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Literature summary for 2.7.11.1 extracted from
- Too much of a good thing: The role of protein kinase CK2 in tumorigenesis and prospects for therapeutic inhibition of CK2 (2008), Biochim. Biophys. Acta, 1784, 33-47.
Application
| Application | Comment | Organism |
|---|---|---|
| pharmacology | CK2 is a potential therapeutic target and a target for inhibitor design, e.g. in anti-cancer therapy | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| targeted overexpression of both CK2 and either c-Myc or Tal-1 in T-cells, as well as in tumor suppressor p53 (-/-) mice or murine BALB/c 3T3 fibroblasts | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| additional information | targeted overexpression of both CK2 and either c-Myc or Tal-1 in T-cells, as well as the overexpression of CK2 in tumor suppressor p53 (-/-) mice, results in an increase in oncogenic activity and progression of tumorigenesis, a cooperative increase in oncogenic activity is also observed in BALB/c 3T3 fibroblasts co-expressing H-Ras and CK2alpha', overview, knockdown studies of CK2 using RNAi shows that CK2 negatively regulate apoptosis in IR damage and affects the cell cycle progression in HeLa cells | Homo sapiens |
| V66A/I174A | site-directed mutagenesis, an engineered TBB inhibitor-resistant CK2 mutant CK2alpha'R | Homo sapiens |
| V67A/I175A | site-directed mutagenesis, an inhibitor-resistant CK2 mutant CK2alpha'R | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (5-oxo-5,6-dihydroindolo[1,2-a]quinazolin-7-yl)acetic acid | i.e. IQA | Homo sapiens |  |
| 2-dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole | i.e. DMAT | Homo sapiens | |
| 4,5,6,7-tetrabromo-1H-benzotriazole | i.e. TBB | Homo sapiens | |
| 4,5,6,7-tetrabromobenzimidazole | i.e. TBBz or TBI | Homo sapiens | |
| apigenin | - |
Homo sapiens | |
| DRB | - |
Homo sapiens | |
| ellagic acid | - |
Homo sapiens | |
| emodin | - |
Homo sapiens | |
| additional information | in vivo inhibition strategies in the mouse model, validation of CK2 targets identification of bona fide targets, overview | Homo sapiens | |
| TBCA | - |
Homo sapiens | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + geminin | Homo sapiens | a cell cycle regulatory protein | ADP + phosphorylated geminin | - |
? | |
| ATP + M3-muscarnic receptor | Homo sapiens | - |
ADP + phosphorylated M3-muscarnic receptor | - |
? | |
| ATP + procaspase-2 | Homo sapiens | phosphorylation of procaspase-2 by CK2 prevents the activation of caspase activity by inhibiting the dimerization of procaspase-2, CK2 activity is involved in the direct regulation of the caspase-8 pathway, where it can control caspase-8 activity through the phosphorylation of ARC or by preventing the ability of caspase-8 to cleave its target Bid | ADP + phosphorylated procaspase-2 | - |
? | |
| additional information | Homo sapiens | CK2 plays a role in the protection of cells from apoptosis via the regulation of tumor suppressor and oncogene activity and stability, e.g. in the NF-kappaB or the Wnt signaling pathways, molecular mechanisms, detailed overview, CK2 activity is linked to Her-2/neu oncogene, which is overexpressed in 30% of breast cancers, regulation of apoptotic machinery by CK2 and its anti-apoptotic effect, overview, role of CK2 in chromosomal DNA strand break repair and the maintenance of genomic integrity, mutational study, overview | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| additional information | elevated CK2 activity occurs with the malignant transformation of several tissues and is associated with aggressive tumor behaviour | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + geminin | - |
Homo sapiens | ADP + phosphorylated geminin | - |
? | |
| ATP + geminin | a cell cycle regulatory protein | Homo sapiens | ADP + phosphorylated geminin | - |
? | |
| ATP + M3-muscarnic receptor | - |
Homo sapiens | ADP + phosphorylated M3-muscarnic receptor | - |
? | |
| ATP + procaspase-2 | - |
Homo sapiens | ADP + phosphorylated procaspase-2 | - |
? | |
| ATP + procaspase-2 | phosphorylation of procaspase-2 by CK2 prevents the activation of caspase activity by inhibiting the dimerization of procaspase-2, CK2 activity is involved in the direct regulation of the caspase-8 pathway, where it can control caspase-8 activity through the phosphorylation of ARC or by preventing the ability of caspase-8 to cleave its target Bid | Homo sapiens | ADP + phosphorylated procaspase-2 | - |
? | |
| additional information | CK2 plays a role in the protection of cells from apoptosis via the regulation of tumor suppressor and oncogene activity and stability, e.g. in the NF-kappaB or the Wnt signaling pathways, molecular mechanisms, detailed overview, CK2 activity is linked to Her-2/neu oncogene, which is overexpressed in 30% of breast cancers, regulation of apoptotic machinery by CK2 and its anti-apoptotic effect, overview, role of CK2 in chromosomal DNA strand break repair and the maintenance of genomic integrity, mutational study, overview | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| CK2 | - |
Homo sapiens |
| protein kinase CK2 | - |
Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00002 | - |
ellagic acid | - |
Homo sapiens | |
| 0.00004 | - |
2-dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole | - |
Homo sapiens | |
| 0.000077 | - |
TBCA | - |
Homo sapiens | |
| 0.00017 | - |
(5-oxo-5,6-dihydroindolo[1,2-a]quinazolin-7-yl)acetic acid | - |
Homo sapiens | |
| 0.0004 | - |
4,5,6,7-tetrabromo-1H-benzotriazole | - |
Homo sapiens | |
| 0.0007 | - |
4,5,6,7-tetrabromobenzimidazole | - |
Homo sapiens | |
| 0.00074 | - |
apigenin | - |
Homo sapiens | |
| 0.00185 | - |
emodin | - |
Homo sapiens | |
| 0.0045 | - |
DRB | - |
Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00004 | - |
- |
Homo sapiens | ellagic acid | |
| 0.00011 | - |
- |
Homo sapiens | TBCA | |
| 0.00014 | - |
- |
Homo sapiens | DMAT | |
| 0.00039 | - |
- |
Homo sapiens | IQA | |
| 0.0005 | - |
- |
Homo sapiens | TBB | |
| 0.0005 | - |
- |
Homo sapiens | TBBz | |
| 0.0008 | - |
- |
Homo sapiens | apigenin | |
| 0.002 | - |
- |
Homo sapiens | emodin | |
| 0.013 | - |
- |
Homo sapiens | DRB | |
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