› 8vkz

X-ray diffraction
2.13Å resolution

Crystal structure of Glucocorticoid Receptor in complex with an inhibitor

Released:
DOI: 10.2210/pdb8vkz/pdb
PDB entry 8vkz coloured by chain, front view.
PDB entry 8vkz coloured by chain, side view.
PDB entry 8vkz coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties.
Hobson AD, Zhu H, Qiu W, Judge RA, Longenecker K
RSC Med Chem 15 832-838 (2024)
PMID: 38516584

Function and Biology Details

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

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: 252 amino acids
Theoretical weight: 29.29 KDa
Source organism: Homo sapiens
Expression system: Escherichia phage Ecwhy_1
UniProt:
  • Canonical: P04150 (Residues: 528-777; Coverage: 32%)
Gene names: GRL, NR3C1
Sequence domains: Ligand-binding domain of nuclear hormone receptor
Nuclear receptor coactivator 2 Chains: D, E
Molecule details ›
Chains: D, E
Length: 14 amino acids
Theoretical weight: 1.71 KDa
Source organism: Homo sapiens
Expression system: Not provided
UniProt:
  • Canonical: Q15596 (Residues: 740-753; Coverage: 1%)
Gene names: BHLHE75, NCOA2, SRC2, TIF2

Ligands and Environments

1 bound ligand:
Ligand A1ACE 2 x A1ACE
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 17-ID
Spacegroup: P21
Unit cell:
a: 38.51Å b: 141.65Å c: 47.9Å
α: 90° β: 93.46° γ: 90°
R-values:
R R work R free
0.19 0.187 0.245
Expression systems:
  • Escherichia phage Ecwhy_1
  • Not provided

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