› 1osv

X-ray diffraction
2.5Å resolution

STRUCTURAL BASIS FOR BILE ACID BINDING AND ACTIVATION OF THE NUCLEAR RECEPTOR FXR

Released:
DOI: 10.2210/pdb1osv/pdb
PDB entry 1osv coloured by chain, front view.
PDB entry 1osv coloured by chain, side view.
PDB entry 1osv coloured by chain, top view.
Source organisms:
Primary publication:
Structural basis for bile acid binding and activation of the nuclear receptor FXR.
Mi LZ, Devarakonda S, Harp JM, Han Q, Pellicciari R, Willson TM, Khorasanizadeh S, Rastinejad F
Mol Cell 11 1093-100 (2003)
PMID: 12718893

Function and Biology Details

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

Structure analysis Details

Assemblies composition:
hetero dimer (preferred)
hetero trimer
Assembly name:
PDBe Complex ID:
PDB-CPX-178852 (preferred)
Entry contents:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Bile acid receptor Chains: A, B
Molecule details ›
Chains: A, B
Length: 230 amino acids
Theoretical weight: 26.85 KDa
Source organism: Rattus norvegicus
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: Q62735 (Residues: 240-469; Coverage: 49%)
Gene names: Bar, Fxr, Nr1h4, Rip14
Sequence domains: Ligand-binding domain of nuclear hormone receptor
Structure domains: Retinoid X Receptor
Nuclear receptor coactivator 2 Chains: C, D, E
Molecule details ›
Chains: C, D, E
Length: 12 amino acids
Theoretical weight: 1.46 KDa
Source organism: Mus musculus
Expression system: Not provided
UniProt:
  • Canonical: Q61026 (Residues: 741-752; Coverage: 1%)
Gene names: Grip1, Ncoa2, Src2, Tif2

Ligands and Environments

1 bound ligand:
Ligand CHC 2 x CHC
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 19-BM
Spacegroup: P21212
Unit cell:
a: 98.97Å b: 108.518Å c: 69.464Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.242 0.242 0.276
Expression systems:
  • Escherichia coli BL21(DE3)
  • Not provided

Quick links

Citations

42 review citations

Role of bile acids and bile acid receptors in metabolic regulation.
Lefebvre et al. (2009)
41 more

30 mentions without citation

An updated review on drug-induced cholestasis: mechanisms and investigation of physicochemical properties and pharmacokinetic parameters.
Yang et al. (2013)
29 more