3V9T: Crystal Structure Of The Ppargamma-Lbd Complexed With A Cercosporamide Derivative Modulator

Peroxisome proliferator-activated receptor gamma (PPARgamma) is a potential drug target for treating type 2 diabetes. The selective PPARgamma modulators (SPPARMs), which partially activate the PPARgamma transcriptional activity, are considered to improve the plasma glucose level with attenuated PPARgamma related adverse effects. However, the relationships between desired pharmacological profiles and ligand specific PPARgamma transcriptional profiles have been unclear. And there is also little knowledge of how to control ligand specific PPARgamma transcriptional profiles. Herein, we present synthesis of novel derivatives containing substituent at naphthalene C3 position of compound 1. The novel derivatives showed various maximal efficacies as PPARgamma partial agonist.
PDB ID: 3V9TDownload
MMDB ID: 96950
PDB Deposition Date: 2011/12/28
Updated in MMDB: 2012/02
Experimental Method:
x-ray diffraction
Resolution: 1.65  Å
Source Organism:
Similar Structures:
Biological Unit for 3V9T: dimeric; determined by author and by software (PISA)
Molecular Components in 3V9T
Label Count Molecule
Proteins (2 molecules)
Peroxisome Proliferator-activated Receptor Gamma(Gene symbol: PPARG)
Molecule annotation
Peptide From Peroxisome Proliferator-activated Receptor Gamma Coactivator 1-alpha(Gene symbol: PPARGC1A)
Molecule annotation
Chemical (1 molecule)
* Click molecule labels to explore molecular sequence information.

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