Structure of PDB 5dsx Chain A

Receptor sequence
>5dsxA (length=316) Species: 9606 (Homo sapiens) [Search protein sequence]
LELRLKSPVGAEPAVYPWPLPVYDKHHDAAHEIIETIRWVCEEIPDLKLA
MENYVLIDYDTKSFESMQRLCDKYNRAIDSIHQLWKGTNTRPSTGLLRHI
LQQVYNHSVTDPEKLEPFSPEVYGETSFDLVAQMIDEIKMTDDDLFVDLG
SGVGQVVLQVAAATNCKHHYGVEKADIPAKYAETMDREFRKWMKWYGKKH
AEYTLERGDFLSEEWRERIANTSVIFVNNFAFGPEVDHQLKERFANMKEG
GRIVSSKPFAPLNFRINSRNLSDIGTIMRVVELSPLKSWTGKPVSYYLHT
IDRTILENYFSSLKNP
3D structure
PDB5dsx Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
ChainA
Resolution2.41 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 5EW A F131 S140 D161 S164 V169 V240 N241 F243 S268 S269 F118 S127 D148 S151 V156 V227 N228 F230 S255 S256 MOAD: ic50=10nM
PDBbind-CN: -logKd/Ki=8.00,IC50=10nM
BindingDB: IC50=10.0nM
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:5dsx, PDBe:5dsx, PDBj:5dsx
PDBsum5dsx
PubMed27563395
UniProtQ8TEK3|DOT1L_HUMAN Histone-lysine N-methyltransferase, H3 lysine-79 specific (Gene Name=DOT1L)

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