PPAR𝜶 Ligands as Antitumorigenic and Antiangiogenic Agents

Table 1

Effect of PPARα activation on angiogenesis and tumorigenesis.

Ligand	Cell type	Effect	Target	Reference
WY14643	Endothelial cells	Inhibition of cell proliferation and tubulogenesis in vitro Antiangiogenic activity in vivo	Downregulation of arachidonate epoxygenase synthesis	[38]
WY14643	Endothelial cells	Enhanced endothelial tube formation in vitro Proangiogenic activity in vivo	Upregulation of VEGF production	[37]
Fenofibrate WY14643 ETYA	Endothelial cells	Inhibition of VEGF- or FGF2-mediated cell proliferation in vitro Antiangiogenic activity in vivo	Downregulation of VEGF production Upregulation of thrombospondin and endostatin production	[48]
Fenofibrate WY14643	Endothelial cells	Reduced cell migration	Inhibition of Akt activation	[24]
Fenofibrate	Endothelial cells	Reduced cell proliferation	Inhibition of cyclooxygenase-2 expression	[25]
Fenofibrate	Endothelial cells	Reduced cell proliferation	Inhibition of VEGFR2 expression	[23]
Clofibrate	Ovarian cancer cells	Reduced cell proliferation in vitro Antitumorigenic activity in vivo	Reduced prostanoid and VEGF levels via upregulation of carbonyl reductase expression	[49]
Methylclofenapate	Colonic adenocarcinoma	Reduced cell proliferation	Not investigated	[50]
Methylclofenapate	Apc^Min/+ mice	Reduced number of intestinal polyps	Not investigated	[50]
Bezafibrate	APC^1309mice Apc^Min/+ mice	Reduced number of intestinal polyps	Reduced serum level of triglycerides and increased lipoprotein lipase synthesis	[27, 51]
WY14643	Wild-type mice	Enhanced hepatocellular proliferation and tumorigenesis in vivo	Downregulation of the miRNA let-7C with increased c-myc expression	[52]