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Literature summary extracted from

  • Anderson, K.E.; Jackson, S.P.
    Class I phosphoinositide 3-kinases (2003), Int. J. Biochem. Cell Biol., 35, 1028-1033.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.1.137 betagamma subunit of heterotrimeric G-proteins direct activation, acts synergistically with Ras Mammalia
2.7.1.137 additional information downstream lipid products affect the enzyme activity via effectors, enzyme activation occurs via G-protein-coupled receptors, cell adhesion, and phosphorylation by tyrosine kinase, the subunits are differently sensitive, overview Mammalia
2.7.1.137 Ras acts synergistically with betagamma subunit of heterotrimeric G-proteins Mammalia

Application

EC Number Application Comment Organism
2.7.1.137 pharmacology development of specific isozyme inhibitors may offer therapeutic benefit in a broad range of clinical settings related to cancer, inflammatory and immunological diseases Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.137 LY294002 specific inhibitor Mammalia
2.7.1.137 additional information downstream lipid products affect the enzyme activity via effectors Mammalia
2.7.1.137 Wortmannin specific inhibitor Mammalia

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.7.1.137 85000
-
 1 * 85000 + 1 * 110000 Homo sapiens
2.7.1.137 85000
-
 1 * 85000, regulatory/adaptor subunit, + 1 * 110000, catalytic subunit Mammalia
2.7.1.137 110000
-
 1 * 85000 + 1 * 110000 Homo sapiens
2.7.1.137 110000
-
 1 * 85000, regulatory/adaptor subunit, + 1 * 110000, catalytic subunit Mammalia

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.1.137 ATP + phosphatidylinositol 4,5-bisphosphate Mammalia class I enzyme, preferred substrate in vivo ADP + phosphatidylinositol 3,4,5-trisphosphate
-
 ?
2.7.1.137 ATP + phosphatidylinositol 4,5-bisphosphate Homo sapiens class I enzyme, preferred substrate in vivo, physiologic regulation and mode of action ADP + phosphatidylinositol 3,4,5-trisphosphate
-
 ?
2.7.1.137 additional information Mammalia the enzyme 3'-phosphorylates the inositol head group of membrane phosphoinositides, isozymes are subject to differential regulation and may play distinct roles in the cell, e.g. in cell survival, vesicle trafficking, cytoskeletal reorganization, and chemotaxis, the enzymeis involved in diverse signalling pathways, detailed schematic overview ?
-
 ?
2.7.1.137 additional information Homo sapiens the enzyme 3'-phosphorylates the inositol head group of membrane phosphoinositides, isozymes are subject to differential regulation and may play distinct roles in the cell, the enzyme is involved in many cellular responses important in pathogenesis of disease ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.137 Homo sapiens
-
 class I isozymes
-
2.7.1.137 Mammalia
-
 class I isozymes, 2 subgroups Ia and Ib, subgroup Ia contains 3 isozymes alpha, beta, and gamma, different splicing variants of subunits
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.1.137 phosphoprotein phosphorylation by tyrosine kinases activates the enzyme Mammalia

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.1.137 leukocyte isozyme Ia gamma Mammalia
-
2.7.1.137 leukocyte isozyme Ia gamma Homo sapiens
-
2.7.1.137 additional information isozymes Ia alpha and beta are widely expressed in tissues Mammalia
-
2.7.1.137 additional information isozymes Ia alpha and Ia beta are widely expressed in tissues Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.137 ATP + phosphatidylinositol class I enzyme Mammalia ADP + phosphatidylinositol 3-phosphate
-
 ?
2.7.1.137 ATP + phosphatidylinositol class I enzyme, preferred substrate of the class III enzyme Homo sapiens ADP + phosphatidylinositol 3-phosphate
-
 ?
2.7.1.137 ATP + phosphatidylinositol 4,5-bisphosphate class I enzyme, preferred substrate in vivo Mammalia ADP + phosphatidylinositol 3,4,5-trisphosphate
-
 ?
2.7.1.137 ATP + phosphatidylinositol 4,5-bisphosphate class I enzyme, preferred substrate in vivo, physiologic regulation and mode of action Homo sapiens ADP + phosphatidylinositol 3,4,5-trisphosphate
-
 ?
2.7.1.137 ATP + phosphatidylinositol 4,5-bisphosphate class I enzyme Mammalia ADP + phosphatidylinositol 3,4,5-trisphosphate
-
 ?
2.7.1.137 ATP + phosphatidylinositol 4,5-bisphosphate class I enzyme, preferred substrate of the class I enzyme Homo sapiens ADP + phosphatidylinositol 3,4,5-trisphosphate
-
 ?
2.7.1.137 ATP + phosphatidylinositol 4-phosphate class I enzyme Mammalia ADP + phosphatidylinositol 3,4-bisphosphate
-
 ?
2.7.1.137 ATP + phosphatidylinositol 4-phosphate class I enzyme, preferred substrate of the class II enzyme Homo sapiens ADP + phosphatidylinositol 3,4-bisphosphate
-
 ?
2.7.1.137 additional information the enzyme 3'-phosphorylates the inositol head group of membrane phosphoinositides, isozymes are subject to differential regulation and may play distinct roles in the cell, e.g. in cell survival, vesicle trafficking, cytoskeletal reorganization, and chemotaxis, the enzymeis involved in diverse signalling pathways, detailed schematic overview Mammalia ?
-
 ?
2.7.1.137 additional information the enzyme 3'-phosphorylates the inositol head group of membrane phosphoinositides, isozymes are subject to differential regulation and may play distinct roles in the cell, the enzyme is involved in many cellular responses important in pathogenesis of disease Homo sapiens ?
-
 ?
2.7.1.137 additional information the enzyme interacts with other proteins and substrates via the pleckstrin homology PH domain Homo sapiens ?
-
 ?
2.7.1.137 additional information the enzyme interacts with other proteins and substrates via the pleckstrin homology PH domain, class I isozyme subgroups Ia and Ib are divided due to their mode of action and structure Mammalia ?
-
 ?

Subunits

EC Number Subunits Comment Organism
2.7.1.137 dimer 1 * 85000 + 1 * 110000 Homo sapiens
2.7.1.137 dimer 1 * 85000, regulatory/adaptor subunit, + 1 * 110000, catalytic subunit Mammalia
2.7.1.137 More different splicing variants of subunits, class I isozyme subgroups Ia and Ib are divided due to their mode of action and structure, the 110 kDa catalytic subunit contains at least 4 domains, the catalytic lipid kinase domain, a PI kinase domain, a C2 phospholipid binding domain, and a Ras-binding domain, the regulatory 85 kDa subunit contains a Src homology 3 SH3 domain, 2 Src homology 2 SH2 domains, a Bcr homologue, and a proline-rich region, domain organization and functions of class I-III enzymes, overview Mammalia

Synonyms

EC Number Synonyms Comment Organism
2.7.1.137 class I phosphoinositide 3-kinase
-
 Mammalia
2.7.1.137 class I phosphoinositide 3-kinase
-
 Homo sapiens
2.7.1.137 PI3-kinase
-
 Mammalia
2.7.1.137 PI3-kinase
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.1.137 ATP
-
 Mammalia
2.7.1.137 ATP
-
 Homo sapiens