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微粒体前列腺素E2合酶:比环氧化酶更安全的靶点?

Microsomal prostaglandin E2 synthase: a safer target than cyclooxygenases?

作者信息

Timmers Leo, Pasterkamp Gerard, de Kleijn Dominique P V

机构信息

Laboratory of Experimental Cardiology, University Medical Center Utrecht, the Netherlands.

出版信息

Mol Interv. 2007 Aug;7(4):195-9, 180. doi: 10.1124/mi.7.4.5.

Abstract

Non-steroidal anti-inflammatory drugs (NSAIDs) are inhibitors of the cyclo-oxygenase (COX)-1 and -2 activities of prostaglandin G/H synthase-1 and -2, respectively. They have been extensively used in the treatment of prostaglandin E(2)-mediated chronic inflammatory diseases. Selective COX-2 inhibitors (coxibs), which were developed to provide an alternative with reduced gastrointestinal risk for the traditional NSAIDs, have been associated with an increased incidence of major adverse cardiovascular events. Could the targeting of microsomal prostaglandin E(2) synthase (mPGES-1) lead to novel anti-inflammatory drugs with possibly reduced risks of gastrointestinal and cardiovascular side effects?

摘要

非甾体抗炎药(NSAIDs)分别是前列腺素G/H合酶-1和-2的环氧化酶(COX)-1和-2活性的抑制剂。它们已被广泛用于治疗前列腺素E2介导的慢性炎症性疾病。选择性COX-2抑制剂(coxibs)的研发旨在为传统NSAIDs提供一种胃肠道风险降低的替代药物,但却与主要不良心血管事件的发生率增加有关。靶向微粒体前列腺素E2合酶(mPGES-1)能否产生胃肠道和心血管副作用风险可能降低的新型抗炎药物呢?

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