Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Mills, S.J.; Vandeput, F.; Trusselle, M.N.; Safrany, S.T.; Erneux, C.; Potter, B.V.
    Benzene polyphosphates as tools for cell signalling: inhibition of inositol 1,4,5-trisphosphate 5-phosphatase and interaction with the pH domain of protein kinase Balpha (2008), ChemBioChem, 9, 1757-1766.
    View publication on PubMedView publication on EuropePMC

Application

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

Cloned(Commentary)

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

Inhibitors

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

Natural Substrates/ Products (Substrates)

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 ?
-
?

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.3.36 brain
-
Homo sapiens
-

Substrates and Products (Substrate)

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 ?
-
?

Synonyms

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

Ki Value [mM]

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

IC50 Value

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

General Information

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