Structure of PDB 6ten Chain B

Receptor sequence
>6tenB (length=322) Species: 9606 (Homo sapiens) [Search protein sequence]
KLELRLKSPVGAEPAVYPWPLPVYDKHHDAAHEIIETIRWVCEEIPDLKL
AMENYVLIDYDTKSFESMQRLCDKYNRAIDSIHQLWKGTLNTRPSTGLLR
HILQQVYNHSVTDPEKLNNYEPFSPEVYGETSFDLVAQMIDEIKMTDDDL
FVDLGSGVGQVVLQVAAATNCKHHYGVEKADIPAKYAETMDREFRKWMKW
YGKKHAEYTLERGDFLSEEWRERIANTSVIFVNNFAFGPEVDHQLKERFA
NMKEGGRIVSSKPFAPLNFRINSRNLSDIGTIMRVVELSPLKGSVSWTGK
PVSYYLHTIDRTILENYFSSLK
3D structure
PDB6ten New Potent DOT1L Inhibitors forin VivoEvaluation in Mouse.
ChainB
Resolution2.21 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 N5K B P130 F131 S140 L143 V169 F239 V240 N241 F243 V267 S268 S269 V310 S311 Y312 P122 F123 S132 L135 V161 F231 V232 N233 F235 V259 S260 S261 V302 S303 Y304 MOAD: ic50=0.00017uM
BindingDB: IC50=0.170000nM
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:6ten, PDBe:6ten, PDBj:6ten
PDBsum6ten
PubMed31857842
UniProtQ8TEK3|DOT1L_HUMAN Histone-lysine N-methyltransferase, H3 lysine-79 specific (Gene Name=DOT1L)

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