Structure of PDB 3tjp Chain A

Receptor sequence
>3tjpA (length=840) Species: 9606 (Homo sapiens) [Search protein sequence]
SEESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGLVTPRMAEVASRDP
KLYAMHPWVTSKPLPEYLWKKIANNCIFIVIHRSTTSQTIKVSPDDTPGA
ILQSFFTKMQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNGEEIHVVLD
TPPDPALDEVRKECDRKFRVKIRGIDIPVLTDLTVFVEANIQHGQQVLCQ
RRTSPKPFTEEVLWNVWLEFSIKIKDLPKGALLNLQIYCVRLLYYVNLLL
IDHRFLLRRGEYVLHMWQISGKSFNADKLTSATNPDKENSMSISILLDNY
CHPAEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPK
LFSSVKWGQQEIVAKTYQLLARREVWDQSALDVGLTMQLLDCNFSDENVR
AIAVQKLESLEDDDVLHYLLQLVQAVKFEPYHDSALARFLLKRGLRNKRI
GHFLFWFLRSEIAQSRHYQQRFAVILEAYLRGCGTAMLHDFTQQVQVIEM
LQKVTLDIKSLSAEKYDVSSQVISQLKQKLENLQNSQLPESFRVPYDPGL
KAGALAIEKCKVMASKKKPLWLEFKCADPTANETIGIIFKHGDDLRQDML
ILQILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAKIQQ
STVGNTGAFKDEVLNHWLKEKSPTEEKFQAAVERFVYSCAGYCVATFVLG
IGDRHNDNIMITETGNLFHIDFGHILGNERVPFVLTPDFLFVMGTSGKTS
PHFQKFQDICVKAYLALRHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRD
ALTVGKNEEDAKKYFLDQIEVCRDKGWTVQFNWFLHLVLG
3D structure
PDB3tjp The Identification of 5-(2,4-dimorpholinopyrimidin-6-yl)-4-(trifluoromethyl)pyridin-2-amine (NVP-BKM120) as a Potent, Selective and Orally Bioavailable Class I PI3 Kinase Inhibitor for the Treatment of Cancer
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 13K A M804 I879 E880 I881 V882 T886 M953 I963 D964 M563 I636 E637 I638 V639 T643 M710 I720 D721 BindingDB: IC50=142nM
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:3tjp, PDBe:3tjp, PDBj:3tjp
PDBsum3tjp
PubMed
UniProtP48736|PK3CG_HUMAN Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Gene Name=PIK3CG)

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