5XGI
Crystal structure of PI3K complex with an inhibitor
Functional Information from GO Data
| Chain | GOid | namespace | contents |
| A | 0001944 | biological_process | vasculature development |
| A | 0004674 | molecular_function | protein serine/threonine kinase activity |
| A | 0005515 | molecular_function | protein binding |
| A | 0005737 | cellular_component | cytoplasm |
| A | 0005829 | cellular_component | cytosol |
| A | 0005886 | cellular_component | plasma membrane |
| A | 0005942 | cellular_component | phosphatidylinositol 3-kinase complex |
| A | 0005943 | cellular_component | phosphatidylinositol 3-kinase complex, class IA |
| A | 0005944 | cellular_component | phosphatidylinositol 3-kinase complex, class IB |
| A | 0007173 | biological_process | epidermal growth factor receptor signaling pathway |
| A | 0008286 | biological_process | insulin receptor signaling pathway |
| A | 0010592 | biological_process | positive regulation of lamellipodium assembly |
| A | 0010629 | biological_process | negative regulation of gene expression |
| A | 0014704 | cellular_component | intercalated disc |
| A | 0014823 | biological_process | response to activity |
| A | 0014870 | biological_process | response to muscle inactivity |
| A | 0016242 | biological_process | negative regulation of macroautophagy |
| A | 0016301 | molecular_function | kinase activity |
| A | 0016303 | molecular_function | 1-phosphatidylinositol-3-kinase activity |
| A | 0016477 | biological_process | cell migration |
| A | 0030027 | cellular_component | lamellipodium |
| A | 0030036 | biological_process | actin cytoskeleton organization |
| A | 0030168 | biological_process | platelet activation |
| A | 0030295 | molecular_function | protein kinase activator activity |
| A | 0030835 | biological_process | negative regulation of actin filament depolymerization |
| A | 0032008 | biological_process | positive regulation of TOR signaling |
| A | 0032869 | biological_process | cellular response to insulin stimulus |
| A | 0035005 | molecular_function | 1-phosphatidylinositol-4-phosphate 3-kinase activity |
| A | 0035994 | biological_process | response to muscle stretch |
| A | 0036092 | biological_process | phosphatidylinositol-3-phosphate biosynthetic process |
| A | 0038084 | biological_process | vascular endothelial growth factor signaling pathway |
| A | 0038203 | biological_process | TORC2 signaling |
| A | 0043201 | biological_process | response to L-leucine |
| A | 0043276 | biological_process | anoikis |
| A | 0043491 | biological_process | phosphatidylinositol 3-kinase/protein kinase B signal transduction |
| A | 0043542 | biological_process | endothelial cell migration |
| A | 0043560 | molecular_function | insulin receptor substrate binding |
| A | 0045860 | biological_process | positive regulation of protein kinase activity |
| A | 0046854 | biological_process | phosphatidylinositol phosphate biosynthetic process |
| A | 0046934 | molecular_function | 1-phosphatidylinositol-4,5-bisphosphate 3-kinase activity |
| A | 0048009 | biological_process | insulin-like growth factor receptor signaling pathway |
| A | 0048015 | biological_process | phosphatidylinositol-mediated signaling |
| A | 0048471 | cellular_component | perinuclear region of cytoplasm |
| A | 0048661 | biological_process | positive regulation of smooth muscle cell proliferation |
| A | 0050852 | biological_process | T cell receptor signaling pathway |
| A | 0051897 | biological_process | positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction |
| A | 0055119 | biological_process | relaxation of cardiac muscle |
| A | 0060048 | biological_process | cardiac muscle contraction |
| A | 0071464 | biological_process | cellular response to hydrostatic pressure |
| A | 0071548 | biological_process | response to dexamethasone |
| A | 0086003 | biological_process | cardiac muscle cell contraction |
| A | 0106310 | molecular_function | protein serine kinase activity |
| A | 0110053 | biological_process | regulation of actin filament organization |
