Structure of PDB 5dt2 Chain B

Receptor sequence
>5dt2B (length=315) Species: 9606 (Homo sapiens) [Search protein sequence]
KLELRLKSPVGAEPAVYPWPLPVYDKHHDAAHEIIETIRWVCEEIPDLKL
AMENYVLIDYDTKSFESMQRLCDKYNRAIDSIHQLWKGTLNTRPSTGLLR
HILQQVYNHSVTDPEKPFSPEVYGETSFDLVAQMIDEIKMTDDDLFVDLG
SGVGQVVLQVAAATNCKHHYGVEKADIPAKYAETMDREFRKWMKWYGKKH
AEYTLERGDFLSEEWRERIANTSVIFVNNFAFGPEVDHQLKERFANMKEG
GRIVSSKPFAPLNFRINSRNLSDIGTIMRVVELSPLKVSWTGKPVSYYLH
TIDRTILENYFSSLK
3D structure
PDB5dt2 Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
ChainB
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 5EV B F131 S140 L143 V144 M147 D161 S164 V169 F239 V240 N241 F243 S268 S269 F118 S127 L130 V131 M134 D148 S151 V156 F226 V227 N228 F230 S255 S256 MOAD: ic50=150nM
BindingDB: IC50=150nM
Gene Ontology
Molecular Function
GO:0031151 histone H3K79 methyltransferase activity
Biological Process
GO:0051726 regulation of cell cycle

View graph for
Molecular Function
View graph for
Biological Process
External links
PDB RCSB:5dt2, PDBe:5dt2, PDBj:5dt2
PDBsum5dt2
PubMed27563395
UniProtQ8TEK3|DOT1L_HUMAN Histone-lysine N-methyltransferase, H3 lysine-79 specific (Gene Name=DOT1L)

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