homo sapiens | - |
| neuroblastoma cell | - |
Homo sapiens | - |
| prostate | - |
Homo sapiens | - |
| testis | - |
Mus musculus | - |
| testis | - |
Homo sapiens | - |
| testis | - |
Rattus norvegicus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + choline | - |
Mus musculus | ADP + O-phosphocholine | - |
? | |
| ATP + choline | - |
Homo sapiens | ADP + O-phosphocholine | - |
? | |
| ATP + choline | - |
Rattus norvegicus | ADP + O-phosphocholine | - |
? | |
| ATP + choline | - |
Saccharomyces cerevisiae | ADP + O-phosphocholine | - |
? | |
| ATP + choline | - |
Schizosaccharomyces pombe | ADP + O-phosphocholine | - |
? | |
| ATP + choline | - |
Caenorhabditis elegans | ADP + O-phosphocholine | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| homotetramer | - |
Homo sapiens |
| homotetramer | 4 * 12750 | Rattus norvegicus |
| homotetramer | 4 * 13000 | Mus musculus |
| monomer | 1 * 66000 | Saccharomyces cerevisiae |
| monomer | 1 * 52000 | Schizosaccharomyces pombe |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Chka | - |
Mus musculus |
| Chka | - |
Homo sapiens |
| Chka | - |
Rattus norvegicus |
| ChoK | - |
Mus musculus |
| ChoK | - |
Homo sapiens |
| ChoK | - |
Rattus norvegicus |
| choline kinase alpa | - |
Homo sapiens |
| choline kinase alpha | - |
Mus musculus |
| choline kinase alpha | - |
Rattus norvegicus |
| ckb | - |
Caenorhabditis elegans |
| CKII | - |
Saccharomyces cerevisiae |
| putative choline kinase | - |
Schizosaccharomyces pombe |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 8 | 9.5 | - |
Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Mus musculus | |
| ATP | - |
Homo sapiens | |
| ATP | - |
Rattus norvegicus | |
| ATP | - |
Saccharomyces cerevisiae | |
| ATP | - |
Schizosaccharomyces pombe | |
| ATP | - |
Caenorhabditis elegans | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.057 | - |
weak inhibitor, IC50: 0.057 mM | Homo sapiens | hemicholinium-3 | |
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Release 2023.1 (January 2023)
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