Article
Oxicams bind in a novel mode to the cyclooxygenase active site via a two-water-mediated H-bonding Network.
The Journal of biological chemistry - 7 Mar 2014
Xu Shu, Hermanson Daniel J, Banerjee Surajit, Ghebreselasie Kebreab, Clayton Gina M, Garavito R Michael, Marnett Lawrence J
Abstract excerpt
Oxicams are widely used nonsteroidal anti-inflammatory drugs (NSAIDs), but little is known about the molecular basis of the interaction with their target enzymes, the cyclooxygenases (COX). Isoxicam is a nonselective inhibitor of COX-1 and COX-2 whereas meloxicam displays some selectivity for COX-2. Here we report crystal complexes of COX-2 with isoxicam and meloxicam at 2.0 and 2.45 angstroms, respectively, and...
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