针对mPGES-1小分子抑制剂的筛选体系的建立文献综述

利用分子对接技术验证mPGES-1抑制剂的活性张雨霏摘要：前列腺素E2（PGE2）是人体内调节各种生理和病理过程的重要物质，与炎症，癌症，发热，疼痛相关。

微粒体前列腺素E2合成酶（mPGES-1）是谷胱甘肽（GSH）依赖性的诱导型酶，诱导PGE2的生成。

mPGES-1靶点位于炎症通路下游，可以直接抑制mPGES-1从而减少PGE2的产生。

而目前常用的非甾体类抗炎药（NSAIDs），由于同时抑制COX-1/2的病理生理表达，产生了严重的胃肠道和心血管副作用，选择性mPGES-1抑制剂可以减少PGE2的合成，不影响其他前列腺素（PGs）和血栓素（TX），提高特异性，减少副作用。

近十年来，科学家们一直致力于研究mPGES-1，提出mPGES-1可以作为炎症治疗的新靶点。

然而选择性mPGES-1抑制剂在临床尚且没有应用，关于mPGES-1的研究也十分稀少。

本文就近十年研究和mPGES-1蛋白结构及其分子对接技术做一综述。

关键词：mPGES-1；炎症；分子对接Abstract： Prostaglandin E2 (PGE2) is a significant substance in human body for that it regulates a variety of physiological and pathological processes, for example, inflammation, cancer, fever and pain. Microsomal prostaglandin E2 synthase (mPGES-1) is glutathione (GSH) dependent and enzymatic induction. Target mPGES-1 is in the pathways of PGE2-induced inflammatory downstream, directly inhibiting mPGES-1 can reduce the production of PGE2. Currently common used non-steroidal anti-inflammatory drugs (NSAIDs) inhibit the expression of pathophysiological and physical COX-1/2, resulting in a serious sideeffects about gastrointestinal tract and angiocarpy. Selective mPGES-1 inhibitors can reduce the synthesis of PGE2, and does not affect other prostaglandins (PGs) and thromboxane (TX), improving the specificity and reducing the side effects. In the past ten years, scientists have been dedicated to study the mechanism of mPGES-1, proposing that mPGES-1 --- a new target can be used as the treatment of inflammation. However, selective mPGES-1 inhibitors have no research clinically and have rare research about it. The ten years of research and the structure of mPGES-1 protein and its molecular docking technology are reviewed in this paper.Keyword：mPGES-1 inflammation molecular docking technology炎症是困扰人们健康的最大问题，长期的炎症反应导致炎症因子诱发癌症。

目前，治疗炎症的药物大多是非甾体抗炎药物（NSAIDs），其可分为两类，非特异性NSAIDs和特异性COX-2抑制剂。