||Albani, C., Bertolacci, L., Cavalli, A., De Vivo, M., Dionisi, M., Garau, G., Lambruschini, C., Magotti, P., Piomelli, D., Romeo, E., Scarpelli, R., Veronesi, M.
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.
J.Am.Chem.Soc. 2013 Jan; 135(1):22-25 doi:10.1021/ja308733u