Structure of PDB 4xe0 Chain A

Receptor sequence
>4xe0A (length=815) Species: 10090 (Mus musculus) [Search protein sequence]
VKKLINSQISLLIGKGLHEFDSLRDPEVNDFRTKMRQFCEEAAAHRQQLG
WVEWLQYSFPLQLEPNRALLVNVKFEGSEESFTFQVSTKDMPLALMACAL
RKKATVFRQQPEEYALQVNGRHEYLYGNYPLCHFQYICSCLHSGLTPHLT
MVHSSSILAMRDEQSNLWSLEQPFSIELIEGRKVNAMKLVVQAGLFHGNE
MLCKTVSSSEVNVCSEPVWKQRLEFDISVCDLPRMARLCFALYAVVCPIA
WANLMLFDYKDQLKTGERCLYMWPSVLLNPAGTVRGNPNTESAAALVIYL
PEVAPVYFPALEKILELLREILEYEHEKDLVWKMRHEVQEHFPEALARLL
LVTKWNKHEDVAQMLYLLCSWPELPVLSALELLDFSFPDCYVGSFAIKSL
RKLTDDELFQYLLQLVQVLKYESYLDCELTKFLLGRALANRKIGHFLFWH
LRSEMHVPSVALRFGLIMEAYCRGSTHHMKVLMKQGEALSKLKALNDFVK
VSSQKTTKPQTKEMMHMCMRQETYMEALSHLQSPLDPSTLLEEVCVEQCT
FMDSKMKPLWIMYSSEEAGSAGNVGIIFKNGDDLRQDMLTLQMIQLMDVL
WKQEGLDLRMTPYGCLPTGDRTGLIEVVLHSDTIANIQLNKSNMAATAAF
NKDALLNWLKSKNPGEALDRAIEEFTLSCAGYCVATYVLGIGDRHSDNIM
IRESGQLFHIDFGHFLGNRVPFILTYDFVHVIQQGKTNNSEKFERFRGYC
ERAYTILRRHGLLFLHLFALMRAAGLPELSCSKDIQYLKDSLALGKTEEE
ALKHFRVKFNEALRE
3D structure
PDB4xe0 Structural, Biochemical, and Biophysical Characterization of Idelalisib Binding to Phosphoinositide 3-Kinase delta.
ChainA
Resolution2.434 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 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 40L A M752 P758 W760 I777 Y813 E826 V828 T833 N836 M900 I910 M552 P558 W560 I577 Y613 E626 V628 T633 N636 M700 I710 MOAD: ic50=19nM
PDBbind-CN: -logKd/Ki=7.72,IC50=19nM
Gene Ontology
Molecular Function
GO:0016301 kinase activity
GO:0016303 1-phosphatidylinositol-3-kinase activity
Biological Process
GO:0043491 phosphatidylinositol 3-kinase/protein kinase B signal transduction
GO:0046854 phosphatidylinositol phosphate biosynthetic process

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:4xe0, PDBe:4xe0, PDBj:4xe0
PDBsum4xe0
PubMed25631052
UniProtO35904|PK3CD_MOUSE Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Gene Name=Pik3cd)

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