Monoacylglycerol lipase inhibitors: modulators for lipid metabolism in cancer malignancy,neurological and metabolic disorders

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外文摘要：Monoacylglycerol lipase (MAGL) is a serine hydrolase that plays a crucial role catalysing the hydrolysis of monoglycerides into glycerol and fatty acids.It links the endocannabinoid and eicosanoid systems together by degradation of the abundant endocannabinoid 2-arachidaoylglycerol into arachidonic acid,the precursor of prostaglandins and other inflammatory mediators.MAGL inhibitors have been considered as important agents in many therapeutic fields,including anti-nociceptive,anxiolytic,antiinflammatory,and even anti-cancer.Currently,ABX-1431,a first-in-class inhibitor of MAGL,is entering clinical phase 2 studies for neurological disorders and other diseases.This review summarizes the diverse (patho)physiological roles of MAGL and will provide an overview on the development of MAGL inhibitors.Although a large number of MAGL inhibitors have been reported,novel inhibitors are still required,particularly reversible ones.

外文关键词：

Monoacylglycerol lipases2-ArachidaoylglycerolArachidonic acidDrug discoveryCancerNeuroinflammationMetabolic syndrome

作者：

Hui Deng、Weimin Li

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作者单位：

Precision Medicine Key Laboratory of Sichuan Province & Precision Medicine Center, West China Hospital,Sichuan University, Chengdu 610041, China

基金：

This work was supported by the National Natural Science Foundation of ChinaSichuan Natural Science Foundation,China

项目编号：

218070762019YJ0112

出版年：

2020

药学学报(英文版)

CSTPCDCSCDSCI

ISSN：

年,卷(期)：2020.10(4)

被引量8
参考文献量113