Structure of PDB 3uwp Chain A

Receptor sequence
>3uwpA (length=341) Species: 9606 (Homo sapiens) [Search protein sequence]
KLELRLKSPVGAEPAVYPWPLPVYDKHHDAAHEIIETIRWVCEEIPDLKL
AMENYVLIDYDTKSFESMQRLCDKYNRAIDSIHQLWKGTTQPMKLNTRPS
TGLLRHILQQVYNHSVTDPEKLNNYEPFSPEVYGETSFDLVAQMIDEIKM
TDDDLFVDLGSGVGQVVLQVAAATNCKHHYGVEKADIPAKYAETMDREFR
KWMKWYGKKHAEYTLERGDFLSEEWRERIANTSVIFVNNFAFGPEVDHQL
KERFANMKEGGRIVSSKPFAPLNFRINSRNLSDIGTIMRVVELSPLKGSV
SWTGKPVSYYLHTIDRTILENYFSSLKNPKLREEQEAARRR
3D structure
PDB3uwp Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
ChainA
Resolution2.05 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 5ID A E129 G163 E186 K187 D222 F223 E126 G160 E183 K184 D219 F220 BindingDB: IC50=7000nM
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:3uwp, PDBe:3uwp, PDBj:3uwp
PDBsum3uwp
PubMed23250418
UniProtQ8TEK3|DOT1L_HUMAN Histone-lysine N-methyltransferase, H3 lysine-79 specific (Gene Name=DOT1L)

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