Entry Database : PDB / ID : 6gvh Structure visualization Downloads & linksTitle Crystal structure of PI3K alpha in complex with 3-(2-Amino-benzooxazol-5-yl)-4-chloro-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-6-ylamine ComponentsPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Details Keywords TRANSFERASE / LIPID KINASE / INHIBITOR / PI3K ALPHA / TRANSFERASE-TRANSFERASE INHIBITOR COMPLEX / TRANSFERASE-TRANSFERASE REGULATOR COMPLEXFunction / homology Function and homology informationFunction Domain/homology Component
response to muscle inactivity / negative regulation of actin filament depolymerization / response to L-leucine / regulation of actin filament organization / response to butyrate / IRS-mediated signalling / cellular response to hydrostatic pressure / autosome genomic imprinting / PI3K events in ERBB4 signaling / Activated NTRK2 signals through PI3K ... response to muscle inactivity / negative regulation of actin filament depolymerization / response to L-leucine / regulation of actin filament organization / response to butyrate / IRS-mediated signalling / cellular response to hydrostatic pressure / autosome genomic imprinting / PI3K events in ERBB4 signaling / Activated NTRK2 signals through PI3K / positive regulation of protein localization to membrane / Activated NTRK3 signals through PI3K / negative regulation of fibroblast apoptotic process / phosphatidylinositol 3-kinase complex, class IB / vasculature development / regulation of cellular respiration / Signaling by cytosolic FGFR1 fusion mutants / cardiac muscle cell contraction / phosphatidylinositol 3-kinase complex, class IA / phosphatidylinositol 3-kinase complex / Nephrin family interactions / relaxation of cardiac muscle / anoikis / Signaling by LTK in cancer / Costimulation by the CD28 family / 1-phosphatidylinositol-4-phosphate 3-kinase activity / 1-phosphatidylinositol-4,5-bisphosphate 3-kinase activity / Signaling by LTK / MET activates PI3K/AKT signaling / phosphatidylinositol-4,5-bisphosphate 3-kinase / PI3K/AKT activation / phosphatidylinositol 3-kinase / vascular endothelial growth factor signaling pathway / phosphatidylinositol-3-phosphate biosynthetic process / 1-phosphatidylinositol-3-kinase activity / Signaling by ALK / negative regulation of macroautophagy / PI-3K cascade:FGFR3 / Erythropoietin activates Phosphoinositide-3-kinase (PI3K) / PI-3K cascade:FGFR2 / protein kinase activator activity / PI-3K cascade:FGFR4 / response to dexamethasone / PI-3K cascade:FGFR1 / Synthesis of PIPs at the plasma membrane / phosphatidylinositol-mediated signaling / CD28 dependent PI3K/Akt signaling / phosphatidylinositol phosphate biosynthetic process / PI3K events in ERBB2 signaling / intercalated disc / negative regulation of anoikis / RET signaling / insulin receptor substrate binding / Interleukin-3, Interleukin-5 and GM-CSF signaling / regulation of multicellular organism growth / PI3K Cascade / endothelial cell migration / positive regulation of TOR signaling / RAC2 GTPase cycle / GAB1 signalosome / Role of phospholipids in phagocytosis / adipose tissue development / Role of LAT2/NTAL/LAB on calcium mobilization / Interleukin receptor SHC signaling / positive regulation of lamellipodium assembly / Signaling by PDGFRA transmembrane, juxtamembrane and kinase domain mutants / Signaling by PDGFRA extracellular domain mutants / phagocytosis / Signaling by FGFR4 in disease / cardiac muscle contraction / energy homeostasis / Signaling by FLT3 ITD and TKD mutants / Signaling by FGFR3 in disease / Tie2 Signaling / GPVI-mediated activation cascade / phosphorylation / Signaling by FGFR2 in disease / T cell costimulation / RAC1 GTPase cycle / response to muscle stretch / Signaling by FLT3 fusion proteins / FLT3 Signaling / Signaling by FGFR1 in disease / phosphatidylinositol 3-kinase/protein kinase B signal transduction / Downstream signal transduction / Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants / insulin-like growth factor receptor signaling pathway / liver development / response to activity / Regulation of signaling by CBL / cellular response to glucose stimulus / positive regulation of smooth muscle cell proliferation / regulation of protein phosphorylation / Constitutive Signaling by EGFRvIII / Signaling by ERBB2 ECD mutants / Signaling by SCF-KIT / epidermal growth factor receptor