Inhibitors of diacylglycerol lipases in neurodegenerative and metabolic disorders

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• 作者：Freek J. Janssen ; Mario van der Stelt ; ^{m.van.der.stelt@chem.leidenuniv.nl" class="auth_mail" title="E-mail the corresponding author}
• 关键词：2-AG ; 2-arachidonoylglycerol ; ABPP ; activity-based protein profiling ; ABHD6 and ABHD12 ; α/β-hydrolase domain proteins 6 and 12 ; CB1R and CB2R ; cannabinoid receptors type 1 and 2 ; DAGLs ; sn-1 specific diacylglycerol lipases α and β ; FAAH ; fatty acid amide hydrolase ; MAGL ; monoacylglycerol lipase
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 August 2016
• 年：2016
• 卷：26
• 期：16
• 页码：3831-3837
• 全文大小：497 K

文摘

2-Arachidonoylglycerol (2-AG) is an endocannabinoid that activates the cannabinoid receptors type 1 and 2. It also serves as an important lipid precursor for the eicosanoid signaling pathway. Consequently, 2-AG is involved in many physiological functions, including anxiety, food intake, inflammation, memory, pain sensation and neurotransmission. Diacylglycerol lipases (DAGLs) are the main biosynthetic enzymes for 2-AG and their role in several pathophysiological conditions is currently under investigation. In this Digest we review all DAGL inhibitors reported to date and their effects in preclinical models of neurodegeneration and metabolic disorders.