Rheumatology Unit, Department of Medicine, Karolinska Institutet, Stockholm, Sweden.
Basic Clin Pharmacol Toxicol. 2014 Jan;114(1):64-9. doi: 10.1111/bcpt.12162. Epub 2013 Nov 11.
Microsomal prostaglandin E synthase-1 (mPGES-1) is an inducible terminal synthase in PGE2 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.
微粒体前列腺素 E 合酶-1（mPGES-1）是炎症细胞和癌细胞中 PGE2 生物合成的诱导性终端合成酶。临床和实验数据强调，与传统的 NSAIDs 或选择性 COX-2 抑制剂相比，mPGES-1 可能是一种有价值的靶点，在治疗炎症性疾病、不同类型的癌症以及外周炎症引起的中枢症状方面，具有更好的选择性和安全性。自 mPGES-1 的首次表征以来，有关 mPGES-1 结构、发病作用和抑制剂开发的出版物数量呈指数级增长；然而，目前尚无临床可用的选择性 mPGES-1 抑制剂。在这篇 MiniReview 中，我们重点介绍了选择性 mPGES-1 活性抑制剂的最新进展，旨在讨论在体外和体内不同炎症模型中靶向 mPGES-1 的效果。
