Journal
BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY
Volume 114, Issue 1, Pages 64-69Publisher
WILEY
DOI: 10.1111/bcpt.12162
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Funding
- The Swedish Research Council
- The Swedish Rheumatism Association
- King Gustaf V 80 years Foundation
- The Swedish Society of Medicine
- Karolinska Institutet Foundation
- The Swedish County Council
- Marianne and Marcus Wallenberg foundation
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Microsomal prostaglandin E synthase-1 (mPGES-1) is an inducible terminal synthase in PGE(2) biosynthesis by inflammatory and cancer cells. Clinical and experimental data emphasize that mPGES-1 might be a valuable target, with improved selectivity and safety compared to traditional NSAIDs 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 mPGES-1, the numbers of publications on mPGES-1 structure, pathogenic role and inhibitor development have increased exponentially; however, there are currently no selective mPGES-1 inhibitors available for clinical use. In this MiniReview, we focus on recent advances in the development of selective inhibitors of mPGES-1 activity, with the aim to discuss the effects of targeting mPGES-1 in different inflammatory models in vitro and in vivo.
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