› 1t5z

X-ray diffraction
2.3Å resolution

Crystal Structure of the Androgen Receptor Ligand Binding Domain (LBD) with DHT and a peptide derived from its physiological coactivator ARA70

Released:
DOI: 10.2210/pdb1t5z/pdb
PDB entry 1t5z coloured by chain, front view.
PDB entry 1t5z coloured by chain, side view.
PDB entry 1t5z coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
The molecular mechanisms of coactivator utilization in ligand-dependent transactivation by the androgen receptor.
Estébanez-Perpiñá E, Moore JM, Mar E, Delgado-Rodrigues E, Nguyen P, Baxter JD, Buehrer BM, Webb P, Fletterick RJ, Guy RK
J Biol Chem 280 8060-8 (2005)
PMID: 15563469

Function and Biology Details

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

Structure analysis Details

Assembly composition:
hetero dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-145243 (preferred)
Entry contents:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Androgen receptor Chain: A
Molecule details ›
Chain: A
Length: 251 amino acids
Theoretical weight: 29.28 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P10275 (Residues: 670-920; Coverage: 27%)
Gene names: AR, DHTR, NR3C4
Sequence domains: Ligand-binding domain of nuclear hormone receptor
Structure domains: Retinoid X Receptor
Nuclear receptor coactivator 4 Chain: B
Molecule details ›
Chain: B
Length: 15 amino acids
Theoretical weight: 1.89 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: Q13772 (Residues: 322-336; Coverage: 2%)
Gene names: ARA70, ELE1, NCOA4, RFG

Ligands and Environments

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

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 8.3.1
Spacegroup: P212121
Unit cell:
a: 55.68Å b: 66.423Å c: 68.253Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.228 0.228 0.26
Expression system: Escherichia coli

Quick links

Citations

19 review citations

Androgen receptor: structure, role in prostate cancer and drug discovery.
Tan et al. (2015)
18 more

12 mentions without citation

Allosteric Antagonism of the Pregnane X Receptor (PXR): Current-State-of-the-Art and Prediction of Novel Allosteric Sites.
Kamaraj et al. (2022)
11 more