› 6x7c

X-ray diffraction
2.7Å resolution

BRD4 Bromodomain 1 in complex with multi-action inhibitor SRX3212

Released:
DOI: 10.2210/pdb6x7c/pdb
PDB entry 6x7c coloured by chain, front view.
PDB entry 6x7c coloured by chain, side view.
PDB entry 6x7c coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Design of thienopyranone-based BET inhibitors that bind multiple synthetic lethality targets.
Vann KR, Pal D, Morales GA, Burgoyne AM, Durden DL, Kutateladze TG
Sci Rep 10 12027 (2020)
PMID: 32694708

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)
Assembly name:
PDBe Complex ID:
PDB-CPX-130112 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Bromodomain-containing protein 4 Chain: A
Molecule details ›
Chain: A
Length: 134 amino acids
Theoretical weight: 15.85 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: O60885 (Residues: 44-176; Coverage: 10%)
Gene names: BRD4, HUNK1
Sequence domains: Bromodomain

Ligands and Environments

1 bound ligand:
Ligand KV9 1 x KV9
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU MICROMAX-007 HF
Spacegroup: P1
Unit cell:
a: 30.547Å b: 34.65Å c: 36.033Å
α: 62.87° β: 83.59° γ: 85.49°
R-values:
R R work R free
0.206 0.2 0.257
Expression system: Escherichia coli

Quick links

Citations

6 citation in other articles

Combinatorial inhibition of BTK, PI3K-AKT and BRD4-MYC as a strategy for treatment of mantle cell lymphoma.
Vann et al. (2022)
5 more