Literature summary for 2.7.11.1 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.

Search for more literature for 2.7.11.1

Application

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(Commentary)

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

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/ Products (Substrates)

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

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	enzyme binds both soluble inositol polyphosphates and inositol phospholipids	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
AKT	-	Homo sapiens
PKBalpha	-	Homo sapiens
protein kinas B	-	Homo sapiens
protein kinase Balpha	-	Homo sapiens

Ki Value [mM]

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

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

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Release 2023.1 (January 2023)