Structure of PDB 5ylt Chain A

Receptor sequence
>5yltA (length=247) Species: 9606 (Homo sapiens) [Search protein sequence]
RHGVCWIYYPDGGSLVGEVNEDGEMTGEKIAYVYPDERTALYGKFIDGEM
IEGKLATLMSTEEGRPHFELMPGNSVYHFDKSTSSCISTNALLPDPYESE
RVYVAESLISSAGEGLFSKVAVGPNTVMSFYNGVRITHQEVDSRDWALNG
NTLSLDEETVIDVPEPYNHVSKYCASLGHKANHSFTPNCIYDMFVHPRFG
PIKCIRTLRAVEADEELTVAYGYDHSPPGKSAPEWYQVELKAFQATQ
3D structure
PDB5ylt Development of Novel Inhibitors for Histone Methyltransferase SET7/9 based on Cyproheptadine.
ChainA
Resolution1.69 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) Y245 H293 H297 Y305 Y335
Catalytic site (residue number reindexed from 1) Y131 H179 H183 Y191 Y221
Enzyme Commision number 2.1.1.364: [histone H3]-lysine(4) N-methyltransferase.
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 SFG A A226 E228 G264 N265 H293 K294 N296 H297 Y335 W352 E356 A112 E114 G150 N151 H179 K180 N182 H183 Y221 W235 E239 BindingDB: IC50=2500nM
BS02 C7N A N263 G264 T266 Y305 Y335 G336 D338 P341 Y353 N149 G150 T152 Y191 Y221 G222 D224 P227 Y236 MOAD: ic50=0.41uM
PDBbind-CN: -logKd/Ki=6.39,IC50=0.41uM
Gene Ontology
Molecular Function
GO:0016279 protein-lysine N-methyltransferase activity
GO:0140945 histone H3K4 monomethyltransferase activity
Biological Process
GO:0006355 regulation of DNA-templated transcription
Cellular Component
GO:0005694 chromosome

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Molecular Function
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Cellular Component
External links
PDB RCSB:5ylt, PDBe:5ylt, PDBj:5ylt
PDBsum5ylt
PubMed29882380
UniProtQ8WTS6|SETD7_HUMAN Histone-lysine N-methyltransferase SETD7 (Gene Name=SETD7)

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