Structure of PDB 6te6 Chain B

Receptor sequence
>6te6B (length=323) Species: 9606 (Homo sapiens) [Search protein sequence]
KLELRLKSPVGAEPAVYPWPLPVYDKHHDAAHEIIETIRWVCEEIPDLKL
AMENYVLIDYDTKSFESMQRLCDKYNRAIDSIHQLWKGTLNTRPSTGLLR
HILQQVYNHSVTDPEKLNNYEPFSPEVYGETSFDLVAQMIDEIKMTDDDL
FVDLGSGVGQVVLQVAAATNCKHHYGVEKADIPAKYAETMDREFRKWMKW
YGKKHAEYTLERGDFLSEEWRERIANTSVIFVNNFAFGPEVDHQLKERFA
NMKEGGRIVSSKPFAPLNFRINSRNLSDIGTIMRVVELSPLKGSVSWTGK
PVSYYLHTIDRTILENYFSSLKN
3D structure
PDB6te6 New Potent DOT1L Inhibitors forin VivoEvaluation in Mouse.
ChainB
Resolution1.98 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 N4W B P130 F131 S140 L143 M147 V169 F239 N241 F243 S268 S269 V310 S311 Y312 P122 F123 S132 L135 M139 V161 F231 N233 F235 S260 S261 V302 S303 Y304 MOAD: ic50=0.27uM
BindingDB: IC50=270nM
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:6te6, PDBe:6te6, PDBj:6te6
PDBsum6te6
PubMed31857842
UniProtQ8TEK3|DOT1L_HUMAN Histone-lysine N-methyltransferase, H3 lysine-79 specific (Gene Name=DOT1L)

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