Structure of PDB 3apc Chain A

Receptor sequence
>3apcA (length=839) Species: 9606 (Homo sapiens) [Search protein sequence]
SEESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGLVTPRMAEVASRDP
KLYAMHPWVTSKPLPEYLWKKIANNCIFIVIHRSTTSQTIKVSPDDTPGA
ILQSFFTKMASEQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNGEEIHV
VLDTPPDPALDEVRKECDRKFRVKIRGIDIPVLPRNTDLTVFVEANIQHG
QQVLCQRRTSPKPFTEEVLWNVWLEFSIKIKDLPKGALLNLQIYCVQLLY
YVNLLLIDHRFLLRRGEYVLHMWQISGFNADKLTSATNPDKENSMSISIL
LDEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLF
SSVKWGQQEIVAKTYQLLARREVWDQSALDVGLTMQLLDCNFSDENVRAI
AVQKLESLEDDDVLHYLLQLVQAVKFEPYHDSALARFLLKRGLRNKRIGH
FLFWFLRSEIAQSRHYQQRFAVILEAYLRGCGTAMLHDFTQQVQVIEMLQ
KVTLDIKSLSADVSSQVISQLKQKLENLQNSQLPESFRVPYDPGLKAGAL
AIEKCKVMASKKKPLWLEFKCADPTALSNETIGIIFKHGDDLRQDMLILQ
ILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAKIQQSTV
GNTGAFKDEVLNHWLKEKSPTEEKFQAAVERFVYSCAGYCVATFVLGIGD
RHNDNIMITETGNLFHIDFGHILGNKERVPFVLTPDFLFVMGTSGKKTSP
HFQKFQDICVKAYLALRHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDA
LTVGKNEEDAKKYFLDQIEVCRDKGWTVQFNWFLHLVLG
3D structure
PDB3apc Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799
ChainA
Resolution2.544 Å
3D
structure
[Spin on]
[Spin off]
[Reset orientation]

[High quality]
[Low quality]

[White background]
[Black background]

[Download]
[Download structure with residue number starting from 1]
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 MMD A M804 I831 K833 D836 I879 E880 I881 V882 M953 I963 D964 M558 I585 K587 D590 I633 E634 I635 V636 M707 I717 D718 PDBbind-CN: -logKd/Ki=7.44,IC50=0.036uM
BindingDB: IC50=36nM
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:3apc, PDBe:3apc, PDBj:3apc
PDBsum3apc
PubMed21316229
UniProtP48736|PK3CG_HUMAN Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Gene Name=PIK3CG)

[Back to BioLiP]