Inhibitors of diacylglycerol lipases in neurodegenerative and metabolic disorders

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:26

Article

Janssen, Freek J.¹  van der Stelt, Mario¹ 

[1] Leiden Univ, Leiden Inst Chem, Dept Mol Physiol, POB 9502, NL-2300 RA Leiden, Netherlands

关键词: Diacylglycerol lipases;    2-Arachidonoylglycerol;    Neurodegenerative diseases;    Neuroinflammation;    Obesity;    Metabolic syndrome;    Drug development;   

DOI  :  10.1016/j.bmcl.2016.06.076

来源: Elsevier

【 摘 要 】

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. (C) 2016 Elsevier Ltd. All rights reserved.

【 授权许可】

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