› 2pob

X-ray diffraction
2.3Å resolution

PPARgamma Ligand binding domain complexed with a farglitazar analogue gw4709

Released:
DOI: 10.2210/pdb2pob/pdb
PDB entry 2pob coloured by chain, front view.
PDB entry 2pob coloured by chain, side view.
PDB entry 2pob coloured by chain, top view.
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)
Assembly name:
PDBe Complex ID:
PDB-CPX-153379 (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

1 review citation

The PPAR Ω Pocket: Renewed Opportunities for Drug Development.
Kaupang et al. (2020)
4 other articles

4 mentions without citation

Review of the Structural and Dynamic Mechanisms of PPARγ Partial Agonism.
Kroker et al. (2015)
3 more