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Chemical tools to modulate 2‐arachidonoylglycerol biosynthesis
Author(s) -
Deng Hui,
der Stelt Mario
Publication year - 2017
Publication title -
biotechnology and applied biochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 70
eISSN - 1470-8744
pISSN - 0885-4513
DOI - 10.1002/bab.1568
Subject(s) - endocannabinoid system , 2 arachidonoylglycerol , lipid signaling , cannabinoid receptor , enzyme , receptor , diacylglycerol kinase , biochemistry , diacylglycerol lipase , chemistry , biology , neuroscience , monoacylglycerol lipase , protein kinase c , agonist
2‐Arachidonoylglycerol (2‐AG) is an important endogenous signaling lipid that activates the cannabinoid receptors (CB 1 R and CB 2 R), thereby regulating a diverse range of physiological processes including anxiety, appetite, inflammation, memory, pain sensation, and nociception. Diacylglycerol lipases (DAGLs) are the principle enzymes responsible for 2‐AG biosynthesis. Recently, the (patho)physiological functions of DAGLs have been explored by both genetic methods and chemical tools. This review will focus on the recent efforts to develop highly selective and in vivo active DAGLs inhibitors using activity‐based protein profiling.