Protein family
Protein sequence
Protein function
Catalytic activity
EC number
EC number description
2.7.1.137
Transferases;
Transferring phosphorus-containing groups;
Phosphotransferases with an alcohol group as acceptor;
phosphatidylinositol 3-kinase
2.7.1.153
Transferases;
Transferring phosphorus-containing groups;
Phosphotransferases with an alcohol group as acceptor;
phosphatidylinositol-4,5-bisphosphate 3-kinase
2.7.1.154
Transferases;
Transferring phosphorus-containing groups;
Phosphotransferases with an alcohol group as acceptor;
phosphatidylinositol-4-phosphate 3-kinase
2.7.11.1
Transferases;
Transferring phosphorus-containing groups;
Protein-serine/threonine kinases;
non-specific serine/threonine protein kinase
PDB | Resolution (Å) | PDB name |
---|---|---|
1E8Y | 2.0 | Structure determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin and staurosporine |
1E8Z | 2.4 | Structure determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin and staurosporine |
1HE8 | 3.0 | Ras G12V - PI 3-kinase gamma complex |
2A4Z | 2.9 | Crystal Structure of human PI3Kgamma complexed with AS604850 |
2A5U | 2.7 | Crystal Structure of human PI3Kgamma complexed with AS605240 |
2CHW | 2.6 | A pharmacological map of the PI3-K family defines a role for p110 alpha in signaling: The structure of complex of phosphoinositide 3- kinase gamma with inhibitor PIK-39 |
2CHX | 2.5 | A pharmacological map of the PI3-K family defines a role for p110alpha in signaling: The structure of complex of phosphoinositide 3-kinase gamma with inhibitor PIK-90 |
2CHZ | 2.6 | A pharmacological map of the PI3-K family defines a role for p110alpha in signaling: The structure of complex of phosphoinositide 3-kinase gamma with inhibitor PIK-93 |
2V4L | 2.5 | complex of human phosphoinositide 3-kinase catalytic subunit gamma (p110 gamma) with PIK-284 |
3APC | 2.544 | Crystal structure of human PI3K-gamma in complex with CH5132799 |
3APD | 2.55 | Crystal structure of human PI3K-gamma in complex with CH5108134 |
3APF | 2.82 | Crystal structure of human PI3K-gamma in complex with CH5039699 |
3CSF | 2.8 | Crystal structure of PI3K p110gamma catalytical domain in complex with organoruthenium inhibitor DW2 |
3CST | 3.2 | Crystal structure of PI3K p110gamma catalytical domain in complex with organoruthenium inhibitor E5E2 |
3DBS | 2.8 | Structure of PI3K gamma in complex with GDC0941 |
3DPD | 2.85 | Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-Dihydro-2H-benzo[1,4]oxazines |
3ENE | 2.4 | Complex of PI3K gamma with an inhibitor |
3IBE | 2.798 | Crystal Structure of a Pyrazolopyrimidine Inhibitor Bound to PI3 Kinase Gamma |
3L08 | 2.7 | Structure of Pi3K gamma with a potent inhibitor: GSK2126458 |
3L13 | 3.0 | Crystal Structures of Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors |
3L16 | 2.9 | Discovery of (thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer |
3L17 | 3.0 | Discovery of (thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer |
3L54 | 2.3 | Structure of Pi3K gamma with inhibitor |
3LJ3 | 2.43 | PI3-kinase-gamma with a pyrrolopyridine-benzofuran inhibitor |
3MJW | 2.87 | PI3 Kinase gamma with a benzofuranone inhibitor |
3ML8 | 2.7 | Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04691502 through Structure Based Drug Design |
3ML9 | 2.55 | Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04691502 through Structure Based Drug Design |
3NZS | 2.75 | Structure-based Optimization of Pyrazolo -Pyrimidine and -Pyridine Inhibitors of PI3-Kinase |
3NZU | 2.6 | Structure-based Optimization of Pyrazolo -Pyrimidine and -Pyridine Inhibitors of PI3-Kinase |
3OAW | 2.75 | 4-Methylpteridineones as Orally Active and Selective PI3K/mTOR Dual Inhibitors |
