Conservative Secondary Shell Substitution In Cyclooxygenase-2 Reduces Inhibition by Indomethacin Amides and Esters via Altered Enzyme Dynamics

[Image: see text] The cyclooxygenase enzymes (COX-1 and COX-2) are the therapeutic targets of nonsteroidal anti-inflammatory drugs (NSAIDs). Neutralization of the carboxylic acid moiety of the NSAID indomethacin to an ester or amide functionality confers COX-2 selectivity, but the molecular basis fo...

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Detalles Bibliográficos
Autores principales: Konkle, Mary E., Blobaum, Anna L., Moth, Christopher W., Prusakiewicz, Jeffery J., Xu, Shu, Ghebreselasie, Kebreab, Akingbade, Dapo, Jacobs, Aaron T., Rouzer, Carol A., Lybrand, Terry P., Marnett, Lawrence J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2015
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4721528/
https://www.ncbi.nlm.nih.gov/pubmed/26704937
http://dx.doi.org/10.1021/acs.biochem.5b01222

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