Sonia E. Step, Hee-Woong Lim, Jill M. Marinis
May 1, 2014
Citations
4
Influential Citations
88
Citations
Quality indicators
Journal
Genes & Development
Abstract
Rosiglitazone (rosi) is a powerful insulin sensitizer, but serious toxicities have curtailed its widespread clinical use. Rosi functions as a high-affinity ligand for PPARγ, the adipocyte-predominant nuclear receptor. Here, Lazar and colleagues investigate the direct effects of rosi on gene transcription. The authors delineate a novel mechanism by which rosi represses adipocyte gene transcription at endogenous levels of PPARγ and other transcription factors on a genome-wide scale. This study suggests that rosi activates and represses transcription by fundamentally different mechanisms that could inform anti-diabetic drug development.