期刊
CURRENT MEDICINAL CHEMISTRY
卷 25, 期 21, 页码 2418-2447出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/0929867325666180117103919
关键词
Cytosolic phospholipase A2 alpha; inflammation; anti-inflammatory; cPLA2 alpha inhibitors; structure-activity relationship; arachidonic acid
资金
- Belgian Fund for Scientific Research (FRS-FNRS) [34553.08]
- FER (ULB)
- Department of International Relationship (BRIC)
Group IV cytosolic phospholipase A2 (cPLA2 alpha) plays a critical role in inflammatory processes. It produces arachidonic acid which is the main source of the pro-inflammatory eicosanoids mediators that are important in innate immune system. In some cases, these proinflammatory mediators cause damages to the host tissues and therefore promote autoimmune diseases. Consequently, development of potent inhibitors against cPLA2 alpha could improve the therapy of inflammatory diseases. In the last two decades, intense efforts have been done to find potent cPLA2 alpha inhibitors. Several scaffolds have been developed with the use of structure-activity relationship (SAR) studies, and potent inhibitors have been obtained. The poor absorption of these compounds from intestine was the main challenge for clinical application. This review illustrates the search for cPLA2 alpha inhibitors, their SAR studies and biological effects.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据