Advances in the development of covalent small molecule inhibitors of monoacylglycerol lipase.

Author: Junlai WANG ¹ ; Sen LIU ¹
Author Information

1. Cooperative Innovation Center of Industrial Fermentation (Ministry of Education & Hubei Province), Hubei University of Technology, Wuhan 430068, Hubei, China.
Publication Type:Journal Article
Keywords: covalent binding; covalent inhibitor; monoacylglycerol lipase; targeting inhibition; treatment of cancer
MeSH: Monoacylglycerol Lipases/metabolism*; Endocannabinoids/metabolism*
From: Chinese Journal of Biotechnology 2023;39(11):4397-4412
CountryChina
Language:Chinese
Abstract: Monoacylglycerol lipase (MGL) is a serine hydrolase that plays a major role in the degradation of endogenous cannabinoid 2-arachidonoylglycerol. The role of MGL in some cancer cells has been confirmed, where inhibition of the MGL activity shows inhibition on cell proliferation. This makes MGL a promising drug target for the treatment of cancer. Recently, the development of covalent inhibitors of MGL has developed rapidly. These drugs have strong covalent binding ability, high affinity, long duration, low dose and low risk of drug resistance, so they have received increasing attention. This article introduces the structure and function of MGL, the characteristics, mechanisms and progress of covalent MGL inhibitors, providing reference for the development of novel covalent small molecule inhibitors of MGL.