› 3mo5

X-ray diffraction
2.14Å resolution

Human G9a-like (GLP, also known as EHMT1) in complex with inhibitor E72

Released:
DOI: 10.2210/pdb3mo5/pdb
PDB entry 3mo5 coloured by chain, front view.
PDB entry 3mo5 coloured by chain, side view.
PDB entry 3mo5 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Adding a lysine mimic in the design of potent inhibitors of histone lysine methyltransferases.
Chang Y, Ganesh T, Horton JR, Spannhoff A, Liu J, Sun A, Zhang X, Bedford MT, Shinkai Y, Snyder JP, Cheng X
J Mol Biol 400 1-7 (2010)
PMID: 20434463

Function and Biology Details

Reaction catalysed: 
S-adenosyl-L-methionine + a [histone H3]-L-lysine(9) = S-adenosyl-L-homocysteine + a [histone H3]-N(6)-methyl-L-lysine(9)
Biochemical function:
Biological process:
  • not assigned
Cellular component:
Sequence domains:

Structure analysis Details

Assemblies composition:
monomeric (preferred)
homo dimer
Assembly name:
PDBe Complex ID:
PDB-CPX-190698 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Histone-lysine N-methyltransferase EHMT1 Chains: A, B, C, D
Molecule details ›
Chains: A, B, C, D
Length: 285 amino acids
Theoretical weight: 32.83 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: Q9H9B1 (Residues: 982-1266; Coverage: 22%)
Gene names: EHMT1, EUHMTASE1, GLP, KIAA1876, KMT1D
Sequence domains:
Structure domains: SET domain

Ligands and Environments

3 bound ligands:
Ligand ZN 16 x ZN
Ligand E72 4 x E72
Ligand SAH 2 x SAH
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 22-ID
Spacegroup: P21
Unit cell:
a: 59.9Å b: 162.9Å c: 69.1Å
α: 90° β: 99° γ: 90°
R-values:
R R work R free
0.196 0.196 0.233
Expression system: Escherichia coli

Quick links

Citations

24 review citations

Epigenetic protein families: a new frontier for drug discovery.
Arrowsmith et al. (2012)
23 more

6 mentions without citation

Targeting protein lysine methylation and demethylation in cancers.
He et al. (2012)
5 more