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Literature summary extracted from

  • Ihle, N.T.; Powis, G.
    Take your PIK: phosphatidylinositol 3-kinase inhibitors race through the clinic and toward cancer therapy (2009), Mol. Cancer Ther., 8, 1-9.
    View publication on PubMedView publication on EuropePMC

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.1.153 additional information the PI3K/Akt pathway is directly activated through loss or inactivation of PTEN, a tumor suppressor. Inhibition of mTor has the ability to activate PI3K signaling either by feedback to growth factor receptors, or by promoting the formation of an alternative mTor complex with rictor, that may serve to phosphorylate Akt, seen in both cell models and clinical samples Homo sapiens
2.7.1.153 Ras active RAs activates class 1 enzymes Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.7.1.153 additional information the most common sites for hotspot mutations of PI3Kalpha are around amino acid 1047 in the kinase domain, and amino acid 545 in the helical domain, the mutations are involved in breast and colon tumorigenesis Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.153 17-hydroxywortmannin
-
 Homo sapiens
2.7.1.153 CAL-101 a specific inhibitor of the PI3Kdelta isoform Homo sapiens
2.7.1.153 IC87114 a specific inhibitor of the PI3Kdelta isoform, inhibits AML proliferation and augments the effects of a topoisomerase 2 inhibitor Homo sapiens
2.7.1.153 LY294002 a quercetin analogue Homo sapiens
2.7.1.153 PI-103 shows increased efficacy in inhibiting the growth of glioma cells due to its activity against both the class I PI3Ks and the PIK family member mTor Homo sapiens
2.7.1.153 PX-866 irreversible PI3K inhibitor, shows selectivity for the alpha, delta, and gamma class I PI3K isoforms, inhibits the beta isoform at higher concentrations, and shows decreased selectivity for mTor Homo sapiens
2.7.1.153 WAY-266175
-
 Homo sapiens
2.7.1.153 WAY-266176
-
 Homo sapiens
2.7.1.153 Wortmannin member of a class of steroidal furanoids, shows equally potent activity against all the class I PI3K enzymes, has antiproliferative effect Homo sapiens
2.7.1.153 XL147 targets only the class I PI3Ks Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.1.153 membrane
-
 Homo sapiens 16020
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.1.153 ATP + phosphatidylinositol-4,5-bisphosphate Homo sapiens class I PI3Ks ADP + phosphatidylinositol-3,4,5-trisphosphate the product allows for the recruitment to the plasma membrane of proteins containing a pleckstrin homology domain ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.153 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.1.153 glioma cell
-
 Homo sapiens
-
2.7.1.153 HCT-116 cell
-
 Homo sapiens
-
2.7.1.153 myeloid cell line PI3Kdelta isoform is most prominently expressed in myeloid cells Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.153 ATP + phosphatidylinositol-4,5-bisphosphate class I PI3Ks Homo sapiens ADP + phosphatidylinositol-3,4,5-trisphosphate
-
 ?
2.7.1.153 ATP + phosphatidylinositol-4,5-bisphosphate class I PI3Ks Homo sapiens ADP + phosphatidylinositol-3,4,5-trisphosphate the product allows for the recruitment to the plasma membrane of proteins containing a pleckstrin homology domain ?

Subunits

EC Number Subunits Comment Organism
2.7.1.153 dimer class I PI3Ks exist as heterodimers consisting of one of four p110 catalytic subunit isoforms and one of two families of regulatory subunit forms. PI3K class III has only one member known as Vps34 Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.7.1.153 PI3K
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.1.153 ATP
-
 Homo sapiens

General Information

EC Number General Information Comment Organism
2.7.1.153 malfunction aberrant PI3K signaling has been found to play an important role in multiple aspects of tumorgenesis including uncontrolled proliferation, resistance to apoptosis, angiogenesis and metastatic capability. The PI3Kbeta isoform is implicated as necessary for transformation induced by the loss or inactivation of the PTEN tumor suppressor both in vitro and in vivo Homo sapiens
2.7.1.153 metabolism the signaling cascade involving the enzyme is known as the PI3K/Akt/mTor axis Homo sapiens