Cloned (Comment) | Organism |
---|---|
recombinant expression of His6-tagged wild-type full-length PI3Kgamma isozyme in Spodoptera frugiperda Sf9 cells using the baculovirus transfection method | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
Ly-294002 | - |
Homo sapiens | |
Wortmannin | - |
Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Homo sapiens | |
Mn2+ | required | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + Src protein | Homo sapiens | - |
ADP + phosphorylated Src protein | - |
? | |
additional information | Homo sapiens | the enzyme is also active as lipid kinase generating phosphatidylinositol 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate from 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P48736 | isozyme PI3Kgamma | - |
Purification (Comment) | Organism |
---|---|
recombinant His6-tagged wild-type full-length PI3Kgamma isozyme from Spodoptera frugiperda Sf9 cells by nickel affinity chromatography | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + Src protein | - |
Homo sapiens | ADP + phosphorylated Src protein | - |
? | |
ATP + Src protein | recombinant Src expressed in HEK-293 cells, specific phosphorylation of Ser70, no activity with S70A Src mutant | Homo sapiens | ADP + phosphorylated Src protein | - |
? | |
additional information | the enzyme is also active as lipid kinase generating phosphatidylinositol 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate from 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
phosphoinositide 3-kinase | - |
Homo sapiens |
PI3K | - |
Homo sapiens |
PI3Kgamma | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
30 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
General Information | Comment | Organism |
---|---|---|
malfunction | isoproterenol-induced EGFR transactivation is abolished in PI3Kgamma null mutants or through enzyme inhibition by wortmannin or LY-294002 | Homo sapiens |
metabolism | the enzyme is involved in isoproterenol-induced EGFR transactivation. PI3K is required for beta2AR-stimulated EGFR transactivation | Homo sapiens |
physiological function | the generation of phosphatidylinositol (3,4,5)-tris-phosphate (PIP3) by the lipid kinase function stabilizes beta2AR-EGFR complexes while the protein kinase activity of PI3K regulates Src activation by direct phosphorylation. Phosphorylation of Src by phosphoinositide 3-kinase regulates beta-adrenergic receptor-mediated EGFR transactivation. EGFR transactivation is a mechanism by which the EGF receptor is stimulated, internalized, and downstream signaling initiated following agonist stimulation by a GPCR, such as the beta-adrenergic receptor. The protein kinase activity of PI3K phosphorylates serine residue 70 on Src to enhance its activity and induce EGFR transactivation following beta-adrenergic receptor stimulation. This additional function for PI3K, whereby Src is a substrate for the protein kinase activity of enzyme PI3K, is of importance since Src plays a key role in pathological and physiological signaling | Homo sapiens |