Targeting inflammation: multiple innovative ways to reduce prostaglandin E₂.
Targeting inflammation: multiple innovative ways to reduce prostaglandin E₂.
复制标题
DOI：
10.4155/ppa.12.90
复制
发表时间：
2013-03
影响因子：
1.3
通讯作者：
Meuillet EJ
中科院分区：
文献类型：
--
作者：
Norberg JK;Sells E;Chang HH;Alla SR;Zhang S;Meuillet EJ
PGE 2通路在炎症驱动的疾病中是重要的，并且由于与长期使用考克斯-2抑制剂相关的心血管问题，需要诱导型mPGES-1的特异性靶向。本文综述了mPGES-1活性测定方法、靶向mPGES-1的药物和其他细胞外游离PGE 2浓度调节剂的专利。还提出了关于这些药物的地位的观点和结论。重要的是，尚未发现靶向mPGES-1的选择性抑制剂，尽管已发表的专利数量很高，但这些药物尚未进入临床试验。
The PGE2 pathway is important in inflammation-driven diseases and specific targeting of the inducible mPGES-1 is warranted due to the cardiovascular problems associated with the long-term use of COX-2 inhibitors. This review focuses on patents issued on methods of measuring mPGES-1 activity, on drugs targeting mPGES-1 and on other modulators of free extracellular PGE2 concentration. Perspectives and conclusions regarding the status of these drugs are also presented. Importantly, no selective inhibitors targeting mPGES-1 have been identified and, despite the high number of published patents, none of these drugs have yet made it to clinical trials.