Troglitazone

Troglitazone is a potent antiproliferative and apoptosis inducer and is a selective PPARγ agonist. There was no activation of PPARα and PPARδ observed at concentrations up to 10 µM. Troglitazone binds to the PPARγ ligand-binding domain (LBD) but fails to induce interaction of the PPARγ LBD with the transcriptional coactivators SRC-1, TIF2, AIB1, p300, or TRAP220. PPARγ is mainly expressed in adipose tissue, one of the target tissues for insulin, but has subsequently been found to be expressed in vascular smooth muscle cells, endothelial cells, macrophages, and some cancer cells. Troglitazone also induces cell cycle arrest and apoptosis in several cancer cell lines with an EC50 of 10 µM