Structure of PDB 4tv3 Chain A

Receptor sequence
>4tv3A (length=879) Species: 9606 (Homo sapiens) [Search protein sequence]
NREEKILNREIGFAIGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDL
NSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSPNNDKQK
YTLKINHDCVPEQVIAEAIRKKTRSMLYQGKYILKVCGCDEYFLEKYPLS
QYKYIRSCIMLGRMPNLMLMAKESLYSQLPMDCFTMPSYSRKSLWVINSA
LRIKILCATYVNVNDKIYVRTGIYHGGEPLCDNVNTQRVPCSNPRWNEWL
NYDIYIPDLPRAARLCLSICSVKEEHCPLAWGNINLFDYTDTLVSGKMAL
NLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWFSSVVKFPDMSVIE
EHANWSVSREAGFSYSHAGLSNRLARDNELRENDKEQLKAISTRDPLSEI
TEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPI
KPEQAMELLDCNYPDPMVRGFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQ
YLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCR
ACGMYLKHLNRQVEAMEKLINLTDILKQEKKDETQKVQMKFLVEQMRRPD
FMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLWLNWENPDIMSELL
FQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLSIGD
CVGLIEVVRNSHTIMQIQCKGFNSHTLHQWLKDKNKGEIYDAAIDLFTRS
CAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDRVPFVLTQDFL
IVISTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFD
DIAYIRKTLALDKTEQEALEYFMKQMNDA
3D structure
PDB4tv3 Engineering of an isolated p110 alpha subunit of PI3K alpha permits crystallization and provides a platform for structure-based drug design.
ChainA
Resolution2.85 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 ML9 A R770 I800 K802 D810 Y836 V851 Q859 M922 I932 D933 R627 I657 K659 D667 Y693 V708 Q716 M772 I782 D783 PDBbind-CN: -logKd/Ki=8.72,Kd=1.9nM
BindingDB: IC50=8.3nM,Ki=0.57nM
Gene Ontology
Molecular Function
GO:0016301 kinase activity
Biological Process
GO:0046854 phosphatidylinositol phosphate biosynthetic process

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:4tv3, PDBe:4tv3, PDBj:4tv3
PDBsum4tv3
PubMed25043846
UniProtP42336|PK3CA_HUMAN Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (Gene Name=PIK3CA)

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