Structure of PDB 5jha Chain A

Receptor sequence
>5jhaA (length=803) Species: 9606 (Homo sapiens) [Search protein sequence]
EESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGLVTPRMAEVASRDPK
LYAMHPWVTSKPLPEYLWKKIANNCIFIVIHSQTIKVSPDDTPGAILQSF
FTQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNGEEIHVVLDTPPDPAL
DEVRKECDRKFRVKIRGIDIPVLLTVFVEANIQHGQQVLCQRRTSPKPFT
EEVLWNVWLEFSIKIKDLPKGALLNLQIYCLLYYVNLLLIDHRFLLRRGE
YVLHMWQISGFNADKLTSATNPDKENSMSISILLDNAEMPNQLRKQLEAI
IATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSSVKWGQQEIVAKTY
QLLARREVWDQSALDVGLTMQLLDCNFSDENVRAIAVQKLESLEDDDVLH
YLLQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFLFWFLRSEIAQSRH
YQQRFAVILEAYLRGCGTAMLHDFTQQVQVIEMLQKVTLDIKSLSAEKYD
VSSQVISQLKQKLENLQNPESFRVPYDPGLKAGALAIEKCKVMASKKKPL
WLEFKCADPTALSNETIGIIFKHGDDLRQDMLILQILRIMESIWETESLD
LCLLPYGCISTGDKIGMIEIVKDATTIAKIQQSTVFKDEVLNHWLKEKSP
TEEKFQAAVERFVYSCAGYCVATFVLGIGDRHNDNIMITETGNLFHIDFG
HIRVPFVLTPDFLFVMGTTSPHFQKFQDICVKAYLALRHHTNLLIILFSM
MLMTGMPTSKEDIEYIRDALTVGKNEEDAKKYFLDQIEVCRDKGWTVQFN
WFL
3D structure
PDB5jha Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention.
ChainA
Resolution2.51 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 6K7 A I831 K833 D836 I879 E880 I881 V882 I963 D964 I570 K572 D575 I618 E619 I620 V621 I697 D698 PDBbind-CN: -logKd/Ki=5.90,Ki=1264nM
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:5jha, PDBe:5jha, PDBj:5jha
PDBsum5jha
PubMed28276440
UniProtP48736|PK3CG_HUMAN Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Gene Name=PIK3CG)

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