Paper Report for: Casida_2010_Bioorg.Med.Chem_18_1942
Reference
Title: S-Arachidonoyl-2-thioglycerol synthesis and use for fluorimetric and colorimetric assays of monoacylglycerol lipase Casida JE, Gulevich AG, Sarpong R, Bunnelle EM Ref: Bioorganic & Medicinal Chemistry, 18:1942, 2010 : PubMed
We report the first synthesis of 2-thioglycerol and S-arachidonoyl-2-thioglycerol (the thioester analog of the endocannabinoid 2-arachidonoylglycerol) in an eight or nine step procedure with a yield of approximately 25% and establish the use of this substrate for maleimide-based fluorescent and dithiobis(2-nitrobenzoic acid)-based colorimetric assays of human recombinant monoacylglycerol (MAG) lipase (hMAGL) and human brain membrane MAG hydrolase activity. Inhibitor structure-activity relationships observed here for hMAGL and 2-ATG correlate well (r(2)=0.93, n=9) with earlier findings for mouse brain MAG hydrolase with non-thiol substrates.
        
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Casida JE, Gulevich AG, Sarpong R, Bunnelle EM (2010) S-Arachidonoyl-2-thioglycerol synthesis and use for fluorimetric and colorimetric assays of monoacylglycerol lipase Bioorganic & Medicinal Chemistry18: 1942-7
Casida JE, Gulevich AG, Sarpong R, Bunnelle EM (2010) Bioorganic & Medicinal Chemistry18: 1942-7