• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Journal of the American Chemical Society >A Binding Site for Nonsteroidal Anti-inflammatory Drugs in Fatty Acid Amide Hydrolase
【24h】

A Binding Site for Nonsteroidal Anti-inflammatory Drugs in Fatty Acid Amide Hydrolase

机译：脂肪酸酰胺水解酶中非甾体类抗炎药的结合位点

获取原文
获取原文并翻译 | 示例
       
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

In addition to inhibiting the cyclooxygenase (COX)-mediated biosynthesis of prostanoids, various widely used nonsteroidal anti-inflammatory drugs (NSAIDs) enhance endocannabinoid signaling by blocking the anandamide-degrading membrane enzyme fatty acid amide hydrolase (FAAH). The X-ray structure of FAAH in complex with the NSAID carprofen, along with site-directed mutagenesis, enzyme activity assays, and NMR analysis, has revealed the molecular details of this interaction, providing information that may guide the design of dual FAAH-COX inhibitors with superior analgesic efficacy.
机译：除了抑制环加氧酶（COX）介导的前列腺素的生物合成外，各种广泛使用的非甾体抗炎药（NSAID）还可以通过阻断降解腺苷酰胺的膜酶脂肪酸酰胺水解酶（FAAH）来增强内源性大麻素信号传导。 FAAH与NSAID卡洛芬复合的X射线结构，以及定点诱变，酶活性测定和NMR分析，揭示了这种相互作用的分子细节，为指导双FAAH-COX的设计提供了信息具有优异的镇痛作用的抑制剂。

著录项

  • 来源
    《Journal of the American Chemical Society》 |2013年第1期|22-25|共4页
  • 作者

    Laura Bertolacci; Elisa Romeo; Marina Veronesi; Paola Magotti; Clara Albani; Mauro Dionisi; Chiara Lambruschini; Rita Scarpelli; Andrea Cavalli; Marco De Vivo; Daniele Piomelli; Gianpiero Garau;

  • 作者单位

    Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy;

    Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy;

    Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy;

    Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy;

    Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy;

    Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy;

    Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy;

    Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy;

    Department of Pharmaceutical Sciences, University of Bologna, 40126 Bologna, Italy;

    Department of Pharmaceutical Sciences, University of Bologna, 40126 Bologna, Italy;

    Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy,Department of Pharmacology, University of California, Irvine, California 92697, United States;

    Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy;

  • 收录信息 美国《科学引文索引》(SCI);美国《工程索引》(EI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

  • 入库时间 2022-08-18 03:12:27

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号