› 3vso

X-ray diffraction
2Å resolution

Human PPAR gamma ligand binding domain in complex with a gamma selective agonist mekt21

Released:
DOI: 10.2210/pdb3vso/pdb
PDB entry 3vso coloured by chain, front view.
PDB entry 3vso coloured by chain, side view.
PDB entry 3vso coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Design and synthesis of a series of α-benzyl phenylpropanoic acid-type peroxisome proliferator-activated receptor (PPAR) gamma partial agonists with improved aqueous solubility.
Ohashi M, Oyama T, Putranto EW, Waku T, Nobusada H, Kataoka K, Matsuno K, Yashiro M, Morikawa K, Huh NH, Miyachi H
Bioorg Med Chem 21 2319-2332 (2013)
PMID: 23490155

Function and Biology Details

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

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: 286 amino acids
Theoretical weight: 32.53 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P37231 (Residues: 223-504; Coverage: 56%)
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 EK1 1 x EK1
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SPRING-8 BEAMLINE BL38B1
Spacegroup: C2
Unit cell:
a: 93.346Å b: 61.706Å c: 118.984Å
α: 90° β: 102.79° γ: 90°
R-values:
R R work R free
0.221 0.219 0.257
Expression system: Escherichia coli

Quick links

Citations

6 review citations

A new dawn for the use of thiazolidinediones in cancer therapy.
Joshi et al. (2014)
5 more

8 mentions without citation

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