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8GUB

Cryo-EM structure of cancer-specific PI3Kalpha mutant H1047R in complex with BYL-719

Functional Information from GO Data
ChainGOidnamespacecontents
A0001525biological_processangiogenesis
A0001889biological_processliver development
A0001944biological_processvasculature development
A0004674molecular_functionprotein serine/threonine kinase activity
A0004676molecular_function3-phosphoinositide-dependent protein kinase activity
A0004677molecular_functionDNA-dependent protein kinase activity
A0004679molecular_functionAMP-activated protein kinase activity
A0004694molecular_functioneukaryotic translation initiation factor 2alpha kinase activity
A0004711molecular_functionribosomal protein S6 kinase activity
A0005515molecular_functionprotein binding
A0005524molecular_functionATP binding
A0005737cellular_componentcytoplasm
A0005829cellular_componentcytosol
A0005886cellular_componentplasma membrane
A0005942cellular_componentphosphatidylinositol 3-kinase complex
A0005943cellular_componentphosphatidylinositol 3-kinase complex, class IA
A0005944cellular_componentphosphatidylinositol 3-kinase complex, class IB
A0006006biological_processglucose metabolic process
A0006629biological_processlipid metabolic process
A0006909biological_processphagocytosis
A0007173biological_processepidermal growth factor receptor signaling pathway
A0008286biological_processinsulin receptor signaling pathway
A0010468biological_processregulation of gene expression
A0010592biological_processpositive regulation of lamellipodium assembly
A0010629biological_processnegative regulation of gene expression
A0014704cellular_componentintercalated disc
A0014823biological_processresponse to activity
A0014870biological_processresponse to muscle inactivity
A0016242biological_processnegative regulation of macroautophagy
A0016301molecular_functionkinase activity
A0016303molecular_function1-phosphatidylinositol-3-kinase activity
A0030027cellular_componentlamellipodium
A0030036biological_processactin cytoskeleton organization
A0030168biological_processplatelet activation
A0030295molecular_functionprotein kinase activator activity
A0030835biological_processnegative regulation of actin filament depolymerization
A0031295biological_processT cell costimulation
A0032008biological_processpositive regulation of TOR signaling
A0032869biological_processcellular response to insulin stimulus
A0035005molecular_function1-phosphatidylinositol-4-phosphate 3-kinase activity
A0035175molecular_functionhistone H3S10 kinase activity
A0035402molecular_functionhistone H3T11 kinase activity
A0035403molecular_functionhistone H3T6 kinase activity
A0035979molecular_functionhistone H2AXS139 kinase activity
A0035994biological_processresponse to muscle stretch
A0036092biological_processphosphatidylinositol-3-phosphate biosynthetic process
A0038084biological_processvascular endothelial growth factor signaling pathway
A0040014biological_processregulation of multicellular organism growth
A0043201biological_processresponse to L-leucine
A0043276biological_processanoikis
A0043457biological_processregulation of cellular respiration
A0043491biological_processphosphatidylinositol 3-kinase/protein kinase B signal transduction
A0043524biological_processnegative regulation of neuron apoptotic process
A0043542biological_processendothelial cell migration
A0043560molecular_functioninsulin receptor substrate binding
A0044022molecular_functionhistone H3S28 kinase activity
A0044023molecular_functionhistone H4S1 kinase activity
A0044024molecular_functionhistone H2AS1 kinase activity
A0044025molecular_functionhistone H2BS14 kinase activity
A0046854biological_processphosphatidylinositol phosphate biosynthetic process
A0046934molecular_function1-phosphatidylinositol-4,5-bisphosphate 3-kinase activity
A0048009biological_processinsulin-like growth factor receptor signaling pathway
A0048015biological_processphosphatidylinositol-mediated signaling
A0048471cellular_componentperinuclear region of cytoplasm
A0048661biological_processpositive regulation of smooth muscle cell proliferation
A0050852biological_processT cell receptor signaling pathway
A0051897biological_processpositive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
A0055119biological_processrelaxation of cardiac muscle
A0060048biological_processcardiac muscle contraction
A0060612biological_processadipose tissue development
A0071333biological_processcellular response to glucose stimulus
A0071464biological_processcellular response to hydrostatic pressure
A0071548biological_processresponse to dexamethasone
A0072354molecular_functionhistone H3T3 kinase activity
A0072371molecular_functionhistone H2AS121 kinase activity
A0072518molecular_functionRho-dependent protein serine/threonine kinase activity
A0086003biological_processcardiac muscle cell contraction
A0097009biological_processenergy homeostasis
A0106310molecular_functionprotein serine kinase activity
A0110053biological_processregulation of actin filament organization
A0140823molecular_functionhistone H2BS36 kinase activity
A0140855molecular_functionhistone H3S57 kinase activity
A0140857molecular_functionhistone H3T45 kinase activity
A0141068biological_processautosome genomic imprinting
A1903544biological_processresponse to butyrate
A1905477biological_processpositive regulation of protein localization to membrane
A1990244molecular_functionhistone H2AT120 kinase activity
A2000270biological_processnegative regulation of fibroblast apoptotic process
A2000811biological_processnegative regulation of anoikis
B0001678biological_processintracellular glucose homeostasis
B0001784molecular_functionphosphotyrosine residue binding
B0001953biological_processnegative regulation of cell-matrix adhesion
