EC Number | Application | Comment | Organism |
---|---|---|---|
2.7.11.1 | drug development | the kinase activity of protein kinase Balpha has received considerable attention as a drug target, since protein kinase Balpha is constituently active in cancerous cells and requires strict regulation, inhibition of phosphatidylinositol 3,4,5-trisphosphate binding to the PH domain by small molecules has also become a priority target for anticancer treatment | Homo sapiens |
EC Number | Cloned (Comment) | Organism |
---|---|---|
2.7.11.1 | the PH domain of PKBalpha (amino acids 1-123) is subcloned into the BamH1 restriction site of the Escherichia coli expression vector pGEX2T | Homo sapiens |
EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
2.7.11.1 | benzene 1,2,3,4-tetrakisphosphate | - |
Homo sapiens | |
2.7.11.1 | benzene 1,2,3,5-tetrakisphosphate | - |
Homo sapiens | |
2.7.11.1 | benzene 1,2,3-trisphosphate | - |
Homo sapiens | |
2.7.11.1 | benzene 1,2,4,5-tetrakisphosphate | - |
Homo sapiens | |
2.7.11.1 | benzene 1,2,4-trisphosphate | - |
Homo sapiens | |
2.7.11.1 | benzene 1,3,5-trisphosphate | - |
Homo sapiens | |
2.7.11.1 | biphenyl 2,3',4,5',6-pentakisphosphate | - |
Homo sapiens | |
2.7.11.1 | D-myo-Inositol 1,3,4,5-tetrakisphosphate | - |
Homo sapiens | |
2.7.11.1 | diC8-phosphatidylinositol 3,4,5-trisphosphate | - |
Homo sapiens | |
3.1.3.36 | 3-benzyl-oxybenzene 1,2,4-trisphosphate | - |
Homo sapiens | |
3.1.3.36 | 3-hydroxybenzene 1,2,4-trisphosphate | - |
Homo sapiens | |
3.1.3.36 | benzene 1,2,3,4-tetrakisphosphate | - |
Homo sapiens | |
3.1.3.36 | benzene 1,2,3,5-tetrakisphosphate | - |
Homo sapiens | |
3.1.3.36 | benzene 1,2,3-trisphosphate | - |
Homo sapiens | |
3.1.3.36 | benzene 1,2,4,5-tetrakisphosphate | - |
Homo sapiens | |
3.1.3.36 | benzene 1,2,4-trisphosphate | - |
Homo sapiens | |
3.1.3.36 | benzene 1,3,5-trisphosphate | - |
Homo sapiens | |
3.1.3.36 | biphenyl 2,3',4,5',6-pentakisphosphate | - |
Homo sapiens | |
3.1.3.56 | 3-benzyloxybenzene 1,2,4-trisphosphate | - |
Homo sapiens | |
3.1.3.56 | 3-hydroxybenzene 1,2,4-trisphosphate | - |
Homo sapiens | |
3.1.3.56 | benzene 1,2,3,4-tetrakisphosphate | - |
Homo sapiens | |
3.1.3.56 | benzene 1,2,3,5-tetrakisphosphate | - |
Homo sapiens | |
3.1.3.56 | benzene 1,2,3-trisphosphate | - |
Homo sapiens | |
3.1.3.56 | benzene 1,2,4,5-tetrakisphosphate | - |
Homo sapiens | |
3.1.3.56 | benzene 1,2,4-trisphosphate | - |
Homo sapiens | |
3.1.3.56 | benzene 1,2-bisphosphate | - |
Homo sapiens | |
3.1.3.56 | benzene 1,3,5-trisphosphate | - |
Homo sapiens | |
3.1.3.56 | biphenyl 2,3',4,5',6-pentakisphosphate | - |
Homo sapiens |
EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
2.7.11.1 | additional information | Homo sapiens | enzyme binds both soluble inositol polyphosphates and inositol phospholipids | ? | - |
? | |
3.1.3.56 | additional information | Homo sapiens | enzyme only binds soluble inositol polyphosphates | ? | - |
? |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
2.7.11.1 | Homo sapiens | - |
- |
- |
3.1.3.36 | Homo sapiens | - |
- |
- |
3.1.3.56 | Homo sapiens | - |
- |
- |
EC Number | Source Tissue | Comment | Organism | Textmining |
---|---|---|---|---|
3.1.3.36 | brain | - |
Homo sapiens | - |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
2.7.11.1 | additional information | enzyme binds both soluble inositol polyphosphates and inositol phospholipids | Homo sapiens | ? | - |
? | |
3.1.3.36 | 1D-myo-inositol 1,4,5-trisphosphate + H2O | - |
Homo sapiens | 1D-myo-inositol 1,4-bisphosphate + phosphate | - |
? | |
3.1.3.56 | additional information | enzyme only binds soluble inositol polyphosphates | Homo sapiens | ? | - |
? |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
2.7.11.1 | AKT | - |
Homo sapiens |
2.7.11.1 | PKBalpha | - |
Homo sapiens |
2.7.11.1 | protein kinas B | - |
Homo sapiens |
2.7.11.1 | protein kinase Balpha | - |
Homo sapiens |
3.1.3.36 | inositol 1,4,5-trisphosphate 5-phosphatase | - |
Homo sapiens |
3.1.3.56 | inositol 1,4,5-trisphosphate 5-phosphatase | - |
Homo sapiens |
3.1.3.56 | Ins(1,4,5)P3 5-phosphatase | - |
Homo sapiens |
3.1.3.56 | trisphosphate 5-phosphatase | - |
Homo sapiens |
3.1.3.56 | type I inositol-1,4,5-trisphosphate 5-phosphatase | - |
Homo sapiens |
