› 1z95

X-ray diffraction
1.8Å resolution

Crystal Structure of the Androgen Receptor Ligand-binding Domain W741L Mutant Complex with R-bicalutamide

Released:
DOI: 10.2210/pdb1z95/pdb
PDB entry 1z95 coloured by chain, front view.
PDB entry 1z95 coloured by chain, side view.
PDB entry 1z95 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structural basis for antagonism and resistance of bicalutamide in prostate cancer.
Bohl CE, Gao W, Miller DD, Bell CE, Dalton JT
Proc Natl Acad Sci U S A 102 6201-6 (2005)
PMID: 15833816

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-145222 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Androgen receptor Chain: A
Molecule details ›
Chain: A
Length: 246 amino acids
Theoretical weight: 28.65 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P10275 (Residues: 673-918; Coverage: 27%)
Gene names: AR, DHTR, NR3C4
Sequence domains: Ligand-binding domain of nuclear hormone receptor
Structure domains: Retinoid X Receptor

Ligands and Environments

2 bound ligands:
Ligand SO4 1 x SO4
Ligand 198 1 x 198
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU RU300
Spacegroup: P212121
Unit cell:
a: 56.49Å b: 66.47Å c: 72.16Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.223 0.223 0.256
Expression system: Escherichia coli

Quick links

Citations

54 review citations

Biology of progressive, castration-resistant prostate cancer: directed therapies targeting the androgen-receptor signaling axis.
Scher et al. (2005)
53 more

41 mentions without citation

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