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

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.

SUBMITTER: Bertolacci L 

PROVIDER: S-EPMC3562592 | biostudies-literature | 2013 Jan

REPOSITORIES: biostudies-literature