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.
基金
supported by the National Natural Science Foundation of China(No.21807076)
the Sichuan Natural Science Foundation,China(No.2019YJ0112).
作者简介
Corresponding author:Hui Deng,Tel./fax:t862885422197.E-mail addresses:huideng0923@hotmail.com;Corresponding author:Weimin Li,weimin003@163.com
