› 3cld

X-ray diffraction
2.84Å resolution

Ligand binding domain of the glucocorticoid receptor complexed with fluticazone furoate

Released:
DOI: 10.2210/pdb3cld/pdb
PDB entry 3cld coloured by chain, front view.
PDB entry 3cld coloured by chain, side view.
PDB entry 3cld coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
X-ray crystal structure of the novel enhanced-affinity glucocorticoid agonist fluticasone furoate in the glucocorticoid receptor-ligand binding domain.
Biggadike K, Bledsoe RK, Hassell AM, Kirk BE, McLay IM, Shewchuk LM, Stewart EL
J Med Chem 51 3349-52 (2008)
PMID: 18522385

Function and Biology Details

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

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, B
Molecule details ›
Chains: A, B
Length: 259 amino acids
Theoretical weight: 29.99 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: C, H
Molecule details ›
Chains: C, H
Length: 12 amino acids
Theoretical weight: 1.48 KDa
Source organism: Homo sapiens
Expression system: Not provided
UniProt:
  • Canonical: Q15596 (Residues: 740-751; Coverage: 1%)
Gene names: BHLHE75, NCOA2, SRC2, TIF2

Ligands and Environments

1 bound ligand:
Ligand GW6 2 x GW6
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 17-ID
Spacegroup: P61
Unit cell:
a: 127.34Å b: 127.34Å c: 77.772Å
α: 90° β: 90° γ: 120°
R-values:
R R work R free
0.21 0.207 0.267
Expression systems:
  • Escherichia coli BL21(DE3)
  • Not provided

Quick links

Citations

14 review citations

Structural overview of the nuclear receptor superfamily: insights into physiology and therapeutics.
Huang et al. (2010)
13 more

5 mentions without citation

The Biologist's Guide to the Glucocorticoid Receptor's Structure.
Deploey et al. (2023)
4 more