Assay of Monoacylglycerol Lipase Activity. 2023

Kwang-Mook Jung, and Daniele Piomelli
Department of Anatomy and Neurobiology, University of California, Irvine, Irvine, CA, USA.

Monoacylglycerol lipase (MGL/MAGL/MGLL) is a serine hydrolase involved in the biological deactivation of the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG). 2-AG is the most abundant endogenous lipid agonists for cannabinoid receptors in the brain and elsewhere in the body. In the central nervous system (CNS), MGL is localized to presynaptic nerve terminals of both excitatory and inhibitory synapses, where it controls the regulatory actions of 2-AG on synaptic transmission and plasticity. In this chapter, we describe an in vitro method to assess MGL activity by liquid chromatography/mass spectrometry (LC/MS)-based quantitation of its reaction product. The method may be used to determine basal or altered MGL activity in cells or tissues after pharmacological, genetic, or biological interventions. In addition, the assay can be used for MGL inhibitor screening using purified recombinant enzyme or MGL-overexpressing cells.

UI MeSH Term Description Entries
D008994 Monoacylglycerol Lipases An enzyme that catalyzes the hydrolysis of glycerol monoesters of long-chain fatty acids EC 3.1.1.23. Glycerol Monoester Hydrolase,Glycerol Monoester Hydrolases,Monoacylglycerol Lipase,Monoglyceride Esterase,Monoglyceride Esterases,Monoglyceride Lipase,Monoglyceride Lipases,Monoglyceride Hydrolase,Esterase, Monoglyceride,Esterases, Monoglyceride,Hydrolase, Glycerol Monoester,Hydrolase, Monoglyceride,Hydrolases, Glycerol Monoester,Lipase, Monoacylglycerol,Lipase, Monoglyceride,Lipases, Monoacylglycerol,Lipases, Monoglyceride,Monoester Hydrolase, Glycerol,Monoester Hydrolases, Glycerol
D005990 Glycerol A trihydroxy sugar alcohol that is an intermediate in carbohydrate and lipid metabolism. It is used as a solvent, emollient, pharmaceutical agent, or sweetening agent. 1,2,3-Propanetriol,Glycerin,1,2,3-Trihydroxypropane,Glycerine
D001095 Arachidonic Acids Eicosatetraenoic Acids,Acids, Arachidonic,Acids, Eicosatetraenoic
D012694 Serine A non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from GLYCINE or THREONINE. It is involved in the biosynthesis of PURINES; PYRIMIDINES; and other amino acids. L-Serine,L Serine
D043882 Receptors, Cannabinoid A class of G-protein-coupled receptors that are specific for CANNABINOIDS such as those derived from CANNABIS. They also bind a structurally distinct class of endogenous factors referred to as ENDOCANNABINOIDS. The receptor class may play a role in modulating the release of signaling molecules such as NEUROTRANSMITTERS and CYTOKINES. Cannabinoid Receptor,Cannabinoid Receptors,Receptor, Cannabinoid
D063388 Endocannabinoids Fatty acid derivatives that have specificity for CANNABINOID RECEPTORS. They are structurally distinct from CANNABINOIDS and were originally discovered as a group of endogenous CANNABINOID RECEPTOR AGONISTS. Endocannabinoid

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