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Characterization of Microsomal Prostaglandin E Synthase 1 Inhibitors
Author(s) -
Korotkova Marina,
Jakobsson PerJohan
Publication year - 2014
Publication title -
basic and clinical pharmacology and toxicology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.805
H-Index - 90
eISSN - 1742-7843
pISSN - 1742-7835
DOI - 10.1111/bcpt.12162
Subject(s) - atp synthase , in vivo , prostaglandin , in vitro , microsome , inflammation , prostaglandin e , enzyme , pharmacology , prostaglandin e2 , chemistry , medicine , biochemistry , biology , immunology , microbiology and biotechnology
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 .