› 2pob

X-ray diffraction
2.3Å resolution

PPARgamma Ligand binding domain complexed with a farglitazar analogue gw4709

Released:
DOI: 10.2210/pdb2pob/pdb
PDB 2pob coloured by chain and viewed from the front.
PDB 2pob coloured by chain and viewed from the side.
PDB 2pob coloured by chain and viewed from the top.
Source organism: Homo sapiens
Primary publication:
Co-crystal structure guided array synthesis of PPARgamma inverse agonists.
Trump RP, Cobb JE, Shearer BG, Lambert MH, Nolte RT, Willson TM, Buckholz RG, Zhao SM, Leesnitzer LM, Iannone MA, Pearce KH, Billin AN, Hoekstra WJ
Bioorg. Med. Chem. Lett. 17 3916-20 (2007)
PMID: 17533125

Function and Biology Details

Biochemical function:
Biological process:
Cellular component:
Sequence domains:
Structure domain:

Structure analysis Details

Assembly composition:
homo dimer (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Peroxisome proliferator-activated receptor gamma Chains: A, B
Molecule details ›
Chains: A, B
Length: 272 amino acids
Theoretical weight: 31.09 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P37231 (Residues: 234-505; Coverage: 54%)
Gene names: NR1C3, PPARG
Sequence domains: Ligand-binding domain of nuclear hormone receptor
Structure domains: Retinoid X Receptor

Ligands and Environments

2 bound ligands:
Ligand GW4 1 x GW4
Ligand GOL 1 x GOL
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 17-ID
Spacegroup: C2
Unit cell:
a: 92.916Å b: 62.006Å c: 118.172Å
α: 90° β: 101.94° γ: 90°
R-values:
R R work R free
0.226 0.224 0.273
Expression system: Escherichia coli

Quick links

Citations

2 review citations

The PPAR Ω Pocket: Renewed Opportunities for Drug Development.
Kaupang et al. (2020)
1 more