Structure of PDB 5mw4 Chain A

Receptor sequence
>5mw4A (length=305) Species: 9606 (Homo sapiens) [Search protein sequence]
LELRLKSPVGAEPAVYPWPLPVYDKHHDAAHEIIETIRWVCEEIPDLKLA
MENYVLIDYDTKSFESMQRLCDKYNRAIDSIHQLWKGNTRPSTGLLRHIL
QQVYNHSVTDPEKGETSFDLVAQMIDEIKMTDDDLFVDLGSGVGQVVLQV
AAATNCKHHYGVEKADIPAKYAETMDREFRKWMKWYGKKHAEYTLERGDF
LSEEWRERIANTSVIFVNNFAFGPEVDHQLKERFANMKEGGRIVSSKPFA
PLNFRINSRNLSDIGTIMRVVELSPLKSWTGKPVSYYLHTIDRTILENYF
SSLKN
3D structure
PDB5mw4 Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.
ChainA
Resolution2.19 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 5JU A S140 L143 M147 D161 G163 S164 G165 V169 E186 K187 D222 F223 F239 V240 N241 S268 S269 S117 L120 M124 D138 G140 S141 G142 V146 E163 K164 D199 F200 F216 V217 N218 S245 S246 MOAD: Ki=0.002nM
PDBbind-CN: -logKd/Ki=11.70,Ki=0.002nM
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:5mw4, PDBe:5mw4, PDBj:5mw4
PDBsum5mw4
PubMed28337327
UniProtQ8TEK3|DOT1L_HUMAN Histone-lysine N-methyltransferase, H3 lysine-79 specific (Gene Name=DOT1L)

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