› 4ci4

X-ray diffraction
2.3Å resolution

Structural basis for GL479 a dual Peroxisome Proliferator-Activated Receptor alpha agonist

Released:
DOI: 10.2210/pdb4ci4/pdb
PDB entry 4ci4 coloured by chain, front view.
PDB entry 4ci4 coloured by chain, side view.
PDB entry 4ci4 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Different binding and recognition modes of GL479, a dual agonist of Peroxisome Proliferator-Activated Receptor α/γ.
dos Santos JC, Bernardes A, Giampietro L, Ammazzalorso A, De Filippis B, Amoroso R, Polikarpov I
J Struct Biol 191 332-40 (2015)
PMID: 26185032

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 analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-170552 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Peroxisome proliferator-activated receptor alpha Chain: A
Molecule details ›
Chain: A
Length: 274 amino acids
Theoretical weight: 31.02 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: Q07869 (Residues: 195-468; Coverage: 59%)
Gene names: NR1C1, PPAR, PPARA
Sequence domains: Ligand-binding domain of nuclear hormone receptor
Structure domains: Retinoid X Receptor

Ligands and Environments

1 bound ligand:
Ligand Y1N 1 x Y1N
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: LNLS BEAMLINE W01B-MX2
Spacegroup: P41212
Unit cell:
a: 64.526Å b: 64.526Å c: 124.387Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.217 0.215 0.258
Expression system: Escherichia coli BL21(DE3)

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Citations

2 review citations

Current Advances in the Biochemical and Physiological Aspects of the Treatment of Type 2 Diabetes Mellitus with Thiazolidinediones.
Alemán-González-Duhart et al. (2016)
1 more

5 mentions without citation

Development of Heterocyclic PPAR Ligands for Potential Therapeutic Applications.
Virendra et al. (2022)
4 more