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Literature summary extracted from

  • Duncan, J.S.; Litchfield, D.W.
    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.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.11.1 pharmacology CK2 is a potential therapeutic target and a target for inhibitor design, e.g. in anti-cancer therapy Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.1 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

EC Number Protein Variants Comment Organism
2.7.11.1 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
2.7.11.1 V66A/I174A site-directed mutagenesis, an engineered TBB inhibitor-resistant CK2 mutant CK2alpha'R Homo sapiens
2.7.11.1 V67A/I175A site-directed mutagenesis, an inhibitor-resistant CK2 mutant CK2alpha'R Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.1 (5-oxo-5,6-dihydroindolo[1,2-a]quinazolin-7-yl)acetic acid i.e. IQA Homo sapiens
2.7.11.1 2-dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole i.e. DMAT Homo sapiens
2.7.11.1 4,5,6,7-tetrabromo-1H-benzotriazole i.e. TBB Homo sapiens
2.7.11.1 4,5,6,7-tetrabromobenzimidazole i.e. TBBz or TBI Homo sapiens
2.7.11.1 apigenin
-
 Homo sapiens
2.7.11.1 DRB
-
 Homo sapiens
2.7.11.1 ellagic acid
-
 Homo sapiens
2.7.11.1 emodin
-
 Homo sapiens
2.7.11.1 additional information in vivo inhibition strategies in the mouse model, validation of CK2 targets identification of bona fide targets, overview Homo sapiens
2.7.11.1 TBCA
-
 Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.1 Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.1 ATP + geminin Homo sapiens a cell cycle regulatory protein ADP + phosphorylated geminin
-
 ?
2.7.11.1 ATP + M3-muscarnic receptor Homo sapiens
-
 ADP + phosphorylated M3-muscarnic receptor
-
 ?
2.7.11.1 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
-
 ?
2.7.11.1 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

EC Number Organism UniProt Comment Textmining
2.7.11.1 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.1 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)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.1 ATP + geminin
-
 Homo sapiens ADP + phosphorylated geminin
-
 ?
2.7.11.1 ATP + geminin a cell cycle regulatory protein Homo sapiens ADP + phosphorylated geminin
-
 ?
2.7.11.1 ATP + M3-muscarnic receptor
-
 Homo sapiens ADP + phosphorylated M3-muscarnic receptor
-
 ?
2.7.11.1 ATP + procaspase-2
-
 Homo sapiens ADP + phosphorylated procaspase-2
-
 ?
2.7.11.1 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
-
 ?
2.7.11.1 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

EC Number Synonyms Comment Organism
2.7.11.1 CK2
-
 Homo sapiens
2.7.11.1 protein kinase CK2
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.1 ATP
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.11.1 0.00002
-
 ellagic acid
-
 Homo sapiens
2.7.11.1 0.00004
-
 2-dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole
-
 Homo sapiens
2.7.11.1 0.000077
-
 TBCA
-
 Homo sapiens
2.7.11.1 0.00017
-
 (5-oxo-5,6-dihydroindolo[1,2-a]quinazolin-7-yl)acetic acid
-
 Homo sapiens
2.7.11.1 0.0004
-
 4,5,6,7-tetrabromo-1H-benzotriazole
-
 Homo sapiens
2.7.11.1 0.0007
-
 4,5,6,7-tetrabromobenzimidazole
-
 Homo sapiens
2.7.11.1 0.00074
-
 apigenin
-
 Homo sapiens
2.7.11.1 0.00185
-
 emodin
-
 Homo sapiens
2.7.11.1 0.0045
-
 DRB
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.1 0.00004
-
-
 Homo sapiens ellagic acid
2.7.11.1 0.00011
-
-
 Homo sapiens TBCA
2.7.11.1 0.00014
-
-
 Homo sapiens DMAT
2.7.11.1 0.00039
-
-
 Homo sapiens IQA
2.7.11.1 0.0005
-
-
 Homo sapiens TBB
2.7.11.1 0.0005
-
-
 Homo sapiens TBBz
2.7.11.1 0.0008
-
-
 Homo sapiens apigenin
2.7.11.1 0.002
-
-
 Homo sapiens emodin
2.7.11.1 0.013
-
-
 Homo sapiens DRB