title: Aspirin metabolites are GPR35 agonists.
abstract: Aspirin is widely used as an anti-inflammatory, anti-platelet, anti-pyretic, and cancer-preventive agent; however, the molecular mode of action is unlikely due entirely to the inhibition of cyclooxygenases. Here, we report the agonist activity of several aspirin metabolites at GPR35, a poorly characterized orphan G protein-coupled receptor. 2,3,5-Trihydroxybenzoic acid, an aspirin catabolite, was found to be the most potent GPR35 agonist among aspirin metabolites. Salicyluric acid, the main metabolite of aspirin, was also active. These results suggest that the GPR35 agonist activity of certain aspirin metabolites may contribute to the clinical features of aspirin.
authors.affiliation: Biochemical Technologies, Science and Technology Division, Corning Inc, Corning, NY 14831, USA.
authors.forename: Huayun
authors.initials: H
authors.lastname: Deng
authors.forename: Ye
authors.initials: Y
authors.lastname: Fang
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000378:metabolism; D058633:Antipyretics / Q000378:metabolism; D001241:Aspirin / Q000378:metabolism*; D005343:Fibrinolytic Agents / Q000378:metabolism; D005707:Gallic Acid / Q000031:analogs & derivatives / Q000494:pharmacology; D005841:Gentisates / Q000494:pharmacology*; D019073:HT29 Cells; D006626:Hippurates / Q000494:pharmacology*; D006801:Humans; D043562:Receptors, G-Protein-Coupled / Q000819:agonists*
chemical_list: C533199:2,3,5-trihydroxybenzoic acid; D000894:Anti-Inflammatory Agents, Non-Steroidal; D058633:Antipyretics; D005343:Fibrinolytic Agents; C111379:GPR35 protein, human; D005841:Gentisates; D006626:Hippurates; D043562:Receptors, G-Protein-Coupled; C016471:gentisuric acid; C000693:salicylurate; D005707:Gallic Acid; D001241:Aspirin