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Literature summary for 2.7.1.153 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
Search for more literature for 2.7.1.153

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

Natural Substrates/ Products (Substrates)

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

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 + 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

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 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. The lipid kinase activity of PI3K is responsible for beta2AR–EGFR 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