› 1pcg

X-ray diffraction
2.7Å resolution

Helix-stabilized cyclic peptides as selective inhibitors of steroid receptor-coactivator interactions

Released:
DOI: 10.2210/pdb1pcg/pdb
PDB entry 1pcg coloured by chain, front view.
PDB entry 1pcg coloured by chain, side view.
PDB entry 1pcg coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Helix-stabilized cyclic peptides as selective inhibitors of steroid receptor-coactivator interactions.
Leduc AM, Trent JO, Wittliff JL, Bramlett KS, Briggs SL, Chirgadze NY, Wang Y, Burris TP, Spatola AF
Proc Natl Acad Sci U S A 100 11273-8 (2003)
PMID: 13679575

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-136923 (preferred)
Entry contents:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Estrogen receptor Chains: A, B
Molecule details ›
Chains: A, B
Length: 244 amino acids
Theoretical weight: 27.82 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P03372 (Residues: 304-547; Coverage: 41%)
Gene names: ESR, ESR1, NR3A1
Sequence domains: Ligand-binding domain of nuclear hormone receptor
Structure domains: Retinoid X Receptor
peptide inhibitor Chains: E, F
Molecule details ›
Chains: E, F
Length: 9 amino acids
Theoretical weight: 1.09 KDa
Source organism: Homo sapiens
Expression system: Not provided

Ligands and Environments

1 bound ligand:
Ligand EST 2 x EST
1 modified residue:
Ligand DCY 2 x DCY

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 17-BM
Spacegroup: C2221
Unit cell:
a: 53.809Å b: 102.432Å c: 195.326Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.219 0.219 0.254
Expression systems:
  • Escherichia coli BL21(DE3)
  • Not provided

Quick links

Citations

28 review citations

Estrogen receptors: how do they signal and what are their targets.
Heldring et al. (2007)
27 more

9 mentions without citation

Structure-Based Design of Inhibitors of Protein-Protein Interactions: Mimicking Peptide Binding Epitopes.
Pelay-Gimeno et al. (2015)
8 more