3P2B | 3.2 | Crystal Structure of PI3K gamma with 3-(2-morpholino-6-(pyridin-3-ylamino)pyrimidin-4-yl)phenol |
3PRE | 2.91 | Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors. |
3PRZ | 2.6 | Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors. |
3PS6 | 2.6 | Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors. |
3QAQ | 2.9 | Crystal structure of PI3K-gamma in complex with triazine-benzimidazole 1 |
3QAR | 2.65 | Crystal structure of PI3K-gamma in complex with triazine-benzimidazole 32 |
3QJZ | 2.9 | Crystal structure of PI3K-gamma in complex with benzothiazole 1 |
3QK0 | 2.85 | Crystal structure of PI3K-gamma in complex with benzothiazole 82 |
3R7Q | 2.5 | Structure-based design of thienobenzoxepin inhibitors of PI3- kinase |
3R7R | 2.9 | Structure-based design of thienobenzoxepin inhibitors of PI3-Kinase |
3S2A | 2.55 | Crystal structure of PI3K-gamma in complex with a quinoline inhibitor |
3SD5 | 3.2 | Crystal Structure of PI3K gamma with 5-(2,4-dimorpholinopyrimidin-6-yl)-4-(trifluoromethyl)pyridin-2-amine |
3T8M | 2.5 | Rational Design of PI3K-alpha Inhibitors that Exhibit Selectivity Over the PI3K-beta Isoform |
3TJP | 2.7 | Crystal Structure of PI3K gamma with N6-(3,4-dimethoxyphenyl)-2-morpholino-[4,5'-bipyrimidine]-2',6-diamine |
3TL5 | 2.788 | Discovery of GDC-0980: a Potent, Selective, and Orally Available Class I Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor for the Treatment of Cancer |
3ZVV | 2.5 | Fragment Bound to PI3Kinase gamma |
3ZW3 | 2.8 | Fragment based discovery of a novel and selective PI3 Kinase inhibitor |
4ANU | 2.81 | Complexes of PI3Kgamma with isoform selective inhibitors. |
4ANV | 2.13 | Complexes of PI3Kgamma with isoform selective inhibitors. |
4ANW | 2.31 | Complexes of PI3Kgamma with isoform selective inhibitors. |
4ANX | 2.73 | Complexes of PI3Kgamma with isoform selective inhibitors. |
4AOF | 3.3 | Selective small molecule inhibitor discovered by chemoproteomic assay platform reveals regulation of Th17 cell differentiation by PI3Kgamma |
4DK5 | 2.95 | Crystal structure of human PI3K-gamma in complex with a pyridyl-triazine inhibitor |
4EZJ | 2.67 | Potent and Selective Inhibitors of PI3K-delta: Obtaining Isoform Selectivity from the Affinity Pocket and Tryptophan Shelf |
4EZK | 2.803 | Potent and Selective Inhibitors of PI3K-delta: Obtaining Isoform Selectivity from the Affinity Pocket and Tryptophan Shelf |
4EZL | 2.94 | Potent and Selective Inhibitors of PI3K-delta: Obtaining Isoform Selectivity from the Affinity Pocket and Tryptophan Shelf |
4F1S | 3.0 | Crystal structure of human PI3K-gamma in complex with a pyridyl-triazine-sulfonamide inhibitor |
4FA6 | 2.7 | Design and Synthesis of a Novel Pyrrolidinyl Pyrido Pyrimidinone Derivative as a Potent Inhibitor of PI3Ka and mTOR |
4FAD | 2.7 | Design and Synthesis of a Novel Pyrrolidinyl Pyrido Pyrimidinone Derivative as a Potent Inhibitor of PI3Ka and mTOR |
4FHJ | 2.6 | Crystal Structure of PI3K-gamma in Complex with Imidazopyridine 2 |
4FHK | 3.0 | Crystal Structure of PI3K-gamma in Complex with Imidazopyridazine 19e |
4FJY | 2.9 | Crystal structure of PI3K-gamma in complex with quinoline-indoline inhibitor 24f |
4FJZ | 3.0 | Crystal structure of PI3K-gamma in complex with pyrrolo-pyridine inhibitor 63 |
4FLH | 2.6 | Crystal structure of human PI3K-gamma in complex with AMG511 |
4FUL | 2.47 | PI3 Kinase Gamma bound to a pyrmidine inhibitor |
4G11 | 3.4 | X-ray structure of PI3K-gamma bound to a 4-(morpholin-4-yl)- (6-oxo-1,6-dihydropyrimidin-2-yl)amide inhibitor |
4GB9 | 2.438 | Potent and Highly Selective Benzimidazole Inhibitors of PI3K-delta |
4HLE | 2.78 | Compound 21 (1-alkyl-substituted 1,2,4-triazoles) |
4HVB | 2.35 | Catalytic unit of PI3Kg in complex with PI3K/mTOR dual inhibitor PF-04979064 |
