Structure of PDB 7t7m Chain A

Receptor sequence

>7t7mA (length=260) Species: 9606 (Homo sapiens)

VERIVSRDIARGYERIPIPCVNAVDSEPCPSNYKYVSQNCVTSPMNIDRN
ITHLQYCVCIDDCSSSNCMCGQLSMRCWYDKDGRLLPEFNMAEPPLIFEC
NHACSCWRNCRNRVVQNGLRARLQLYRTRDMGWGVRSLQDIPPGTFVCEY
VGELISDSEADVREEDSYLFDLDNKGEVYCIDARFYGNVSRFINHHCEPN
LVPVRVFMAHQDLRFPRIAFFSTRLIEAGEQLGFDYGERFWDIKGKLFSC
RCGSPKCRHS

3D structure

• PDB: 7t7m Discovery of the First-in-Class G9a/GLP Covalent Inhibitors.
• Chain: A
• Resolution: 2.85 Å

Enzymatic activity

• Enzyme Commision number: 2.1.1.-
  2.1.1.367: [histone H3]-lysine(9) 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	ZN	A	C1062 C1075 C1105 C1109	C57 C70 C100 C104
BS02	ZN	A	C1068 C1105 C1111 C1115	C63 C100 C106 C110
BS03	ZN	A	C1062 C1064 C1068 C1073	C57 C59 C63 C68
BS04	ZN	A	C1203 C1256 C1258 C1263	C197 C250 C252 C257
BS05	G4R	A	D1162 D1166 D1171 L1174 D1176 C1186 Y1242 R1245 F1246	D157 D161 D166 L169 D171 C180 Y236 R239 F240

Gene Ontology

Molecular Function

• GO:0002039 p53 binding
• GO:0008270 zinc ion binding
• GO:0016279 protein-lysine N-methyltransferase activity
• GO:0042054 histone methyltransferase activity
• GO:0046974 histone H3K9 methyltransferase activity

Cellular Component

• GO:0005634 nucleus

External links

• PDB: RCSB:7t7m, PDBe:7t7m, PDBj:7t7m
• PDBsum: 7t7m
• PubMed: 35763668
• UniProt: Q9H9B1|EHMT1_HUMAN Histone-lysine N-methyltransferase EHMT1 (Gene Name=EHMT1)