› 2fvj

X-ray diffraction
1.99Å resolution

A novel anti-adipogenic partial agonist of peroxisome proliferator-activated receptor-gamma (PPARG) recruits pparg-coactivator-1 alpha (PGC1A) but potentiates insulin signaling in vitro

Released:
DOI: 10.2210/pdb2fvj/pdb
PDB entry 2fvj coloured by chain, front view.
PDB entry 2fvj coloured by chain, side view.
PDB entry 2fvj coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
A novel partial agonist of peroxisome proliferator-activated receptor-gamma (PPARgamma) recruits PPARgamma-coactivator-1alpha, prevents triglyceride accumulation, and potentiates insulin signaling in vitro.
Burgermeister E, Schnoebelen A, Flament A, Benz J, Stihle M, Gsell B, Rufer A, Ruf A, Kuhn B, Märki HP, Mizrahi J, Sebokova E, Niesor E, Meyer M
Mol Endocrinol 20 809-30 (2006)
PMID: 16373399

Function and Biology Details

Reaction catalysed: 
Acetyl-CoA + [protein]-L-lysine = CoA + [protein]-N(6)-acetyl-L-lysine
Biochemical function:
Biological process:
Cellular component:
Sequence domains:
Structure domain:

Structure analysis Details

Assembly composition:
hetero dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-153375 (preferred)
Entry contents:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Peroxisome proliferator-activated receptor gamma Chain: A
Molecule details ›
Chain: A
Length: 271 amino acids
Theoretical weight: 31 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P37231 (Residues: 235-505; Coverage: 54%)
Gene names: NR1C3, PPARG
Sequence domains: Ligand-binding domain of nuclear hormone receptor
Structure domains: Retinoid X Receptor
Nuclear receptor coactivator 1 Chain: B
Molecule details ›
Chain: B
Length: 13 amino acids
Theoretical weight: 1.47 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: Q15788 (Residues: 628-640; Coverage: 1%)
Gene names: BHLHE74, NCOA1, SRC1

Ligands and Environments

2 bound ligands:
Ligand RO0 1 x RO0
Ligand GOL 1 x GOL
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SLS BEAMLINE X06SA
Spacegroup: P212121
Unit cell:
a: 53.483Å b: 65.897Å c: 87.538Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.192 0.189 0.246
Expression system: Escherichia coli

Quick links

Citations

14 review citations

PPARgamma and its ligands: therapeutic implications in cardiovascular disease.
Villacorta et al. (2009)
13 more

12 mentions without citation

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