Structure of PDB 7pg6 Chain A
Receptor sequence
>7pg6A (length=1026) Species:
9606
(Homo sapiens) [
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PRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLITIKHELFKE
ARKYPLHQLLQDESSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVI
EPVGNREEKILNREIGFAIGMPVCEFDMVKDPEVQDFRRNILNVCKEAVD
LRDLNSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSPNN
DKQKYTLKINHDCVPEQVIAEAIRKKTRSKKLSSEQLKLCVLEYQGKYIL
KVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPMDCF
TMPSYSRRISTSTKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGIY
HGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKG
RKGAKEEHCPLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGV
TGSNPNKETPCLELEFDWFSSVVKFPDMSVIEEHANWSVLRENDKEQLKA
ISTRDPLSEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQM
YCLVKDWPPIKPEQAMELLDCNYPDPMVRGFAVRCLEKYLTDDKLSQYLI
QLVQVLKYEQYLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQR
FGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILKQEKKDETQKVQMK
FLVEQMRRPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLWLNW
ENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRM
LPYGCLSIGDCVGLIEVVRNSHTIMQIQCKGQFNSHTLHQWLKDKNKGEI
YDAAIDLFTRSCAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLD
HKKKKFGYKRERVPFVLTQDFLIVISKGAQECTKTREFERFQEMCYKAYL
AIRQHANLFINLFSMMLGSGMPELQSFDDIAYIRKTLALDKTEQEALEYF
MKQMNDAHHGGWTTKMDWIFHTIKQH
3D structure
PDB
7pg6
A small-molecule PI3K alpha activator for cardioprotection and neuroregeneration.
Chain
A
Resolution
2.49944 Å
3D
structure
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Enzymatic activity
Enzyme Commision number
2.7.11.1
: non-specific serine/threonine protein kinase.
2.7.1.137
: phosphatidylinositol 3-kinase.
2.7.1.153
: phosphatidylinositol-4,5-bisphosphate 3-kinase.
Interaction with ligand
Site
#
Ligand
Ligand
chain
Binding residues on receptor
(original residue number in PDB)
Binding residues on receptor
(residue number reindexed from 1)
Binding affinity
BS01
1LT
A
W780 I800 K802 Y836 V851 S854 Q859 M922 I932
W747 I767 K769 Y803 V818 S821 Q826 M883 I893
Gene Ontology
Molecular Function
GO:0004674
protein serine/threonine kinase activity
GO:0005515
protein binding
GO:0005524
ATP binding
GO:0016301
kinase activity
GO:0016303
1-phosphatidylinositol-3-kinase activity
GO:0030295
protein kinase activator activity
GO:0035005
1-phosphatidylinositol-4-phosphate 3-kinase activity
GO:0043560
insulin receptor substrate binding
GO:0044024
histone H2AS1 kinase activity
GO:0046934
1-phosphatidylinositol-4,5-bisphosphate 3-kinase activity
GO:0106310
protein serine kinase activity
Biological Process
GO:0001525
angiogenesis
GO:0001889
liver development
GO:0001944
vasculature development
GO:0006006
glucose metabolic process
GO:0006629
lipid metabolic process
GO:0006909
phagocytosis
GO:0007173
epidermal growth factor receptor signaling pathway
GO:0008286
insulin receptor signaling pathway
GO:0010468
regulation of gene expression
GO:0010592
positive regulation of lamellipodium assembly
GO:0010629
negative regulation of gene expression
GO:0014823
response to activity
GO:0014870
response to muscle inactivity
GO:0016242
negative regulation of macroautophagy
GO:0016310
phosphorylation
GO:0030036
actin cytoskeleton organization
GO:0030168
platelet activation
GO:0030835
negative regulation of actin filament depolymerization
GO:0031295
T cell costimulation
GO:0032008
positive regulation of TOR signaling
GO:0032869
cellular response to insulin stimulus
GO:0035994
response to muscle stretch
GO:0036092
phosphatidylinositol-3-phosphate biosynthetic process
GO:0038084
vascular endothelial growth factor signaling pathway
GO:0040014
regulation of multicellular organism growth
GO:0043201
response to L-leucine
GO:0043276
anoikis
GO:0043457
regulation of cellular respiration
GO:0043491
phosphatidylinositol 3-kinase/protein kinase B signal transduction
GO:0043524
negative regulation of neuron apoptotic process
GO:0043542
endothelial cell migration
GO:0046854
phosphatidylinositol phosphate biosynthetic process
GO:0048009
insulin-like growth factor receptor signaling pathway
GO:0048015
phosphatidylinositol-mediated signaling
GO:0048661
positive regulation of smooth muscle cell proliferation
GO:0050852
T cell receptor signaling pathway
GO:0051897
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
GO:0055119
relaxation of cardiac muscle
GO:0060048
cardiac muscle contraction
GO:0060612
adipose tissue development
GO:0071333
cellular response to glucose stimulus
GO:0071464
cellular response to hydrostatic pressure
GO:0071548
response to dexamethasone
GO:0086003
cardiac muscle cell contraction
GO:0097009
energy homeostasis
GO:0110053
regulation of actin filament organization
GO:0141068
autosome genomic imprinting
GO:1903544
response to butyrate
GO:1905477
positive regulation of protein localization to membrane
GO:2000270
negative regulation of fibroblast apoptotic process
GO:2000811
negative regulation of anoikis
Cellular Component
GO:0005737
cytoplasm
GO:0005829
cytosol
GO:0005886
plasma membrane
GO:0005942
phosphatidylinositol 3-kinase complex
GO:0005943
phosphatidylinositol 3-kinase complex, class IA
GO:0005944
phosphatidylinositol 3-kinase complex, class IB
GO:0014704
intercalated disc
GO:0030027
lamellipodium
GO:0048471
perinuclear region of cytoplasm
View graph for
Molecular Function
View graph for
Biological Process
View graph for
Cellular Component
External links
PDB
RCSB:7pg6
,
PDBe:7pg6
,
PDBj:7pg6
PDBsum
7pg6
PubMed
37225977
UniProt
P42336
|PK3CA_HUMAN Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (Gene Name=PIK3CA)
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