3.0
Summary
| Name |  PIK3CGView Modifications |
| Full Name | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform |
| Synonyms | PI3-kinase subunit gamma, PI3K-gamma, PI3Kgamma, PtdIns-3-kinase subunit gamma, Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma, PtdIns-3-kinase subunit p110-gamma, p110gamma, Phosphoinositide-3-kinase catalytic gamma polypeptide, Serine/threonine protein kinase PIK3CG, 2.7.11.1, p120-PI3K |
| Primary ID | P48736 |
| Links |  -  -  |
| Type | protein |
| Relations | 49 |
| Inhibitors | 5-[(2,2-difluoro-1,3-benzodioxol-5-yl)methylidene]thiazolidine-2,4-dione; 1-[4-[[2-(2-amino-5-pyrimidinyl)-7-methyl-4-(4-morpholinyl)-6-thieno[3,2-d]pyrimidinyl]methyl]-1-piperazinyl]-2-hydroxy-1-propanone; (5Z)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolidine-2,4-dione; GSK2126458; PI-103; pictrelisib; XL765; PIK-90; ZSTK-474; 3-[2,4-diamino-7-(3-hydroxyphenyl)-6-pteridinyl]phenol; PKI-402; GSK1059615; PIK-93; PP121; CAY10505; CH5132799; dactolisib; PKI-587; BKM120; AS-605240; 3-methyladenine; IC-87114 |
| Function | Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Links G-protein coupled receptor activation to PIP3 production. Involved in immune, inflammatory and allergic responses. Modulates leukocyte chemotaxis to inflammatory sites and in response to chemoattractant agents. May control leukocyte polarization and migration by regulating the spatial accumulation of PIP3 and by regulating the organization of F-actin formation and integrin-based adhesion at the leading edge. Controls motility of dendritic cells. Together with PIK3CD is involved in natural killer (NK) cell development and migration towards the sites of inflammation. Participates in T-lymphocyte migration. Regulates T-lymphocyte proliferation and cytokine production. Together with PIK3CD participates in T-lymphocyte development. Required for B-lymphocyte development and signaling. Together with PIK3CD participates in neutrophil respiratory burst. Together with PIK3CD is involved in neutrophil chemotaxis and extravasation. Together with PIK3CB promotes platelet aggregation and thrombosis. Regulates alpha-IIb/beta-3 integrins (ITGA2B/ ITGB3) adhesive function in platelets downstream of P2Y12 through a lipid kinase activity-independent mechanism. May have also a lipid kinase activity-dependent function in platelet aggregation. Involved in endothelial progenitor cell migration. Negative regulator of cardiac contractility. Modulates cardiac contractility by anchoring protein kinase A (PKA) and PDE3B activation, reducing cAMP levels. Regulates cardiac contractility also by promoting beta-adrenergic receptor internalization by binding to GRK2 and by non-muscle tropomyosin phosphorylation. Also has serine/threonine protein kinase activity |
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Modifications Tables
Relations
| Regulator | Mechanism | target | score ℹ | |
|---|---|---|---|---|
| + | PRKCB | up-regulates activity 
phosphorylation
|
PIK3CG | 0.516 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | PIK3CG | up-regulates activity
phosphorylation
|
TPM2 | 0.341 |
| Publications: | 1 | Organism: | In Vitro | |
| + | PIK3CG | up-regulates activity
phosphorylation
|
SRC | 0.373 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | PKA | down-regulates activity 
phosphorylation
|
PIK3CG | 0.2 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | 5-[(2,2-difluoro-1,3-benzodioxol-5-yl)methylidene]thiazolidine-2,4-dione | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | 1-[4-[[2-(2-amino-5-pyrimidinyl)-7-methyl-4-(4-morpholinyl)-6-thieno[3,2-d]pyrimidinyl]methyl]-1-piperazinyl]-2-hydroxy-1-propanone | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | (5Z)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolidine-2,4-dione | down-regulates activity
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Mus Musculus | |
| + | PI3K | up-regulates activity
binding
|
PIK3CG | 0.585 |
| Publications: | 1 | Organism: | Chlorocebus Aethiops | |
| + | PIK3CG | up-regulates
binding
|
PDPK1 | 0.617 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | TNF | up-regulates
binding
|
PIK3CG | 0.3 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | GSK2126458 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | TGFB1 | up-regulates activity 
|
PIK3CG | 0.278 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | PI-103 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | LTK | up-regulates
binding
|
PIK3CG | 0.256 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | IRS2 | up-regulates
binding
|
PIK3CG | 0.543 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | pictrelisib | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| Tissue: | Breast | |||
| + | XL765 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | GNGT1 | up-regulates
binding
|
PIK3CG | 0.465 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | PIK-90 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | ZSTK-474 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | ERBB3 | up-regulates
binding
|
PIK3CG | 0.331 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | ITGB4 | up-regulates
binding
|
PIK3CG | 0.2 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | 3-[2,4-diamino-7-(3-hydroxyphenyl)-6-pteridinyl]phenol | down-regulates activity
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | In Vitro | |
| + | PKI-402 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | ERBB4 | up-regulates
binding
|
PIK3CG | 0.325 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | GSK1059615 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | HRAS | up-regulates
binding
|
PIK3CG | 0.814 |
| Publications: | 2 | Organism: | Homo Sapiens | |
| + | PIK-93 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | NRAS | up-regulates
binding
|
PIK3CG | 0.709 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | PP121 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | CAY10505 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | PIK3AP1 | up-regulates
binding
|
PIK3CG | 0.246 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | CH5132799 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | dactolisib | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | PIK3CG | up-regulates
chemical modification
|
PIP3 | 0.8 |
| Publications: | 2 | Organism: | Homo Sapiens | |
| + | CD28 | up-regulates
binding
|
PIK3CG | 0.376 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | PKI-587 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | KRAS | up-regulates
binding
|
PIK3CG | 0.768 |
| Publications: | 2 | Organism: | Homo Sapiens | |
| + | INS | up-regulates
|
PIK3CG | 0.342 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | PIK3CG | up-regulates
|
Survival | 0.7 |
| Publications: | 1 | Organism: | Chlorocebus Aethiops | |
| + | BKM120 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | AS-605240 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | 3-methyladenine | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | PIK3R1 | up-regulates activity
binding
|
PIK3CG | 0.712 |
| Publications: | 1 | Organism: | Chlorocebus Aethiops | |
| + | 3-[2,4-diamino-7-(3-hydroxyphenyl)-6-pteridinyl]phenol | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | IC-87114 | down-regulates
chemical inhibition
|
PIK3CG | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |