Structure of PDB 4kzc Chain A

Receptor sequence
>4kzcA (length=821) Species: 9606 (Homo sapiens) [Search protein sequence]
SEESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGLVTPRMAEVASRDP
KLYAMHPWVTSKPLPEYLWKNCIFIVIHRSTTSQTIKVSPDDTPGAISFF
TQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNGEEIHVVLDTPPDPALD
EVRKECDRKFRVKIRGIDIPVLTVFVEANIQHGQQVLCQRRTSPKPFTEE
VLWNVWLEFSIKIKDLPKGALLNLQIYCVRLLYYVNLLLIDHRFLLRRGE
YVLHMWQISGNADKLTSATNPDKENSMSISILLDNRAEMPNQLRKQLEAI
IATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSSVKWGQQEIVAKTY
QLLARREVWDQSALDVGLTMQLLDCNFSDENVRAIAVQKLESLEDDDVLH
YLLQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFLFWFLRSEIAQSRH
YQQRFAVILEAYLRGCGTAMLHDFTQQVQVIEMLQKVTLDIKSLSAEKYD
VSSQVISQLKQKLENLQNSQLPESFRVPYDPGLKAGALAIEKCKVMASKK
KPLWLEFKCADPTANETIGIIFKHGDDLRQDMLILQILRIMESIWETESL
DLCLLPYGCISTGDKIGMIEIVKDATTIAKIQQSTVGNTGAFKDEVLNHW
LKEKSPTEEKFQAAVERFVYSCAGYCVATFVLGIGDRHNDNIMITETGNL
FHIDFGHILGNERVPFVLTPDFLFVMGTSKTSPHFQKFQDICVKAYLALR
HHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTVGKNEEDAKKYFLDQ
IEVCRDKGWTVQFNWFLHLVL
3D structure
PDB4kzc Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.
ChainA
Resolution3.25 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 1UK A W812 I831 K833 Y867 I879 I881 V882 A885 M953 I963 D964 W554 I571 K573 Y607 I619 I621 V622 A625 M693 I703 D704 PDBbind-CN: -logKd/Ki=8.09,IC50=8.2nM
BindingDB: IC50=8.2nM
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:4kzc, PDBe:4kzc, PDBj:4kzc
PDBsum4kzc
PubMed23820386
UniProtP48736|PK3CG_HUMAN Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Gene Name=PIK3CG)

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