Structure of PDB 4flh Chain A

Receptor sequence
>4flhA (length=840) Species: 9606 (Homo sapiens) [Search protein sequence]
EESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGLVTPRMAEVASRDPK
LYAMHPWVTSKPLPEYLWKKIANNCIFIVIHRSTTSQTIKVSPDDTPGAI
LQSFFTDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNGEEIHVVLDTPPD
PALDEVRKEVSLWDCDRKFRVKIRGIDIPVLDLTVFVEANIQHGQQVLCQ
RRTSPKPFTEEVLWNVWLEFSIKIKDLPKGALLNLQIYCGKVQLLYYVNL
LLIDHRFLLRRGEYVLHMWQISSFNADKLTSATNPDKENSMSISILLDPI
ALPKHQEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAY
PKLFSSVKWGQQEIVAKTYQLLARREVWDQSALDVGLTMQLLDCNFSDEN
VRAIAVQKLESLEDDDVLHYLLQLVQAVKFEPYHDSALARFLLKRGLRNK
RIGHFLFWFLRSEIAQSRHYQQRFAVILEAYLRGCGTAMLHDFTQQVQVI
EMLQKVTLDIKSLSAEDVSSQVISQLKQKLENLQNSQLPESFRVPYDPGL
KAGALAIEKCKVMASKKKPLWLEFKCADPTALSNETIGIIFKHGDDLRQD
MLILQILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAKI
QQSTVGNTGAFKDEVLNHWLKEKSPTEEKFQAAVERFVYSCAGYCVATFV
LGIGDRHNDNIMITETGNLFHIDFGHIKERVPFVLTPDFLFVMGTSGKKT
SPHFQKFQDICVKAYLALRHHTNLLIILFSMMLMTGMPQLTSKEDIEYIR
DALTVGKNEEDAKKYFLDQIEVCRDKGWTVQFNWFLHLVL
3D structure
PDB4flh Selective Class I Phosphoinositide 3-Kinase Inhibitors: Optimization of a Series of Pyridyltriazines Leading to the Identification of a Clinical Candidate, AMG 511.
ChainA
Resolution2.6 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 14K A K802 M804 I831 K833 D841 Y867 E880 V882 T887 M953 I963 D964 K561 M563 I590 K592 D600 Y626 E639 V641 T646 M712 I722 D723 PDBbind-CN: -logKd/Ki=9.00,Ki=1nM
BindingDB: Ki=1nM
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:4flh, PDBe:4flh, PDBj:4flh
PDBsum4flh
PubMed22897589
UniProtP48736|PK3CG_HUMAN Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Gene Name=PIK3CG)

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