| A | 1903544 | biological_process | response to butyrate |
| A | 1905477 | biological_process | positive regulation of protein localization to membrane |
| A | 2000811 | biological_process | negative regulation of anoikis |
Functional Information from PDB Data
| site_id | AC1 |
| Number of Residues | 11 |
| Details | binding site for residue 84R A 1101 |
| Chain | Residue |
| A | MET772 |
| A | ILE932 |
| A | ASP933 |
| A | LYS802 |
| A | ASP810 |
| A | TYR836 |
| A | ILE848 |
| A | GLU849 |
| A | VAL850 |
| A | VAL851 |
| A | SER854 |
| site_id | AC2 |
| Number of Residues | 6 |
| Details | binding site for residue P6G A 1102 |
| Chain | Residue |
| A | GLU259 |
| A | TYR272 |
| A | ARG281 |
| A | ARG832 |
| A | ASP926 |
| A | GOL1104 |
| site_id | AC3 |
| Number of Residues | 3 |
| Details | binding site for residue GOL A 1104 |
| Chain | Residue |
| A | GLY280 |
| A | ARG281 |
| A | P6G1102 |
| site_id | AC4 |
| Number of Residues | 1 |
| Details | binding site for residue GOL A 1105 |
| Chain | Residue |
| A | TRP386 |
| site_id | AC5 |
| Number of Residues | 8 |
| Details | binding site for residue SO4 B 601 |
| Chain | Residue |
| A | ARG537 |
| B | ARG340 |
| B | ARG358 |
| B | ALA360 |
| B | SER361 |
| B | MET364 |
| B | THR369 |
| B | LYS382 |
| site_id | AC6 |
| Number of Residues | 3 |
| Details | binding site for residue SO4 B 602 |
| Chain | Residue |
| A | GLY451 |
| A | LEU452 |
| B | TYR463 |
Functional Information from PROSITE/UniProt
| site_id | PS00915 |
| Number of Residues | 15 |
| Details | PI3_4_KINASE_1 Phosphatidylinositol 3- and 4-kinases signature 1. FKng.DDLRQDmltlQ |
| Chain | Residue | Details |
| A | PHE801-GLN815 |
| site_id | PS00916 |
| Number of Residues | 21 |
| Details | PI3_4_KINASE_2 Phosphatidylinositol 3- and 4-kinases signature 2. ScAgycVatFILgIgDRHnsN |
| Chain | Residue | Details |
| A | SER900-ASN920 |
Functional Information from SwissProt/UniProt
| site_id | SWS_FT_FI1 |
| Number of Residues | 89 |
| Details | Domain: {"description":"PI3K-ABD","evidences":[{"source":"PROSITE-ProRule","id":"PRU00877","evidenceCode":"ECO:0000255"}]} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI2 |
| Number of Residues | 177 |
| Details | Domain: {"description":"PIK helical","evidences":[{"source":"PROSITE-ProRule","id":"PRU00878","evidenceCode":"ECO:0000255"}]} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI3 |
| Number of Residues | 6 |
| Details | Region: {"description":"G-loop","evidences":[{"source":"PROSITE-ProRule","id":"PRU00269","evidenceCode":"ECO:0000255"}]} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI4 |
| Number of Residues | 8 |
| Details | Region: {"description":"Catalytic loop","evidences":[{"source":"PROSITE-ProRule","id":"PRU00269","evidenceCode":"ECO:0000255"}]} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI5 |
| Number of Residues | 26 |
| Details | Region: {"description":"Activation loop","evidences":[{"source":"PROSITE-ProRule","id":"PRU00269","evidenceCode":"ECO:0000255"}]} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI6 |
| Number of Residues | 1 |
| Details | Site: {"description":"Implicated in the recognition of ATP as well as PIP2. Also crucial for autophosphorylation of the p85alpha subunit","evidences":[{"source":"PubMed","id":"23936502","evidenceCode":"ECO:0000305"}]} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI7 |
| Number of Residues | 95 |
| Details | Domain: {"description":"SH2 1","evidences":[{"source":"PROSITE-ProRule","id":"PRU00191","evidenceCode":"ECO:0000255"}]} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI8 |
| Number of Residues | 1 |
| Details | Modified residue: {"description":"Phosphotyrosine","evidences":[{"source":"UniProtKB","id":"P26450","evidenceCode":"ECO:0000250"}]} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI9 |
| Number of Residues | 1 |
| Details | Modified residue: {"description":"Phosphotyrosine","evidences":[{"source":"PubMed","id":"19369195","evidenceCode":"ECO:0007744"}]} |
| Chain | Residue | Details |
