Herein we describe the evaluation of GW0742 analogs in respect to their ability to modulate transcription mediated by the vitamin D receptor (VDR) and the peroxisome proliferator activated receptor (PPAR) δ. The GW0742 analog bearing a carboxylic ester functionality in place of the carboxylic acid was partially activating both nuclear receptors at low concentration and inhibited transcription a...

peraxisome prolifrator-activated receptors (ppars) are a group of nuclear receptors comprising three isoforms termed alpha, beta/delta and gamma. ppars can modulate metabolic processes especially fatty acid (fa) metabolisms via exerting transcriptional control on activating genes involved in fuel utilization. thus, they can exert positive role in controlling chronic diseases such as diabetes. a...

PPARgamma and PPARdelta agonists represent unique classes of drugs that act through their ability to modulate gene transcription associated with intermediary metabolism, differentiation, tumor suppression, and in some instances proliferation and cell adhesion. PPARgamma agonists are used by millions of people each year to treat type 2 diabetes but may also find additional utility as relatively ...

Peroxisome proliferator-activated receptors (PPARs) are involved in the control of carbohydrate and lipid metabolism and are considered important targets to treat diabetes mellitus and metabolic syndrome. The available PPAR ligands have several side effects leading to health risks justifying the search for new bioactive ligands to activate the PPAR subtypes, in special PPARδ, the less studied P...

14 days had no beneficial effects (Figure 1), and may have caused muscle fatigue. In fact, the control group showed a trend toward better performance, suggesting that long-term injection of AICAR may have bi-directional effects on cognition, similar to exercise (Akerström and Pedersen, 2007). These results are supported by finding that short-term AICAR treatment promoted sirtuin 1 protein expre...