Activating Compound | Comment | Organism | Structure |
---|---|---|---|
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 | |
Ras | active RAs activates class 1 enzymes | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
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 | Comment | Organism | Structure |
---|---|---|---|
17-hydroxywortmannin | - |
Homo sapiens | |
CAL-101 | a specific inhibitor of the PI3Kdelta isoform | Homo sapiens | |
IC87114 | a specific inhibitor of the PI3Kdelta isoform, inhibits AML proliferation and augments the effects of a topoisomerase 2 inhibitor | Homo sapiens | |
LY294002 | a quercetin analogue | Homo sapiens | |
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 | |
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 | |
WAY-266175 | - |
Homo sapiens | |
WAY-266176 | - |
Homo sapiens | |
Wortmannin | member of a class of steroidal furanoids, shows equally potent activity against all the class I PI3K enzymes, has antiproliferative effect | Homo sapiens | |
XL147 | targets only the class I PI3Ks | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
membrane | - |
Homo sapiens | 16020 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
glioma cell | - |
Homo sapiens | - |
HCT-116 cell | - |
Homo sapiens | - |
myeloid cell line | PI3Kdelta isoform is most prominently expressed in myeloid cells | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + phosphatidylinositol-4,5-bisphosphate | class I PI3Ks | Homo sapiens | ADP + phosphatidylinositol-3,4,5-trisphosphate | - |
? | |
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 | Comment | Organism |
---|---|---|
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 | Comment | Organism |
---|---|---|
PI3K | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
General Information | Comment | Organism |
---|---|---|
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 |
metabolism | the signaling cascade involving the enzyme is known as the PI3K/Akt/mTor axis | Homo sapiens |