Identification and development of mPGES-1 inhibitors: where we are at?
Identification and development of mPGES-1 inhibitors: where we are at?
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DOI：
10.4155/fmc.11.136
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发表时间：
2011-11
影响因子：
4.2
通讯作者：
Meuillet EJ
中科院分区：
文献类型：
--
作者：
Chang HH;Meuillet EJ
微粒体前列腺素E合酶-1（mPGES-1）是负责合成促肿瘤性前列腺素E2（PGE 2）的末端合酶。mPGES-1在多种癌症中过表达。自1997年由Bengt Samuelsson及其合作者发现以来，该酶已成为200多篇同行评议文章的对象。虽然今天mPGES-1被认为是一个验证和有前途的抗癌药物发现的治疗靶点，抑制剂设计和选择性的挑战是这样的，到目前为止，只有少数发表的记录小分子抑制剂靶向酶，并表现出一些体内抗癌活性。本文综述了这些新型mPGES-1抑制剂的结构及其体内外活性。还讨论了遇到的挑战。
Microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal synthase responsible for the synthesis of the pro-tumorigenic prostaglandin E2 (PGE2). 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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