Background

PPARG regulates fatty acid storage and glucose metabolism. Many insulin sensitizing drugs used in the treatment of diabetes target PPARG as a means to lower serum glucose without increasing pancreatic insulin secretion. The genes activated by PPARG stimulate lipid uptake and adipogenesis by fat cells. PPARG knockout mice fail to generate adipose tissue when fed a high fat diet.

Protein Classification

transcription

Structure Weight

34246.95 Da

Polymer

1

Molecule

Peroxisome proliferator-activated receptor gamma

Chain Length

296 amino acids

PDB ID

3BC5

MMDB ID

67970

Source

E.coli

Method

X-Ray Diffraction

Resolution

2.27Å

Ligand Chemical Component

ZAA

Gene Name

PPARG

Synonyms

CIMT1; NR1C3; PPARG1; PPARG2; PPAR-gamma; HUMPPARG; OTTHUMP00000185030; OTTHUMP00000185033; OTTHUMP00000185037; PPAR gamma; nuclear receptor subfamily 1 group C member 3; peroxisome proliferative activated receptor gamma; peroxisome proliferator-activated receptor gamma 1; nuclear receptor subfamily 1 group C member 3

UniProt ID

P37231

Gene ID

5468

Chromosome Location

3p25

Function

arachidonic acid binding; drug binding; metal ion binding; prostaglandin receptor activity; protein heterodimerization activity; retinoid X receptor binding; steroid hormone receptor activity; zinc ion binding

Reference

Zhang, H., Ryono, D.E., Devasthale, P., Wang, W., O`Malley, K., Farrelly, D., Gu, L., Harrity, T., Cap, M., Chu, C., Locke, K., Zhang, L., Lippy, J., Kunselman, L., Morgan, N., Flynn, N., Moore, L., Hosagrahara, V., Zhang, L., Kadiyala, P., Xu, C., Doweyko, A.M., Bell, A., Chang, C., Muckelbauer, J., Zahler, R., Hariharan, N., Cheng, P.T. (2009) Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists. Bioorg