Structure of PDB 5oq4 Chain A

Receptor sequence
>5oq4A (length=834) Species: 9606 (Homo sapiens) [Search protein sequence]
EESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGLVTPRMAEVASRDPK
LYAMHPWVTSKPLPEYLWKKIANNCIFIVIHRSTTSQTIKVSPDDTPGAI
LQSFFTKQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNGEEIHVVLDTP
PDPALDEVRKECDRKFRVKIRGIDIPVLNTDLTVFVEANIQHGQQVLCQR
RTSPKPFTEEVLWNVWLEFSIKIKDLPKGALLNLQIYCRLLYYVNLLLID
HRFLLRRGEYVLHMWQISGFNADKLTSATNPDKENSMSISILLDNHPIRA
EMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSS
VKWGQQEIVAKTYQLLARREVWDQSALDVGLTMQLLDCNFSDENVRAIAV
QKLESLEDDDVLHYLLQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFL
FWFLRSEIAQSRHYQQRFAVILEAYLRGCGTAMLHDFTQQVQVIEMLQKV
TLDIKSLSAEKYDVSSQVISQLKQKLENLQNSLPESFRVPYDPGLKAGAL
AIEKCKVMASKKKPLWLEFKCADPTALSNETIGIIFKHGDDLRQDMLILQ
ILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAKIQQSTV
GNTGFKDEVLNHWLKEKSPTEEKFQAAVERFVYSCAGYCVATFVLGIGDR
HNDNIMITETGNLFHIDFGHILGERVPFVLTPDFLFVMGTSGKKTSPHFQ
KFQDICVKAYLALRHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTV
GKNEEDAKKYFLDQIEVCRDKGWTVQFNWFLHLV
3D structure
PDB5oq4 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.
ChainA
Resolution2.7 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 A3W A I831 K833 D836 E880 I881 V882 K890 D964 I585 K587 D590 E634 I635 V636 K644 D717 PDBbind-CN: -logKd/Ki=7.60,Kd=25nM
BindingDB: Kd=25nM,IC50=708nM
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:5oq4, PDBe:5oq4, PDBj:5oq4
PDBsum5oq4
PubMed28829592
UniProtP48736|PK3CG_HUMAN Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Gene Name=PIK3CG)

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