4J6I | 2.9 | Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase beta isoform |
4KZ0 | 2.87 | Structure of PI3K gamma with Imidazopyridine inhibitors |
4KZC | 3.25 | Structure of PI3K gamma with Imidazopyridine inhibitors |
4PS3 | 2.9 | Structure of PI3K gamma in complex with 1-[6-(5-methoxypyridin-3-yl)-1,3-benzothiazol-2-yl]-3-[2-(1-propyl-1H-imidazol-4-yl)ethyl]urea |
4PS7 | 2.69 | Structure of PI3K gamma in complex with N-[6-(pyridin-3-yl)-1,3-benzothiazol-2-yl]acetamide |
4PS8 | 2.99 | Structure of PI3K gamma in complex with N-[6-(5,6-dimethoxypyridin-3-yl)-1,3-benzothiazol-2-yl]acetamide |
4URK | 2.9 | PI3Kg in complex with AZD6482 |
4WWN | 2.7 | Crystal structure of human PI3K-gamma in complex with (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine AMG319 inhibitor |
4WWO | 2.3 | Crystal structure of human PI3K-gamma in complex with phenylquinoline inhibitor N-{(1S)-1-[8-chloro-2-(3-fluorophenyl)quinolin-3-yl]ethyl}-9H-purin-6-amine |
4WWP | 2.4 | Crystal structure of human PI3K-gamma in complex with pyridinylquinoline inhibitor N-{(1S)-1-[8-chloro-2-(2-methylpyridin-3-yl)quinolin-3-yl]ethyl}-9H-purin-6-amine |
4XX5 | 2.76 | Structure of PI3K gamma in complex with an inhibitor |
4XZ4 | 2.6 | Structure of PI3K gamma in complex with an inhibitor |
5EDS | 2.8 | Crystal structure of human PI3K-gamma in complex with benzimidazole inhibitor 5 |
5G2N | 2.68 | X-ray structure of PI3Kinase Gamma in complex with Copanlisib |
5G55 | 2.45 | 3-Quinoline Carboxamides inhibitors of Pi3K |
5JHA | 2.51 | Structure of Phosphoinositide 3-kinase gamma (PI3K) bound to the potent inhibitor PIKin2 |
5JHB | 2.48 | Structure of Phosphoinositide 3-kinase gamma (PI3K) bound to the potent inhibitor PIKin3 |
5KAE | 2.65 | Crystal structure of human PI3K-gamma in complex with quinoline-containing inhibitor 5g |
5OQ4 | 2.7 | PQR309 - a Potent, Brain-Penetrant, Orally Bioavailable, pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology |
5T23 | 2.78 | PI3Kg IN COMPLEX WITH 5d |
6AUD | 2.015 | PI3K-gamma K802T in complex with Cpd 8 10-((1-(tert-butyl)piperidin-4-yl)sulfinyl)-2-(1-isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepine |
6C1S | 2.31 | Phosphoinositide 3-Kinase gamma bound to an pyrrolopyridinone Inhibitor |
6FH5 | 2.84 | PI3Kg IN COMPLEX WITH Compound 7 |
6GQ7 | 2.84 | PI3Kg IN COMPLEX WITH INH |
6T3B | 3.01 | Crystal structure of PI3Kgamma with a dihydropurinone inhibitor (compound 4) |
6T3C | 2.62 | Crystal structure of PI3Kgamma in complex with DNA-PK inhibitor AZD7648 |
6XRL | 2.99 | Crystal structure of human PI3K-gamma in complex with inhibitor IPI-549 |
6XRM | 2.88 | Crystal structure of human PI3K-gamma in complex with Compound 4 |
6XRN | 2.96 | Crystal structure of human PI3K-gamma in complex with Compound 17 |
7JWE | 2.55 | Gedatolisib bound to the PI3Kg catalytic subunit p110 gamma |
7JWZ | 2.65 | IPI-549 bound to the PI3Kg catalytic subunit p110 gamma |
7JX0 | 3.15 | NVS-PI3-4 bound to the PI3Kg catalytic subunit p110 gamma |
7KKE | 2.81 | Phosphoinositide 3-Kinase gamma bound to a thiazole inhibitor |
7MEZ | 2.89 | Structure of the phosphoinositide 3-kinase p110 gamma (PIK3CG) p101 (PIK3R5) complex |
7Z61 | 2.738 | Crystal structure of PI3Kgamma with a dihydropurinone inhibitor (compound 18) |
GO ontology
|
GO term | GO description |
---|---|---|
Biological Process | GO:0007186 | G protein-coupled receptor signaling pathway |
Biological Process | GO:0042110 | T cell activation |
Biological Process | GO:0010818 | T cell chemotaxis |
Biological Process | GO:0042098 | T cell proliferation |
Biological Process | GO:0002250 | adaptive immune response |
Biological Process | GO:0001525 | angiogenesis |
