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[期刊论文]
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Identification and development of mPGES-1 inhibitors: where we are at?
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作 者：
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Hui-Hua Chang;Hui-Hua Chang;Emmanuelle J Meuillet;Emmanuelle J Meuillet;
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出版年：2011
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页 码：1909 - 1934
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出版社：Future Science, LTD
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摘 要：
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Microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal synthase responsible for the synthesis of the pro-tumorigenic prostaglandin E(2) (PGE(2)). mPGES-1 is overexpressed in a wide variety of cancers. Since its discovery in 1997 by Bengt Samuelsson and collaborators, the enzyme has been the object of over 200 peer-reviewed articles. Although today mPGES-1 is considered a validated and promising therapeutic target for anticancer drug discovery, challenges in inhibitor design and selectivity are such that up to this date there are only a few published records of small-molecule inhibitors targeting the enzyme and exhibiting some in vivo anticancer activity. This review summarizes the structures, and the in vitro and in vivo activities of these novel mPGES-1 inhibitors. Challenges that have been encountered are also discussed.
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暂无
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所属期刊
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ISSN: 1756-8919
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来自：Future Science, LTD
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