title: Controlling 2-arachidonoylglycerol metabolism as an anti-inflammatory strategy.
abstract: The endocannabinoid system is implicated in, and regulates, several physiological processes, ranging from food intake and energy balance to pain and inflammation. 2-Arachidonoylglycerol (2-AG) is a full agonist at the cannabinoid receptors which classically mediate its effects. The activity of this bioactive lipid is dependent on its endogenous levels, which are tightly controlled by several hydrolases, monoacylglycerol lipase and α/β-hydrolase domain 6 and 12. Moreover, 2-AG is also a substrate of cyclooxygenase-2, and this reaction leads to the formation of prostaglandin glycerol esters, the effects of which remain to be fully elucidated. In this review we discuss the multiple mechanisms by which 2-AG controls inflammation and the therapeutic potential of 2-AG metabolism inhibitors.
authors.affiliation: Bioanalysis and Pharmacology of Bioactive Lipids Research Group, Louvain Drug Research Institute, Université catholique de Louvain, Av. E. Mounier 72, B1.72.01, B-1200 Bruxelles, Belgium; Medicinal Chemistry Research Group, Louvain Drug Research Institute, Université catholique de Louvain, Av. E. Mounier 73, B1.73.10, B-1200 Bruxelles, Belgium.
authors.forename: Mireille
authors.initials: M
authors.lastname: Alhouayek
authors.affiliation: Bioanalysis and Pharmacology of Bioactive Lipids Research Group, Louvain Drug Research Institute, Université catholique de Louvain, Av. E. Mounier 72, B1.72.01, B-1200 Bruxelles, Belgium.
authors.forename: Julien
authors.initials: J
authors.lastname: Masquelier
authors.affiliation: Bioanalysis and Pharmacology of Bioactive Lipids Research Group, Louvain Drug Research Institute, Université catholique de Louvain, Av. E. Mounier 72, B1.72.01, B-1200 Bruxelles, Belgium. Electronic address: giulio.muccioli@uclouvain.be.
authors.forename: Giulio G
authors.initials: GG
authors.lastname: Muccioli
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D001095:Arachidonic Acids / Q000378:metabolism*; D051546:Cyclooxygenase 2 / Q000378:metabolism; D015195:Drug Design; D063388:Endocannabinoids / Q000378:metabolism*; D004952:Esters / Q000378:metabolism; D005989:Glycerides / Q000378:metabolism*; D006801:Humans; D007249:Inflammation / Q000188:drug therapy* / Q000503:physiopathology; D011453:Prostaglandins / Q000378:metabolism; D043882:Receptors, Cannabinoid / Q000378:metabolism
chemical_list: D000893:Anti-Inflammatory Agents; D001095:Arachidonic Acids; D063388:Endocannabinoids; D004952:Esters; D005989:Glycerides; D011453:Prostaglandins; D043882:Receptors, Cannabinoid; C094503:glyceryl 2-arachidonate; D051546:Cyclooxygenase 2