Application | Comment | Organism |
---|---|---|
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 |
Cloned (Comment) | Organism |
---|---|
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 |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
benzene 1,2,3,4-tetrakisphosphate | - |
Homo sapiens | |
benzene 1,2,3,5-tetrakisphosphate | - |
Homo sapiens | |
benzene 1,2,3-trisphosphate | - |
Homo sapiens | |
benzene 1,2,4,5-tetrakisphosphate | - |
Homo sapiens | |
benzene 1,2,4-trisphosphate | - |
Homo sapiens | |
benzene 1,3,5-trisphosphate | - |
Homo sapiens | |
biphenyl 2,3',4,5',6-pentakisphosphate | - |
Homo sapiens | |
D-myo-Inositol 1,3,4,5-tetrakisphosphate | - |
Homo sapiens | |
diC8-phosphatidylinositol 3,4,5-trisphosphate | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | enzyme binds both soluble inositol polyphosphates and inositol phospholipids | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | enzyme binds both soluble inositol polyphosphates and inositol phospholipids | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
AKT | - |
Homo sapiens |
PKBalpha | - |
Homo sapiens |
protein kinas B | - |
Homo sapiens |
protein kinase Balpha | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 |
General Information | Comment | Organism |
---|---|---|
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 |