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Literature summary for 2.7.1.137 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

Activating Compound Comment Organism Structure
betagamma subunit of heterotrimeric G-proteins direct activation, acts synergistically with Ras Mammalia
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
Ras acts synergistically with betagamma subunit of heterotrimeric G-proteins Mammalia

Application

Application Comment Organism
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

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

Molecular Weight [Da]

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + phosphatidylinositol 4,5-bisphosphate Mammalia class I enzyme, preferred substrate in vivo ADP + phosphatidylinositol 3,4,5-trisphosphate
-
?
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
-
?
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 ?
-
?
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

Organism UniProt Comment Textmining
Homo sapiens
-
class I isozymes
-
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

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

Source Tissue

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + phosphatidylinositol class I enzyme Mammalia ADP + phosphatidylinositol 3-phosphate
-
?
ATP + phosphatidylinositol class I enzyme, preferred substrate of the class III enzyme Homo sapiens ADP + phosphatidylinositol 3-phosphate
-
?
ATP + phosphatidylinositol 4,5-bisphosphate class I enzyme, preferred substrate in vivo Mammalia ADP + phosphatidylinositol 3,4,5-trisphosphate
-
?
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
-
?
ATP + phosphatidylinositol 4,5-bisphosphate class I enzyme Mammalia ADP + phosphatidylinositol 3,4,5-trisphosphate
-
?
ATP + phosphatidylinositol 4,5-bisphosphate class I enzyme, preferred substrate of the class I enzyme Homo sapiens ADP + phosphatidylinositol 3,4,5-trisphosphate
-
?
ATP + phosphatidylinositol 4-phosphate class I enzyme Mammalia ADP + phosphatidylinositol 3,4-bisphosphate
-
?
ATP + phosphatidylinositol 4-phosphate class I enzyme, preferred substrate of the class II enzyme Homo sapiens ADP + phosphatidylinositol 3,4-bisphosphate
-
?
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 ?
-
?
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 ?
-
?
additional information the enzyme interacts with other proteins and substrates via the pleckstrin homology PH domain Homo sapiens ?
-
?
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

Subunits Comment Organism
dimer 1 * 85000 + 1 * 110000 Homo sapiens
dimer 1 * 85000, regulatory/adaptor subunit, + 1 * 110000, catalytic subunit Mammalia
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

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

Cofactor

Cofactor Comment Organism Structure
ATP
-
Mammalia
ATP
-
Homo sapiens