Characterization of Microsomal Prostaglandin E Synthase 1 Inhibitors

Microsomal prostaglandin E synthase‐1 (m PGES ‐1) is an inducible terminal synthase in PGE 2 biosynthesis by inflammatory and cancer cells. Clinical and experimental data emphasize that m PGES ‐1 might be a valuable target, with improved selectivity and safety compared to traditional NSAID s or selective COX ‐2 inhibitors, in the treatment of inflammatory diseases, different types of cancer as well as central symptoms elicited by peripheral inflammation. Since the first characterization of m PGES ‐1, the numbers of publications on m PGES ‐1 structure, pathogenic role and inhibitor development have increased exponentially; however, there are currently no selective m PGES ‐1 inhibitors available for clinical use. In this M ini R eview, we focus on recent advances in the development of selective inhibitors of m PGES ‐1 activity, with the aim to discuss the effects of targeting m PGES ‐1 in different inflammatory models in vitro and in vivo .