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Abstract

Nuclear receptors are ligand-activated transcription factors, which represent a primary class of drug targets. The nuclear receptor peroxisome proliferator-activated receptor gamma (PPARgamma) is a key player in various biological processes. PPARgamma is widely known as the target protein of the thiazolidinediones for treating type 2 diabetes. Moreover, PPARgamma ligands can induce anti-inflammatory and potentially additional beneficial effects. Recent mechanistic insights of PPARgamma modulation give hope the next generation of efficient PPARgamma-based drugs with fewer side effects can be developed. Furthermore, chemical approaches that make use of synergistic action of combinatorial ligands are promising alternatives for providing tailored medicine. Lessons learned from fine-tuning the action of PPARgamma can provide avenues for efficient molecular intervention via many other nuclear receptors to combat common diseases.