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 |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate | Homo sapiens | - |
ADP + 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate | - |
? | |
additional information | Homo sapiens | the enzyme is also active as a serine-dependent protein kinase with Src as substrate and specifically phosphorylating residue Ser70 of Src | ? | - |
? |
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 + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate | - |
Homo sapiens | ADP + 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate | - |
? | |
additional information | the enzyme is also active as a serine-dependent protein kinase with Src as substrate and specifically phosphorylating residue Ser70 of Src | Homo sapiens | ? | - |
? | |
additional information | the enzyme is also active as a serine-dependent protein kinase with Src as substrate and specifically phosphorylating residue Ser70 of Src. No activity with S70A Src mutant | 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 | Homo sapiens |
physiological function | the generation of phosphatidylinositol (3,4,5)-tris-phosphate (PIP3) by the lipid kinase function stabilizes beta2AREGFR complexes while the protein kinase activity of PI3K regulates Src activation by direct phosphorylation. The lipid kinase activity of PI3K is responsible for beta2AREGFR complex formation. 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 |