› 3zyu

X-ray diffraction
1.5Å resolution

Crystal Structure of the first bromodomain of human BRD4 in complex with I-BET151(GSK1210151A)

Released:
DOI: 10.2210/pdb3zyu/pdb
PDB 3zyu coloured by chain and viewed from the front.
PDB 3zyu coloured by chain and viewed from the side.
PDB 3zyu coloured by chain and viewed from the top.
Source organism: Homo sapiens
Entry authors: Chung CW, Mirguet O

Function and Biology Details

Biochemical function:
  • not assigned
Biological process:
  • not assigned
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Bromodomain-containing protein 4 Chains: A, B
Molecule details ›
Chains: A, B
Length: 127 amino acids
Theoretical weight: 15.1 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: O60885 (Residues: 44-168; Coverage: 9%)
Gene names: BRD4, HUNK1
Sequence domains: Bromodomain
Structure domains: Bromodomain-like

Ligands and Environments

2 bound ligands:
Ligand EDO 7 x EDO
Ligand 1GH 2 x 1GH
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ESRF BEAMLINE ID29
Spacegroup: P212121
Unit cell:
a: 41.894Å b: 59.542Å c: 109.195Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.164 0.162 0.201
Expression system: Escherichia coli

Quick links

Citations

289 review citations

A Comprehensive Review of BET Protein Biochemistry, Physiology, and Pathological Roles.
Ali et al. (2022)
288 more

13 mentions without citation

Readout of epigenetic modifications.
Patel et al. (2013)
12 more