B0002687biological_processpositive regulation of leukocyte migration
B0005068molecular_functiontransmembrane receptor protein tyrosine kinase adaptor activity
B0005158molecular_functioninsulin receptor binding
B0005159molecular_functioninsulin-like growth factor receptor binding
B0005168molecular_functionneurotrophin TRKA receptor binding
B0005515molecular_functionprotein binding
B0005634cellular_componentnucleus
B0005737cellular_componentcytoplasm
B0005801cellular_componentcis-Golgi network
B0005829cellular_componentcytosol
B0005886cellular_componentplasma membrane
B0005911cellular_componentcell-cell junction
B0005942cellular_componentphosphatidylinositol 3-kinase complex
B0005943cellular_componentphosphatidylinositol 3-kinase complex, class IA
B0006366biological_processtranscription by RNA polymerase II
B0006606biological_processprotein import into nucleus
B0006955biological_processimmune response
B0007162biological_processnegative regulation of cell adhesion
B0007165biological_processsignal transduction
B0008286biological_processinsulin receptor signaling pathway
B0008625biological_processextrinsic apoptotic signaling pathway via death domain receptors
B0008630biological_processintrinsic apoptotic signaling pathway in response to DNA damage
B0010592biological_processpositive regulation of lamellipodium assembly
B0015031biological_processprotein transport
B0016020cellular_componentmembrane
B0019209molecular_functionkinase activator activity
B0019221biological_processcytokine-mediated signaling pathway
B0019903molecular_functionprotein phosphatase binding
B0030183biological_processB cell differentiation
B0030217biological_processT cell differentiation
B0030316biological_processosteoclast differentiation
B0032760biological_processpositive regulation of tumor necrosis factor production
B0032869biological_processcellular response to insulin stimulus
B0033120biological_processpositive regulation of RNA splicing
B0034143biological_processregulation of toll-like receptor 4 signaling pathway
B0034446biological_processsubstrate adhesion-dependent cell spreading
B0034644biological_processcellular response to UV
B0034976biological_processresponse to endoplasmic reticulum stress
B0035014molecular_functionphosphatidylinositol 3-kinase regulator activity
B0035655biological_processinterleukin-18-mediated signaling pathway
B0036312molecular_functionphosphatidylinositol 3-kinase regulatory subunit binding
B0042267biological_processnatural killer cell mediated cytotoxicity
B0042307biological_processpositive regulation of protein import into nucleus
B0043066biological_processnegative regulation of apoptotic process
B0043125molecular_functionErbB-3 class receptor binding
B0043491biological_processphosphatidylinositol 3-kinase/protein kinase B signal transduction
B0043548molecular_functionphosphatidylinositol 3-kinase binding
B0043559molecular_functioninsulin binding
B0043560molecular_functioninsulin receptor substrate binding
B0045671biological_processnegative regulation of osteoclast differentiation
B0045944biological_processpositive regulation of transcription by RNA polymerase II
B0046326biological_processpositive regulation of D-glucose import
B0046854biological_processphosphatidylinositol phosphate biosynthetic process
B0046935molecular_function1-phosphatidylinositol-3-kinase regulator activity
B0046982molecular_functionprotein heterodimerization activity
B0048009biological_processinsulin-like growth factor receptor signaling pathway
B0048471cellular_componentperinuclear region of cytoplasm
B0048661biological_processpositive regulation of smooth muscle cell proliferation
B0050821biological_processprotein stabilization
B0051491biological_processpositive regulation of filopodium assembly
B0051492biological_processregulation of stress fiber assembly
B0051497biological_processnegative regulation of stress fiber assembly
B0052742molecular_functionphosphatidylinositol kinase activity
B0060396biological_processgrowth hormone receptor signaling pathway
B0061470biological_processT follicular helper cell differentiation
B0097529biological_processmyeloid leukocyte migration
B0120183biological_processpositive regulation of focal adhesion disassembly
B0140767molecular_functionenzyme-substrate adaptor activity
B0141038molecular_functionphosphatidylinositol 3-kinase activator activity
B1900103biological_processpositive regulation of endoplasmic reticulum unfolded protein response
B1903076biological_processregulation of protein localization to plasma membrane
B1903078biological_processpositive regulation of protein localization to plasma membrane
B1990578cellular_componentperinuclear endoplasmic reticulum membrane
Functional Information from PROSITE/UniProt
site_idPS00915
Number of Residues15
DetailsPI3_4_KINASE_1 Phosphatidylinositol 3- and 4-kinases signature 1. FKng.DDLRQDmltlQ
ChainResidueDetails
APHE801-GLN815

site_idPS00916
Number of Residues21
DetailsPI3_4_KINASE_2 Phosphatidylinositol 3- and 4-kinases signature 2. ScAgycVatFILgIgDRHnsN
ChainResidueDetails
ASER900-ASN920

Functional Information from SwissProt/UniProt
site_idSWS_FT_FI1
Number of Residues2
DetailsMOD_RES: Phosphoserine => ECO:0007744|PubMed:23186163
ChainResidueDetails
BSER154
BSER279

site_idSWS_FT_FI2
Number of Residues1
DetailsMOD_RES: Phosphotyrosine => ECO:0000250|UniProtKB:P26450
ChainResidueDetails
BTYR467

site_idSWS_FT_FI3
Number of Residues1
DetailsMOD_RES: Phosphotyrosine => ECO:0007744|PubMed:19369195
ChainResidueDetails
BTYR580

site_idSWS_FT_FI4
Number of Residues1
DetailsMOD_RES: Phosphoserine => ECO:0000250|UniProtKB:P23727
ChainResidueDetails
BSER608

227111

PDB entries from 2024-11-06

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