› 1zeo

X-ray diffraction
2.5Å resolution

Crystal Structure of Human PPAR-gamma Ligand Binding Domain Complexed with an Alpha-Aryloxyphenylacetic Acid Agonist

Released:
DOI: 10.2210/pdb1zeo/pdb
PDB entry 1zeo coloured by chain, front view.
PDB entry 1zeo coloured by chain, side view.
PDB entry 1zeo coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Design and synthesis of alpha-aryloxyphenylacetic acid derivatives: a novel class of PPARalpha/gamma dual agonists with potent antihyperglycemic and lipid modulating activity.
Shi GQ, Dropinski JF, McKeever BM, Xu S, Becker JW, Berger JP, MacNaul KL, Elbrecht A, Zhou G, Doebber TW, Wang P, Chao YS, Forrest M, Heck JV, Moller DE, Jones AB
J Med Chem 48 4457-68 (2005)
PMID: 15974597

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: 277 amino acids
Theoretical weight: 31.59 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P37231 (Residues: 230-505; Coverage: 55%)
Gene names: NR1C3, PPARG
Sequence domains: Ligand-binding domain of nuclear hormone receptor
Structure domains: Retinoid X Receptor

Ligands and Environments

1 bound ligand:
Ligand C01 1 x C01
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU FR-D
Spacegroup: C2
Unit cell:
a: 92.573Å b: 61.442Å c: 118.051Å
α: 90° β: 101.72° γ: 90°
R-values:
R R work R free
0.222 0.219 0.28
Expression system: Escherichia coli BL21(DE3)

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Citations

4 review citations

Drug therapy of the metabolic syndrome: minimizing the emerging crisis in polypharmacy.
Grundy SM. (2006)
3 more

25 mentions without citation

An overview on medicinal perspective of thiazolidine-2,4-dione: A remarkable scaffold in the treatment of type 2 diabetes.
Bansal et al. (2020)
24 more