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Literature summary for 2.7.11.1 extracted from

  • Watson, L.J.; Alexander, K.M.; Mohan, M.L.; Bowman, A.L.; Mangmool, S.; Xiao, K.; Naga Prasad, S.V.; Rockman, H.A.
    Phosphorylation of Src by phosphoinositide 3-kinase regulates beta-adrenergic receptor-mediated EGFR transactivation (2016), Cell. Signal., 28, 1580-1592.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

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

Inhibitors Comment Organism Structure
Ly-294002
-
Homo sapiens
Wortmannin
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens
Mn2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens P48736 isozyme PI3Kgamma
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His6-tagged wild-type full-length PI3Kgamma isozyme from Spodoptera frugiperda Sf9 cells by nickel affinity chromatography Homo sapiens

Substrates and Products (Substrate)

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

Synonyms Comment Organism
phosphoinositide 3-kinase
-
Homo sapiens
PI3K
-
Homo sapiens
PI3Kgamma
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

General Information

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