Structure of PDB 4er6 Chain A

Receptor sequence
>4er6A (length=335) Species: 9606 (Homo sapiens) [Search protein sequence]
KLELRLKSPVGAEPAVYPWPLPVYDKHHDAAHEIIETIRWVCEEIPDLKL
AMENYVLIDYDTKSFESMQRLCDKYNRAIDSIHQLWKGTTQPMKLNTRPS
TGLLRHILQQVYNHSVTDPEKLNPFSPEVYGETSFDLVAQMIDEIKMTDD
DLFVDLGSGVGQVVLQVAAATNCKHHYGVEKADIPAKYAETMDREFRKWM
KWYGKKHAEYTLERGDFLSEEWRERIANTSVIFVNNFAFGPEVDHQLKER
FANMKEGGRIVSSKPFAPLNFRINSRNLSDIGTIMRVVELSPLKGSVSWT
GKPVSYYLHTIDRTILENYFSSLKNPKLREEQEAA
3D structure
PDB4er6 Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
ChainA
Resolution2.3 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 2.1.1.360: [histone H3]-lysine(79) N-trimethyltransferase.
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 AW2 A D161 G163 S164 G165 V169 E186 K187 D222 F223 F239 N241 F245 V267 S268 Y312 D155 G157 S158 G159 V163 E180 K181 D216 F217 F233 N235 F239 V261 S262 Y306 BindingDB: Kd=0.060000nM,IC50=8.8nM,EC50=9.0nM
Gene Ontology
Molecular Function
GO:0031151 histone H3K79 methyltransferase activity
Biological Process
GO:0051726 regulation of cell cycle

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Molecular Function
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Biological Process
External links
PDB RCSB:4er6, PDBe:4er6, PDBj:4er6
PDBsum4er6
PubMed23250418
UniProtQ8TEK3|DOT1L_HUMAN Histone-lysine N-methyltransferase, H3 lysine-79 specific (Gene Name=DOT1L)

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