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      New Diclofenac Derivatives as Anti-Microbial, Anti-Inflammatory Agents: Design, Synthesis, Biological Screening, and Molecular Docking Study

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          The effects of surgical exposures of dental pulps in germ-free and conventional laboratory rats

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            Carrageenin-Induced Edema in Hind Paw of the Rat as an Assay for Antiinflammatory Drugs

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              Crystal structure of rofecoxib bound to human cyclooxygenase-2.

              Rofecoxib (Vioxx) was one of the first selective cyclooxygenase-2 (COX-2) inhibitors (coxibs) to be approved for use in humans. Within five years after its release to the public, Vioxx was withdrawn from the market owing to the adverse cardiovascular effects of the drug. Despite the widespread knowledge of the development and withdrawal of Vioxx, relatively little is known at the molecular level about how the inhibitor binds to COX-2. Vioxx is unique in that the inhibitor contains a methyl sulfone moiety in place of the sulfonamide moiety found in other coxibs such as celecoxib and valdecoxib. Here, new crystallization conditions were identified that allowed the structural determination of human COX-2 in complex with Vioxx and the structure was subsequently determined to 2.7 Å resolution. The crystal structure provides the first atomic level details of the binding of Vioxx to COX-2. As anticipated, Vioxx binds with its methyl sulfone moiety located in the side pocket of the cyclooxygenase channel, providing support for the isoform selectivity of this drug.
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                Author and article information

                Journal
                Russian Journal of Bioorganic Chemistry
                Russ J Bioorg Chem
                Pleiades Publishing Ltd
                1068-1620
                1608-330X
                January 2021
                March 20 2021
                January 2021
                : 47
                : 1
                : 208-220
                Article
                10.1134/S1068162021010088
                90c496be-74fe-417d-b2b4-64bc76316ef8
                © 2021

                http://www.springer.com/tdm

                http://www.springer.com/tdm

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