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Microsomal prostaglandin E2 synthase-1 and its inhibitors: Molecular mechanisms and therapeutic significance.

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资源类型：
Pubmed体系：
作者：
Zhang Yan-Yu[1,2] * ; Yao Yun-Da[1,2] ; Luo Jin-Fang[3] ; Liu Zhong-Qiu[4] ; Huang Yu-Ming[5] ; Wu Fei-Chi[5] ; Sun Qin-Hua[6] ; Liu Jian-Xin[7] ; Zhou Hua[1,2,4,8,*1] ;
机构： [1]Faculty of Chinese Medicine and State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Taipa, Macao, PR China [2]Joint Laboratory for Translational Cancer Research of Chinese Medicine of the Ministry of Education of the People’s Republic of China, Macau University of Science and [3]Guizhou University of Traditional Chinese Medicine, Huaxi District, Guiyang City, Guizhou Province 550025, PR China [4]Joint Laboratory for Translational Cancer Research of Chinese Medicine of the Ministry of Education of the People’s Republic of China, Guangzhou University of [5]Hunan Zhengqing Pharmaceutical Company Group Ltd, Huaihua City, Hunan Province, PR China [6]School of Pharmaceutical Sciences, Hunan University of Medicine, Huaihua City, Hunan Province 418000, PR China [7]School of Public Health, Zhejiang Chinese Medical University, Hangzhou City, Zhejiang Province 310053, PR China [8]Zhuhai Hospital of Integrated Traditional Chinese and Western Medicine, Zhuhai City, Guangdong Province 519000, PR China
出处：
DOI： 10.1016/j.phrs.2021.105977
ISSN：

关键词： MPGES-1 Phospholipid metabolism MPGES-1 inhibitor PGE2 COX-2 Inflammatory disease

摘要：
Inflammation is closely linked to the abnormal phospholipid metabolism chain of cyclooxygenase-2/microsomal prostaglandin E2 synthase-1/prostaglandin E2 (COX-2/mPGES-1/PGE2). In clinical practice, non-steroidal anti-inflammatory drugs (NSAIDs) as upstream COX-2 enzyme activity inhibitors are widely used to block COX-2 cascade to relieve inflammatory response. However, NSAIDs could also cause cardiovascular and gastrointestinal side effects due to its inhibition on other prostaglandins generation. To avoid this, targeting downstream mPGES-1 instead of upstream COX is preferable to selectively block overexpressed PGE2 in inflammatory diseases. Some mPGES-1 inhibitor candidates including synthetic compounds, natural products and existing anti-inflammatory drugs have been proved to be effective in in vitro experiments. After 20 years of in-depth research on mPGES-1 and its inhibitors, ISC 27864 have completed phase II clinical trial. In this review, we intend to summarize mPGES-1 inhibitors focused on their inhibitory specificity with perspectives for future drug development.Copyright © 2021 Elsevier Ltd. All rights reserved.

基金：
This research was funded by the Science and Technology Development Fund, Macao SAR (File no.: 0027/2017/AMJ, 0001/2020/AKP), the National Key Research and Development Program of China (Project No.: 2017YFE0119900), 2020 Hunan Province Science and Technology Innovation Key Projects (Project No.: 2020SK1020), the Joint Research Fund for Overseas Chinese, Hong Kong and Macao Young Scholars of National Science Foundation of China (Project No.: 81929003, 81628016), the National Science Foundation of China for Young Scientist (Project No.: 82803811), and the Science Foundation for Young Scientist of Hunan Province, China (Project No.: 82803811)
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2020]版：
大类 | 2 区 医学
小类 | 2 区 药学
最新[2025]版：
大类 | 2 区 医学
小类 | 1 区 药学
第一作者：
第一作者机构： [1]Faculty of Chinese Medicine and State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Taipa, Macao, PR China [2]Joint Laboratory for Translational Cancer Research of Chinese Medicine of the Ministry of Education of the People’s Republic of China, Macau University of Science and
通讯作者：
通讯机构： [1]Faculty of Chinese Medicine and State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Taipa, Macao, PR China [2]Joint Laboratory for Translational Cancer Research of Chinese Medicine of the Ministry of Education of the People’s Republic of China, Macau University of Science and [4]Joint Laboratory for Translational Cancer Research of Chinese Medicine of the Ministry of Education of the People’s Republic of China, Guangzhou University of [8]Zhuhai Hospital of Integrated Traditional Chinese and Western Medicine, Zhuhai City, Guangdong Province 519000, PR China [*1]Faculty of Chinese Medicine and State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Taipa, Macao, PR China
推荐引用方式(GB/T 7714)：
Zhang Yan-Yu,Yao Yun-Da,Luo Jin-Fang,et al.Microsomal prostaglandin E2 synthase-1 and its inhibitors: Molecular mechanisms and therapeutic significance.[J].Pharmacological research.2021,175:105977.doi:10.1016/j.phrs.2021.105977.
APA：
Zhang Yan-Yu,Yao Yun-Da,Luo Jin-Fang,Liu Zhong-Qiu,Huang Yu-Ming...&Zhou Hua.(2021).Microsomal prostaglandin E2 synthase-1 and its inhibitors: Molecular mechanisms and therapeutic significance..Pharmacological research,175,
MLA：
Zhang Yan-Yu,et al."Microsomal prostaglandin E2 synthase-1 and its inhibitors: Molecular mechanisms and therapeutic significance.".Pharmacological research 175.(2021):105977

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