A high-throughput-compatible assay for determining the activity of fatty acid amide hydrolase

被引：27

作者：

Wilson, SJ ^{[1
]}

Lovenberg, TW ^{[1
]}

Barbier, AJ ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC Neuros, San Diego, CA 92121 USA

来源：

ANALYTICAL BIOCHEMISTRY | 2003年 / 318卷 / 02期

关键词：

fatty acid amide hydrolase; anandamide; endocannabinoid;

D O I：

10.1016/S0003-2697(03)00217-3

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Fatty acid amide hydrolase (EC 3.5.1.4.) is the enzyme responsible for the rapid degradation of lipid-derived chemical messengers such as anandamide, oleamide, and 2-arachidonoylglycerol. The pharmacological characterization of this enzyme in vivo has been hampered by the lack of selective and bioavailable inhibitors. We have developed a simple, radioactive, high-throughput-compatible assay for this enzyme based on the differential absorption of the substrate and its products to activated charcoal. The assay was validated using known inhibitors. It may be applied for the identification of new inhibitors from a compound library. (C) 2003 Elsevier Science (USA). All rights reserved.

引用

页码：270 / 275

页数：6

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