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1: Bioorg Med Chem Lett. 2008 Nov 15;18(22):5838-41. Epub 2008 Jul 2.Click here to read Links

Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling.

Hoover HS, Blankman JL, Niessen S, Cravatt BF.

The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037, USA.

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.

PMID: 18657971 [PubMed - indexed for MEDLINE]

PMCID: PMC2634297 [Available on 2009/11/15]

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