Biological Process | GO:0016477 | cell migration |
Biological Process | GO:0071320 | cellular response to cAMP |
Biological Process | GO:0002407 | dendritic cell chemotaxis |
Biological Process | GO:0006897 | endocytosis |
Biological Process | GO:0097284 | hepatocyte apoptotic process |
Biological Process | GO:0006955 | immune response |
Biological Process | GO:0006954 | inflammatory response |
Biological Process | GO:0045087 | innate immune response |
Biological Process | GO:0043303 | mast cell degranulation |
Biological Process | GO:0035747 | natural killer cell chemotaxis |
Biological Process | GO:0055118 | negative regulation of cardiac muscle contraction |
Biological Process | GO:2000270 | negative regulation of fibroblast apoptotic process |
Biological Process | GO:0010897 | negative regulation of triglyceride catabolic process |
Biological Process | GO:0030593 | neutrophil chemotaxis |
Biological Process | GO:0072672 | neutrophil extravasation |
Biological Process | GO:0014065 | phosphatidylinositol 3-kinase signaling |
Biological Process | GO:0046854 | phosphatidylinositol phosphate biosynthetic process |
Biological Process | GO:0036092 | phosphatidylinositol-3-phosphate biosynthetic process |
Biological Process | GO:0016310 | phosphorylation |
Biological Process | GO:0070527 | platelet aggregation |
Biological Process | GO:0043406 | positive regulation of MAP kinase activity |
Biological Process | GO:0035022 | positive regulation of Rac protein signal transduction |
Biological Process | GO:0002675 | positive regulation of acute inflammatory response |
Biological Process | GO:0001819 | positive regulation of cytokine production |
Biological Process | GO:0007204 | positive regulation of cytosolic calcium ion concentration |
Biological Process | GO:0010595 | positive regulation of endothelial cell migration |
Biological Process | GO:0051897 | positive regulation of protein kinase B signaling |
Biological Process | GO:0006468 | protein phosphorylation |
Biological Process | GO:0045765 | regulation of angiogenesis |
Biological Process | GO:1903169 | regulation of calcium ion transmembrane transport |
Biological Process | GO:0033628 | regulation of cell adhesion mediated by integrin |
Biological Process | GO:0002679 | respiratory burst involved in defense response |
Biological Process | GO:0032252 | secretory granule localization |
Biological Process | GO:0003376 | sphingosine-1-phosphate receptor signaling pathway |
Molecular Function | GO:0016303 | 1-phosphatidylinositol-3-kinase activity |
Molecular Function | GO:0035005 | 1-phosphatidylinositol-4-phosphate 3-kinase activity |
Molecular Function | GO:0005524 | ATP binding |
Molecular Function | GO:0046875 | ephrin receptor binding |
Molecular Function | GO:0042802 | identical protein binding |
Molecular Function | GO:0016301 | kinase activity |
Molecular Function | GO:0035004 | phosphatidylinositol 3-kinase activity |
Molecular Function | GO:0052812 | phosphatidylinositol-3,4-bisphosphate 5-kinase activity |
Molecular Function | GO:0046934 | phosphatidylinositol-4,5-bisphosphate 3-kinase activity |
Molecular Function | GO:0004672 | protein kinase activity |
Molecular Function | GO:0106310 | protein serine kinase activity |
Molecular Function | GO:0004674 | protein serine/threonine kinase activity |
Cellular Component | GO:0005737 | cytoplasm |
Cellular Component | GO:0005829 | cytosol |
Cellular Component | GO:0016020 | membrane |
Cellular Component | GO:0005943 | phosphatidylinositol 3-kinase complex, class IA |
Cellular Component | GO:0005944 | phosphatidylinositol 3-kinase complex, class IB |
Cellular Component | GO:0005886 | plasma membrane |
InterPro
|
InterPro name |
---|---|
IPR000341 | Phosphatidylinositol 3-kinase Ras-binding (PI3K RBD) domain |
