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 | 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 | 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 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 | 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 | 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 | Comment | Organism |
---|---|---|
phosphoprotein | phosphorylation by tyrosine kinases activates the enzyme | Mammalia |
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 | 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 | 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 | Comment | Organism |
---|---|---|
class I phosphoinositide 3-kinase | - |
Mammalia |
class I phosphoinositide 3-kinase | - |
Homo sapiens |
PI3-kinase | - |
Mammalia |
PI3-kinase | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Mammalia | |
ATP | - |
Homo sapiens |