Drug Discov Ther. 2011;5(4):176-180. (DOI: 10.5582/ddt.2011.v5.4.176)
GW501516 acts as an efficient PPARα activator in the mouse liver.
Terada M, Araki M, Ashibe B, Motojima K
SUMMARY
The peroxisome proliferator-activated receptor (PPAR) subtype specificity of GW501516, a well-known PPARδ-specific agonist, was studied by examining its effects on the expression of endogenous genes in primary hepatocytes and the liver of wild-type and PPARα-null mice. GW501516, like the PPARα-specific agonist Wy14,643, induced the expression of several PPAR target genes in a dose-dependent manner but this action was mostly absent in the cells and liver of PPARα-null mice. Results indicated that GW501516 acts as an efficient PPARα activator in the mouse liver.
KEYWORDS: Peroxisome proliferator-activated receptor (PPAR), GW501516, subtype specificity, lipid metabolism