Deng Hui, van der Stelt Mario
Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Leiden, The Netherlands.
Biotechnol Appl Biochem. 2018 Jan;65(1):9-15. doi: 10.1002/bab.1568. Epub 2017 Aug 2.
2-Arachidonoylglycerol (2-AG) is an important endogenous signaling lipid that activates the cannabinoid receptors (CB R and CB 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.
2-花生四烯酸甘油酯（2-AG）是一种重要的内源性信号脂质，可激活大麻素受体（CB1R和CB2R），从而调节包括焦虑、食欲、炎症、记忆、痛觉和伤害感受在内的多种生理过程。二酰基甘油脂肪酶（DAGLs）是负责2-AG生物合成的主要酶。最近，已通过遗传方法和化学工具探索了DAGLs的（病理）生理功能。本综述将重点关注利用基于活性的蛋白质谱分析开发高选择性和体内活性DAGLs抑制剂的最新研究成果。
