| Title : S-Arachidonoyl-2-thioglycerol synthesis and use for fluorimetric and colorimetric assays of monoacylglycerol lipase - Casida_2010_Bioorg.Med.Chem_18_1942 |
| Author(s) : Casida JE , Gulevich AG , Sarpong R , Bunnelle EM |
| Ref : Bioorganic & Medicinal Chemistry , 18 :1942 , 2010 |
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Abstract :
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. |
| PubMedSearch : Casida_2010_Bioorg.Med.Chem_18_1942 |
| PubMedID: 20138526 |
| Substrate | Arachidonoyl-1-thioglycerol |
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 Chemistry
18 :1942
Casida JE, Gulevich AG, Sarpong R, Bunnelle EM (2010)
Bioorganic & Medicinal Chemistry
18 :1942