Structure of PDB 4ezl Chain A

Receptor sequence
>4ezlA (length=834) Species: 9606 (Homo sapiens) [Search protein sequence]
MSEESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGLVTPRMAEVASRD
PKLYAMHPWVTSKPLPEYLWKKIANNCIFIVIHRSTTSQTIKVSPDDTPG
AILQSFFTKEQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNGEEIHVVL
DTPPDPALDEVRKCDRKFRVKIRGIDIPVLPRNTDLTVFVEANIQHGQQV
LCQRRTSPKPFTEEVLWNVWLEFSIKIKDLPKGALLNLQIYCLLYYVNLL
LIDHRFLLRRGEYVLHMWQISGFNADKLTSATNPDKENSMSISILLDNHP
IRAEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKL
FSSVKWGQQEIVAKTYQLLARREVWDQSALDVGLTMQLLDCNFSDENVRA
IAVQKLESLEDDDVLHYLLQLVQAVKFEPYHDSALARFLLKRGLRNKRIG
HFLFWFLRSEIAQSRHYQQRFAVILEAYLRGCGTAMLHDFTQQVQVIEML
QKVTLDIKSLSADVSSQVISQLKQKLENLQNSQLPESFRVPYDPGLKAGA
LAIEKCTVMASKKKPLWLEFKCADPTALSNETIGIIFKHGDDLRQDMLIL
QILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAKIQQST
VGNTGAFKDEVLNHWLKEKSPTEEKFQAAVERFVYSCAGYCVATFVLGIG
DRHNDNIMITETGNLFHIDFGERVPFVLTPDFLFVMGTSGKKTSPHFQKF
QDICVKAYLALRHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTVGK
NEEDAKKYFLDQIEVCRDKGWTVQFNWFLHLVLG
3D structure
PDB4ezl Potent and selective inhibitors of PI3K-delta: obtaining isoform selectivity from the affinity pocket and tryptophan shelf
ChainA
Resolution2.94 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.
2.7.1.154: phosphatidylinositol-4-phosphate 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 0SE A M804 I831 I879 I881 V882 T887 M953 I963 D964 M559 I586 I634 I636 V637 T642 M708 I718 D719 PDBbind-CN: -logKd/Ki=8.59,IC50=2.6nM
Gene Ontology
Molecular Function
GO:0016301 kinase activity
Biological Process
GO:0046854 phosphatidylinositol phosphate biosynthetic process

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Molecular Function
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Biological Process
External links
PDB RCSB:4ezl, PDBe:4ezl, PDBj:4ezl
PDBsum4ezl
PubMed22672799
UniProtP48736|PK3CG_HUMAN Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Gene Name=PIK3CG)

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