› 1m2z

X-ray diffraction
2.5Å resolution

Crystal structure of a dimer complex of the human glucocorticoid receptor ligand-binding domain bound to dexamethasone and a TIF2 coactivator motif

Released:
DOI: 10.2210/pdb1m2z/pdb
PDB entry 1m2z coloured by chain, front view.
PDB entry 1m2z coloured by chain, side view.
PDB entry 1m2z coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Crystal structure of the glucocorticoid receptor ligand binding domain reveals a novel mode of receptor dimerization and coactivator recognition.
Bledsoe RK, Montana VG, Stanley TB, Delves CJ, Apolito CJ, McKee DD, Consler TG, Parks DJ, Stewart EL, Willson TM, Lambert MH, Moore JT, Pearce KH, Xu HE
Cell 110 93-105 (2002)
PMID: 12151000

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 tetramer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-137451 (preferred)
Entry contents:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Glucocorticoid receptor Chains: A, D
Molecule details ›
Chains: A, D
Length: 257 amino acids
Theoretical weight: 29.81 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P04150 (Residues: 521-777; Coverage: 33%)
Gene names: GRL, NR3C1
Sequence domains: Ligand-binding domain of nuclear hormone receptor
Structure domains: Retinoid X Receptor
Nuclear receptor coactivator 2 Chains: B, E
Molecule details ›
Chains: B, E
Length: 21 amino acids
Theoretical weight: 2.45 KDa
Source organism: Homo sapiens
Expression system: Not provided
UniProt:
  • Canonical: Q15596 (Residues: 734-754; Coverage: 1%)
Gene names: BHLHE75, NCOA2, SRC2, TIF2

Ligands and Environments

2 bound ligands:
Ligand BOG 3 x BOG
Ligand DEX 2 x DEX
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 19-BM
Spacegroup: P61
Unit cell:
a: 125.843Å b: 125.843Å c: 85.976Å
α: 90° β: 90° γ: 120°
R-values:
R R work R free
0.267 0.237 0.267
Expression systems:
  • Escherichia coli BL21(DE3)
  • Not provided

Quick links

Citations

134 review citations

Antiinflammatory action of glucocorticoids--new mechanisms for old drugs.
Rhen et al. (2005)
133 more

66 mentions without citation

The nuclear receptor superfamily: A structural perspective.
Weikum et al. (2018)
65 more