Structure of PDB 5ls6 Chain A

Receptor sequence
>5ls6A (length=570) Species: 9606 (Homo sapiens) [Search protein sequence]
KGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQE
WKQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPI
MYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHG
DRECGFINDEIFVELVNALGQYNESRPPRSDKIFEAISSMFPDKGTAEEL
KEKYKELTQPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLH
PFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPN
IEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKE
SSIIAPAHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFP
GCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQR
GSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVY
DKYMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRI
GIFAKRAIQTGEELFFDYRY
3D structure
PDB5ls6 Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.
ChainA
Resolution3.47 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 2.1.1.356: [histone H3]-lysine(27) N-trimethyltransferase.
Interaction with ligand
Gene Ontology
Molecular Function
GO:0042054 histone methyltransferase activity
GO:0046976 histone H3K27 methyltransferase activity
Biological Process
GO:0006338 chromatin remodeling

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Molecular Function
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Biological Process
External links
PDB RCSB:5ls6, PDBe:5ls6, PDBj:5ls6
PDBsum5ls6
PubMed27739677
UniProtQ15910|EZH2_HUMAN Histone-lysine N-methyltransferase EZH2 (Gene Name=EZH2)

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