signaling pathway / Signaling by ERBB2 KD Mutants / platelet activation / VEGFA-VEGFR2 Pathway Similarity search - Function PI3Kalpha, catalytic domain / PI3-kinase family, p85-binding domain / PI3-kinase family, p85-binding domain / Phosphatidylinositol 3-kinase, adaptor-binding domain / Phosphatidylinositol 3-kinase adaptor-binding (PI3K ABD) domain profile. / PI3-kinase family, Ras-binding domain / Phosphatidylinositol 3-kinase Ras-binding (PI3K RBD) domain / Phosphatidylinositol 3-kinase Ras-binding (PI3K RBD) domain profile. / PI3-kinase family, ras-binding domain / Phosphoinositide 3-kinase, region postulated to contain C2 domain ... PI3Kalpha, catalytic domain / PI3-kinase family, p85-binding domain / PI3-kinase family, p85-binding domain / Phosphatidylinositol 3-kinase, adaptor-binding domain / Phosphatidylinositol 3-kinase adaptor-binding (PI3K ABD) domain profile. / PI3-kinase family, Ras-binding domain / Phosphatidylinositol 3-kinase Ras-binding (PI3K RBD) domain / Phosphatidylinositol 3-kinase Ras-binding (PI3K RBD) domain profile. / PI3-kinase family, ras-binding domain / Phosphoinositide 3-kinase, region postulated to contain C2 domain / C2 phosphatidylinositol 3-kinase-type domain / C2 phosphatidylinositol 3-kinase (PI3K)-type domain profile. / Phosphoinositide 3-kinase, accessory (PIK) domain superfamily / Phosphoinositide 3-kinase C2 / Phosphoinositide 3-kinase family, accessory domain (PIK domain) / Phosphoinositide 3-kinase family, accessory domain (PIK domain) / Phosphoinositide 3-kinase, accessory (PIK) domain / Phosphatidylinositol kinase / PIK helical domain profile. / Phosphatidylinositol 3- and 4-kinases signature 1. / Phosphatidylinositol 3/4-kinase, conserved site / Phosphatidylinositol 3- and 4-kinases signature 2. / Phosphatidylinositol 3-/4-kinase, catalytic domain superfamily / Phosphoinositide 3-kinase, catalytic domain / Phosphatidylinositol 3- and 4-kinases catalytic domain profile. / Phosphatidylinositol 3-/4-kinase, catalytic domain / Phosphatidylinositol 3- and 4-kinase / C2 domain superfamily / Armadillo-type fold / Ubiquitin-like domain superfamily / Protein kinase-like domain superfamily Similarity search - Domain/homologyBiological species Homo sapiens (human)Method X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution : 2.74 Å DetailsAuthors Ouvry, G. / Aurelly, M. / Bonnary, L. / Borde, E. / Bouix-Peter, C. / Chantalat, L. / Clary, L. / Defoin-Platel, C. / Deret, S. / Forissier, M. ...Ouvry, G. / Aurelly, M. / Bonnary, L. / Borde, E. / Bouix-Peter, C. / Chantalat, L. / Clary, L. / Defoin-Platel, C. / Deret, S. / Forissier, M. / Harris, C.S. / Isabet, T. / Lamy, L. / Luzy, A.P. / Pascau, J. / Soulet, C. / Taddei, A. / Taquet, N. / Tomas, L. / Thoreau, E. / Varvier, E. / Vial, E. / Hennequin, L.F. CitationJournal : Acs Med.Chem.Lett. / Year : 2019Title : Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors.Authors: Ouvry, G. / Clary, L. / Tomas, L. / Aurelly, M. / Bonnary, L. / Borde, E. / Bouix-Peter, C. / Chantalat, L. / Defoin-Platel, C. / Deret, S. / Forissier, M. / Harris, C.S. / Isabet, T. / ... Authors : Ouvry, G. / Clary, L. / Tomas, L. / Aurelly, M. / Bonnary, L. / Borde, E. / Bouix-Peter, C. / Chantalat, L. / Defoin-Platel, C. / Deret, S. / Forissier, M. / Harris, C.S. / Isabet, T. / Lamy, L. / Luzy, A.P. / Pascau, J. / Soulet, C. / Taddei, A. / Taquet, N. / Thoreau, E. / Varvier, E. / Vial, E. / Hennequin, L.F. History Deposition Jun 21, 2018 Deposition site : PDBE / Processing site : PDBERevision 1.0 Oct 2, 2019 Provider : repository / Type : Initial releaseRevision 1.1 Dec 4, 2019 Group : Database references / Category : citation / citation_authorItem : _citation.country / _citation.journal_abbrev ... _citation.country / _citation.journal_abbrev / _citation.journal_id_CSD / _citation.journal_id_ISSN / _citation.journal_volume / _citation.page_first / _citation.page_last / _citation.pdbx_database_id_DOI / _citation.pdbx_database_id_PubMed / _citation.title / _citation.year / _citation_author.name Revision 1.2 May 15, 2024 Group : Advisory / Data collection / Database referencesCategory : chem_comp_atom / chem_comp_bond ... chem_comp_atom / chem_comp_bond / database_2 / pdbx_unobs_or_zero_occ_atoms Item : _database_2.pdbx_DOI / _database_2.pdbx_database_accession
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