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Literature summary for 2.7.1.153 extracted from

  • Thomas, D.; Powell, J.A.; Green, B.D.; Barry, E.F.; Ma, Y.; Woodcock, J.; Fitter, S.; Zannettino, A.C.; Pitson, S.M.; Hughes, T.P.; Lopez, A.F.; Shepherd, P.R.; Wei, A.H.; Ekert, P.G.; Guthridge, M.A.
    Protein kinase activity of phosphoinositide 3-kinase regulates cytokine-dependent cell survival (2013), PLoS Biol., 11, e1001515.
    View publication on PubMedView publication on EuropePMC
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Activating Compound

Activating Compound Comment Organism Structure
additional information physiological concentrations of cytokine in the picomolar range were sufficient for activating the protein kinase activity of PI3K leading to Ser585 phosphorylation and hemopoietic cell survival but did not activate PI3K lipid kinase signaling or promote proliferation Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information overexpression of the GFP-tagged PH domain of Akt1 blocks the binding of endogenous PH-domain proteins (such as Akt) to phosphatidyl inositol phosphates in the plasma membrane thereby abrogating PI3K lipid signaling but permitting PI3K protein kinase signaling Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information blockade of PI3K lipid signaling by expression of the pleckstrin homology of Akt1 Homo sapiens
PIK-75 a p110alpha-selective PI3K inhibitor Homo sapiens
YM024 a p110alpha-selective PI3K inhibitor Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens phosphoinositide 3-kinase (PI3K) is a dual specificity kinase that is able to phosphorylate both lipid and protein substrates. In addition to their lipid kinase activity, all members of the class 1 PI3K family also possess intrinsic protein kinase activity ?
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 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P42336 isozyme PI3Kalpha
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Source Tissue

Source Tissue Comment Organism Textmining
leukemia cell primary human acute myeloid leukemia (AML) cells Homo sapiens
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information phosphoinositide 3-kinase (PI3K) is a dual specificity kinase that is able to phosphorylate both lipid and protein substrates. In addition to their lipid kinase activity, all members of the class 1 PI3K family also possess intrinsic protein kinase activity Homo sapiens ?
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 ?

Synonyms

Synonyms Comment Organism
p110alpha
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 Homo sapiens
phosphoinositide 3-kinase
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 Homo sapiens
PI3K
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 Homo sapiens

General Information

General Information Comment Organism
physiological function phosphoinositide 3-kinase (PI3K) is a dual specificity kinase that is known to be involved in cell survival and malignant transformation, and it is able to phosphorylate both lipid and protein substrates. PI3K protein kinase activity can directly phosphorylate growth factor receptors on human hematopoietic (blood) cells to promote a survival-only response. The protein kinase activity but not the lipid kinase activity of PI3K promotes cytokine-mediated cell survival. The PI3K lipid kinase activity is not essential for regulating cell survival Homo sapiens