期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 22, 页码 5838-5841出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.06.091
关键词
Activity-based proteomics; Biosynthesis; Endocannabinoid; Inhibitor; Lipase
资金
- NIH [DA017259, DA025285]
- Helen L. Dorris Institute
- Skaggs Institute for Chemical Biology
The endocannabinoid 2- arachidonoylglycerol (2- AG) has been implicated as a key retrograde mediator in the nervous system based on pharmacological studies using inhibitors of the 2- AG biosynthetic enzymes diacyglycerol lipase alpha and beta (DAGL-alpha/beta). Here, we show by competitive activity-based protein profiling that the DAGL-alpha/beta inhibitors, tetrahydrolipstatin (THL) and RHC80267, block several brain serine hydrolases with potencies equal to or greater than their inhibitory activity against DAGL enzymes. Interestingly, a minimal overlap in target profiles was observed for THL and RHC80267, suggesting that pharmacological effects observed with both agents may be viewed as good initial evidence for DAGL-dependent events. (C) 2008 Elsevier Ltd. All rights reserved.
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