IPR000403 | Phosphatidylinositol 3-/4-kinase, catalytic domain |
IPR001263 | Phosphoinositide 3-kinase, accessory (PIK) domain |
IPR002420 | C2 phosphatidylinositol 3-kinase-type domain |
IPR003113 | Phosphatidylinositol 3-kinase, adaptor-binding domain |
IPR011009 | Protein kinase-like domain superfamily |
IPR015433 | Phosphatidylinositol kinase |
IPR016024 | Armadillo-type fold |
IPR018936 | Phosphatidylinositol 3/4-kinase, conserved site |
IPR029071 | Ubiquitin-like domain superfamily |
IPR035892 | C2 domain superfamily |
IPR036940 | Phosphatidylinositol 3-/4-kinase, catalytic domain superfamily |
IPR042236 | Phosphoinositide 3-kinase, accessory (PIK) domain superfamily |
IPR045580 | PIK3 catalytic subunit gamma, adaptor-binding domain |
Pfam
|
Pfam name |
---|---|
PF00454 | Phosphatidylinositol 3- and 4-kinase |
PF00613 | Phosphoinositide 3-kinase family, accessory domain (PIK domain) |
PF00792 | Phosphoinositide 3-kinase C2 |
PF00794 | PI3-kinase family, ras-binding domain |
PF19710 | PIK3 catalytic subunit gamma adaptor-binding domain |
Reactome
|
Reactome Name | Node type
|
Reactome Root | Reactome Root Name |
---|---|---|---|---|
R-HSA-114604 | GPVI-mediated activation cascade | Leaf | R-HSA-109582 | Hemostasis |
R-HSA-1660499 | Synthesis of PIPs at the plasma membrane | Leaf | R-HSA-1430728 | Metabolism |
R-HSA-392451 | G beta:gamma signalling through PI3Kgamma | Leaf | R-HSA-162582 | Signal Transduction |
R-HSA-9027276 | Erythropoietin activates Phosphoinositide-3-kinase (PI3K) | Leaf | R-HSA-162582 | Signal Transduction |
R-HSA-9680350 | Signaling by CSF1 (M-CSF) in myeloid cells | Leaf | R-HSA-168256 | Immune System |
Location
|
ECO term
|
Pubmed |
---|---|---|
Cell membrane | ECO:0000269 | PubMed:12163475 |
Cytoplasm | ECO:0000269 | PubMed:12163475 |
HPO ID
|
HPO name |
---|---|
HP:0000007 | Autosomal recessive inheritance |
HP:0000010 | Recurrent urinary tract infections |
HP:0000403 | Recurrent otitis media |
HP:0000964 | Eczema |
HP:0001252 | Hypotonia |
HP:0001433 | Hepatosplenomegaly |
HP:0001581 | Recurrent skin infections |
HP:0001742 | Nasal congestion |
HP:0001744 | Splenomegaly |
HP:0001873 | Thrombocytopenia |
HP:0001880 | Eosinophilia |
HP:0001888 | Lymphopenia |
HP:0001890 | Autoimmune hemolytic anemia |
HP:0001904 | Neutropenia in presence of anti-neutropil antibodies |
HP:0001945 | Fever |
HP:0002014 | Diarrhea |
HP:0002027 | Abdominal pain |
HP:0002155 | Hypertriglyceridemia |
HP:0002583 | Colitis |
HP:0002716 | Lymphadenopathy |
HP:0002720 | Decreased circulating IgA level |
HP:0002850 | Decreased circulating total IgM |
HP:0002851 | Elevated proportion of CD4-negative, CD8-negative, alpha-beta regulatory T cells |
HP:0003281 | Increased circulating ferritin concentration |
HP:0003621 | Juvenile onset |
HP:0003651 | Foam cells |
HP:0004313 | Decreased circulating antibody level |
HP:0004315 | Decreased circulating IgG level |
HP:0004387 | Enterocolitis |
HP:0005415 | Decreased proportion of CD8-positive T cells |
HP:0005425 | Recurrent sinopulmonary infections |
HP:0011945 | Bronchiolitis obliterans organizing pneumonia |
HP:0012156 | Hemophagocytosis |
HP:0012312 | Monocytopenia |
HP:0012378 | Fatigue |
HP:0020113 | Decreased proportion of CD4+CD25+ regulatory T cells |
HP:0025435 | Increased circulating lactate dehydrogenase concentration |
HP:0032252 | Granuloma |
HP:0040218 | Reduced natural killer cell count |
HP:0100721 | Mediastinal lymphadenopathy |
HP:0500266 | Decreased proportion of CD8-positive, alpha-beta TEMRA T cells |
Disease name | MONDO ID
|
ICD10
|
ICD10 chapter
|
OMIM
|
Orphanet
|
---|---|---|---|---|---|
immunodeficiency 97 with autoinflammation | MONDO:0030717 | - | - | OMIM:619802 |