mPGES-1 as a target for cancer suppression: A comprehensive invited review "Phospholipase A2 and lipid mediators".
mPGES-1 as a target for cancer suppression: A comprehensive invited review "Phospholipase A2 and lipid mediators".
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DOI：
10.1016/j.biochi.2010.02.006
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发表时间：
2010-06
期刊：
影响因子：
3.9
通讯作者：
Rosenberg, Daniel W.
中科院分区：
文献类型：
--
作者：
Nakanishi, Masako;Gokhale, Vijay;Meuillet, Emmanuelle J.;Rosenberg, Daniel W.
前列腺素 E2 (PGE2) 是一种生物活性脂质，可引发与炎症和癌症相关的多种生物效应。 PGE2 的生理作用是多种多样的，部分是通过位于细胞表面的跨膜 EP 受体激活关键的下游信号级联来介导的。人类癌症中经常发现 COX-2 水平升高以及随之而来的 PGE2 过量产生。这些观察结果导致使用非甾体抗炎药（NSAID）作为化学预防剂，特别是对于结直肠癌（CRC）。然而，长期使用它们可能与胃肠道毒性和不良心血管事件风险增加有关，从而促进该途径中其他酶靶标的开发。本综述将重点关注最近针对末端合酶 mPGES-1 进行癌症化学预防的努力。讨论了 mPGES-1 在各种癌症发病机制中的作用。此外，还概述了最近开发高选择性靶向蛋白质的小分子抑制剂的努力。
Prostaglandin E2 (PGE2) is a bioactive lipid that can elicit a wide range of biological effects associated with inflammation and cancer. The physiological roles of PGE2 are diverse, mediated in part through activation of key downstream signaling cascades via transmembrane EP receptors located on the cell surface. Elevated levels of COX-2 and concomitant overproduction of PGE2 are often found in human cancers. These observations have led to the use of non-steroidal anti-inflammatory drugs (NSAIDs) as chemopreventive agents, particularly for colorectal cancer (CRC). Their long-term use, however, may be associated with gastrointestinal toxicity and increased risk of adverse cardiovascular events, prompting the development of other enzymatic targets in this pathway. This review will focus on recent efforts to target the terminal synthase, mPGES-1, for cancer chemoprevention. The role of mPGES-1 in the pathogenesis of various cancers is discussed. In addition, an overview of recent efforts to develop small molecule inhibitors that target the protein with high selectivity is also be reviewed.
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影响因子：
5.8
作者：
Herfs, Michael;Herman, Ludivine;Delvenne, Philippe
通讯作者：
Delvenne, Philippe
DOI：
10.1073/pnas.96.13.7220
发表时间：
1999-06-22
影响因子：
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作者：
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作者：
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通讯作者：
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影响因子：
168.9
作者：
Baron, John A.;Sandler, Robert S.;DeMets, David L.
通讯作者：
DeMets, David L.