S-二十二碳烯酰基-2-硫代甘油的合成及其在单酰基甘油脂肪酶荧光法和比色法测定中的应用。
S-Arachidonoyl-2-thioglycerol synthesis and use for fluorimetric and colorimetric assays of monoacylglycerol lipase.
机构信息
Department of Nutritional Sciences and Toxicology, University of California, Berkeley, CA 94720, USA.
出版信息
Bioorg Med Chem. 2010 Mar 1;18(5):1942-7. doi: 10.1016/j.bmc.2010.01.034. Epub 2010 Jan 18.
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.
我们报告了 2-硫代甘油和 S-花生四烯酰-2-硫代甘油（内源性大麻素 2-花生四烯酰甘油的硫代酯类似物）的首次合成，该合成过程包括八到九个步骤，收率约为 25%，并建立了该底物在马来酰亚胺基荧光和二硫代双（2-硝基苯甲酸）比色测定法中的应用，用于检测人重组单酰基甘油脂肪酶（hMAGL）和人脑组织 MAG 水解酶活性。在此观察到的 hMAGL 和 2-ATG 的抑制剂结构活性关系与以前使用非硫醇底物的鼠脑 MAG 水解酶的发现非常吻合（r(2)=0.93，n=9）。
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