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A binding site for nonsteroidal anti-inflammatory drugs in fatty acid amide hydrolase.

  • Author(s): Bertolacci, Laura
  • Romeo, Elisa
  • Veronesi, Marina
  • Magotti, Paola
  • Albani, Clara
  • Dionisi, Mauro
  • Lambruschini, Chiara
  • Scarpelli, Rita
  • Cavalli, Andrea
  • De Vivo, Marco
  • Piomelli, Daniele
  • Garau, Gianpiero
  • et al.

Published Web Location

https://doi.org/10.1021/ja308733uCreative Commons 'BY' version 4.0 license
Abstract

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.

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