EC Number | Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|---|
2.7.11.1 | 0.000027 | - |
biphenyl 2,3',4,5',6-pentakisphosphate | values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate | Homo sapiens | |
2.7.11.1 | 0.00008 | - |
benzene 1,2,3,4-tetrakisphosphate | values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate | Homo sapiens | |
2.7.11.1 | 0.00011 | - |
benzene 1,2,4,5-tetrakisphosphate | values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate | Homo sapiens | |
2.7.11.1 | 0.00012 | - |
D-myo-Inositol 1,3,4,5-tetrakisphosphate | values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate | Homo sapiens | |
2.7.11.1 | 0.00022 | - |
benzene 1,2,3,5-tetrakisphosphate | values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate | Homo sapiens | |
2.7.11.1 | 0.00023 | - |
diC8-phosphatidylinositol 3,4,5-trisphosphate | values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate | Homo sapiens | |
2.7.11.1 | 0.00059 | - |
benzene 1,2,3-trisphosphate | values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate | Homo sapiens | |
2.7.11.1 | 0.00061 | - |
benzene 1,2,4-trisphosphate | values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate | Homo sapiens | |
2.7.11.1 | 0.00218 | - |
benzene 1,3,5-trisphosphate | values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate | Homo sapiens |
EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|---|
3.1.3.36 | 0.001 | - |
- |
Homo sapiens | biphenyl 2,3',4,5',6-pentakisphosphate | |
3.1.3.36 | 0.004 | - |
- |
Homo sapiens | benzene 1,2,4,5-tetrakisphosphate | |
3.1.3.36 | 0.014 | - |
- |
Homo sapiens | benzene 1,2,4-trisphosphate | |
3.1.3.36 | 0.016 | - |
- |
Homo sapiens | benzene 1,3,5-trisphosphate | |
3.1.3.36 | 0.021 | - |
- |
Homo sapiens | 3-hydroxybenzene 1,2,4-trisphosphate | |
3.1.3.36 | 0.068 | - |
- |
Homo sapiens | 3-benzyl-oxybenzene 1,2,4-trisphosphate | |
3.1.3.36 | 0.078 | - |
- |
Homo sapiens | benzene 1,2,3,5-tetrakisphosphate | |
3.1.3.36 | 0.086 | - |
- |
Homo sapiens | benzene 1,2,3-trisphosphate | |
3.1.3.36 | 0.098 | - |
- |
Homo sapiens | benzene 1,2,3,4-tetrakisphosphate | |
3.1.3.56 | additional information | - |
IC value is higher than 0.2 mM, IC50 value is obtained in the presence of 1 microM D-myo-inositol 1,4,5-trisphosphate as substrate | Homo sapiens | benzene 1,2-bisphosphate | |
3.1.3.56 | 0.001 | - |
IC50 value is obtained in the presence of 1 microM D-myo-inositol 1,4,5-trisphosphate as substrate | Homo sapiens | biphenyl 2,3',4,5',6-pentakisphosphate | |
3.1.3.56 | 0.004 | - |
IC50 value is obtained in the presence of 1 microM D-myo-inositol 1,4,5-trisphosphate as substrate | Homo sapiens | benzene 1,2,4,5-tetrakisphosphate | |
3.1.3.56 | 0.014 | - |
potential mimic of D-myo-inositol 1,4,5-trisphosphate, IC50 value is obtained in the presence of 1 microM D-myo-inositol 1,4,5-trisphosphate as substrate | Homo sapiens | benzene 1,2,4-trisphosphate | |
3.1.3.56 | 0.016 | - |
IC50 value is obtained in the presence of 1 microM D-myo-inositol 1,4,5-trisphosphate as substrate | Homo sapiens | benzene 1,3,5-trisphosphate | |
3.1.3.56 | 0.021 | - |
IC50 value is obtained in the presence of 1 microM D-myo-inositol 1,4,5-trisphosphate as substrate | Homo sapiens | 3-hydroxybenzene 1,2,4-trisphosphate | |
3.1.3.56 | 0.068 | - |
IC50 value is obtained in the presence of 1 microM D-myo-inositol 1,4,5-trisphosphate as substrate | Homo sapiens | 3-benzyloxybenzene 1,2,4-trisphosphate | |
3.1.3.56 | 0.078 | - |
IC50 value is obtained in the presence of 1 microM D-myo-inositol 1,4,5-trisphosphate as substrate 6 | Homo sapiens | benzene 1,2,3,5-tetrakisphosphate | |
3.1.3.56 | 0.086 | - |
IC50 value is obtained in the presence of 1 microM D-myo-inositol 1,4,5-trisphosphate as substrate | Homo sapiens | benzene 1,2,3-trisphosphate | |
3.1.3.56 | 0.098 | - |
IC50 value is obtained in the presence of 1 microM D-myo-inositol 1,4,5-trisphosphate as substrate 6 | Homo sapiens | benzene 1,2,3,4-tetrakisphosphate |
EC Number | General Information | Comment | Organism |
---|---|---|---|
2.7.11.1 | physiological function | protein kinase Balpha is involved in inositol lipid signalling, a pleckstrin homology (PH) domain binds phosphatidylinositol 3,4,5-trisphosphate which is required for PKB phosphorylation and activation | Homo sapiens |