› 6pgu

X-ray diffraction
1.72Å resolution

Crystal structure of the p300 acetyltransferase domain with allosteric inhibitor CPI-076 and CoA

Released:
DOI: 10.2210/pdb6pgu/pdb
PDB entry 6pgu coloured by chain, front view.
PDB entry 6pgu coloured by chain, side view.
PDB entry 6pgu coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Make the right measurement: Discovery of an allosteric inhibition site for p300-HAT.
Gardberg AS, Huhn AJ, Cummings R, Bommi-Reddy A, Poy F, Setser J, Vivat V, Brucelle F, Wilson J
Struct Dyn 6 054702 (2019)
PMID: 31649965

Function and Biology Details

Reaction catalysed: 
Acetyl-CoA + [protein]-L-lysine = CoA + [protein]-N(6)-acetyl-L-lysine
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-170794 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Histone acetyltransferase p300 Chains: A, B
Molecule details ›
Chains: A, B
Length: 323 amino acids
Theoretical weight: 37.19 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: Q09472 (Residues: 1287-1519, 1582-1663; Coverage: 13%)
Gene names: EP300, P300
Sequence domains: Histone acetylation protein

Ligands and Environments


Cofactor: Ligand COA 2 x COA
1 bound ligand:
Ligand OK7 2 x OK7
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 22-ID
Spacegroup: P212121
Unit cell:
a: 66.253Å b: 97.599Å c: 105.932Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.167 0.165 0.206
Expression system: Escherichia coli

Quick links

Citations

2 citation in other articles

MOF upregulates the estrogen receptor α signaling pathway by its acetylase activity in hepatocellular carcinoma.
Wei et al. (2021)
1 more

3 mentions without citation

The Biological Significance of Targeting Acetylation-Mediated Gene Regulation for Designing New Mechanistic Tools and Potential Therapeutics.
O'Garro et al. (2021)
2 more