Monoacylglycerol lipase inhibitors: modulators for lipid metabolism in cancer malignancy,neurological and metabolic disorders
Monoacylglycerol lipase inhibitors: modulators for lipid metabolism in cancer malignancy,neurological and metabolic disorders
复制标题
DOI：
10.1016/j.apsb.2019.10.006
复制
发表时间：
2020
影响因子：
14.5
通讯作者：
Li Weimin
中科院分区：
文献类型：
--
作者：
Deng Hui;Li Weimin
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.
