6ktn

X-ray diffraction
2.75Å resolution

Human PPARgamma ligand-binding domain R288A mutant in complex with imatinib

Released:
Source organism: Homo sapiens
Primary publication:
Structural Basis for the Regulation of PPARγ Activity by Imatinib.
Molecules 24 (2019)
PMID: 31581474

Function and Biology Details

Structure analysis Details

Assembly composition:
hetero dimer (preferred)
Entry contents:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Peroxisome proliferator-activated receptor gamma Chain: A
Molecule details ›
Chain: A
Length: 283 amino acids
Theoretical weight: 32.19 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P37231 (Residues: 223-505; Coverage: 56%)
Gene names: NR1C3, PPARG
Nuclear receptor coactivator 1 Chain: B
Molecule details ›
Chain: B
Length: 16 amino acids
Theoretical weight: 1.91 KDa
Source organism: Homo sapiens
Expression system: Not provided
UniProt:
  • Canonical: Q15788 (Residues: 685-700; Coverage: 1%)
Gene names: BHLHE74, NCOA1, SRC1

Ligands and Environments

1 bound ligand:
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: PHOTON FACTORY BEAMLINE AR-NE3A
Spacegroup: P21212
Unit cell:
a: 130.928Å b: 52.779Å c: 53.438Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.222 0.22 0.256
Expression systems:
  • Escherichia coli BL21(DE3)
  • Not provided