› 5h1t

X-ray diffraction
1.95Å resolution

Complex structure of TRIM24 PHD-bromodomain and inhibitor 1

Released:
DOI: 10.2210/pdb5h1t/pdb
PDB entry 5h1t coloured by chain, front view.
PDB entry 5h1t coloured by chain, side view.
PDB entry 5h1t coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
The polar warhead of a TRIM24 bromodomain inhibitor rearranges a water-mediated interaction network.
Liu J, Li F, Bao H, Jiang Y, Zhang S, Ma R, Gao J, Wu J, Ruan K
FEBS J 284 1082-1095 (2017)
PMID: 28207202

Function and Biology Details

Reaction catalysed: 
S-ubiquitinyl-[E2 ubiquitin-conjugating enzyme]-L-cysteine + [acceptor protein]-L-lysine = [E2 ubiquitin-conjugating enzyme]-L-cysteine + N(6)-ubiquitinyl-[acceptor protein]-L-lysine
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-127337 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Transcription intermediary factor 1-alpha Chains: A, B, C, D
Molecule details ›
Chains: A, B, C, D
Length: 183 amino acids
Theoretical weight: 21.23 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli 'BL21-Gold(DE3)pLysS AG'
UniProt:
  • Canonical: O15164 (Residues: 824-1006; Coverage: 17%)
Gene names: RNF82, TIF1, TIF1A, TRIM24
Sequence domains:
Structure domains:

Ligands and Environments

3 bound ligands:
Ligand ZN 8 x ZN
Ligand 7FF 4 x 7FF
Ligand DMS 2 x DMS
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SSRF BEAMLINE BL19U1
Spacegroup: P1
Unit cell:
a: 36.725Å b: 48.612Å c: 123.454Å
α: 86.56° β: 81.47° γ: 67.81°
R-values:
R R work R free
0.179 0.177 0.22
Expression system: Escherichia coli 'BL21-Gold(DE3)pLysS AG'

Quick links

Citations

4 review citations

Inhibitors of protein-protein interactions (PPIs): an analysis of scaffold choices and buried surface area.
Ran et al. (2018)
3 more

1 mention without citation

The polar warhead of a TRIM24 bromodomain inhibitor rearranges a water-mediated interaction network.
Liu et al. (2017)