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首页> 外文期刊>RSC Advances >Chemistry and biology of microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors as novel anti-inflammatory agents: recent developments and current status
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Chemistry and biology of microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors as novel anti-inflammatory agents: recent developments and current status

机译：微粒体前列腺素E2合成酶-1（MPGES-1）抑制剂作为新型抗炎剂的化学和生物学：最近的发展和现状

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摘要

Prostaglandin (PG) E _(2) , a key mediator of inflammatory pain and fever, is biosynthesized from PGH _(2) by microsomal prostaglandin E _(2) synthase-1 (mPGES-1). During inflammation the expression of mPGES-1 increases resulting in increased PGE _(2) formation. Specific inhibition of mPGES-1 reduces the biosynthesis of PGE _(2) , sparing other physiologically important PGs such as prostacyclin (PGI _(2) ) and thromboxane A _(2) (TXA _(2) ). Inhibition of mPGES-1 might be superior over the inhibition of cyclooxygenases (COX), as the latter leads to the suppression of PGI _(2) , TXA _(2) along with the pathogenic PGE _(2) resulting in gastro-intestinal, renal and cardiovascular complications. Therefore, inhibition of mPGES-1 has been proposed as a promising approach for the development of drugs for inflammation and pain therapy, which only suppresses PGE _(2) biosynthesis, avoiding the side effects caused by nonsteroidal anti-inflammatory drugs (NSAIDs) and specific COX-2 inhibitors. The current review article includes natural and synthetic inhibitors of mPGES-1 reported since 2000 with their in vitro activity (IC _(50) values), in vivo activity, the status of clinical candidates, and critical appraisal of these reported inhibitors.
机译：前列腺素（PG）E _（2），炎症疼痛和发烧的关键介质，由微粒体前列腺素E _（2）合成酶-1（MPGES-1）生物合成。在炎症期间，MPGES-1的表达增加导致增加的PGE _（2）形成。 MPGES-1的特异性抑制减少了PGE _（2）的生物合成，使得其他生理学上重要的PG，例如前列环素（PGI _（2））和血栓素A _（2））（TXA _（2））。 MPGES-1的抑制可以在抑制环氧氢酶（COX）上优异，因为后者导致PGI _（2），TXA _（2）的抑制以及导致胃肠的致病性PGE _（2）。 ，肾和心血管并发症。因此，已经提出了对MPGES-1的抑制作为发育炎症和疼痛治疗的药物的有希望的方法，该方法仅抑制PGE _（2）生物合成，避免由非甾体类抗炎药（NSAID）和的副作用特定的COX-2抑制剂。目前的审查制品包括自2000年以来报告的MPGES-1的天然和合成抑制剂，其体外活性（IC _（50）值），体内活动，临床候选者的状况以及这些报告的抑制剂的批判性评估。

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