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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.

Authors :
Deng H
Li W
Source :
Acta pharmaceutica Sinica. B [Acta Pharm Sin B] 2020 Apr; Vol. 10 (4), pp. 582-602. Date of Electronic Publication: 2019 Oct 18.
Publication Year :
2020

Abstract

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, anti-inflammatory, 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.<br /> (© 2020 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.)

Details

Language :
English
ISSN :
2211-3835
Volume :
10
Issue :
4
Database :
MEDLINE
Journal :
Acta pharmaceutica Sinica. B
Publication Type :
Academic Journal
Accession number :
32322464
Full Text :
https://doi.org/10.1016/j.apsb.2019.10.006