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The First Potent Inhibitor of Mammalian Group X Secreted Phospholipase A(2): Elucidation of Sites for Enhanced Binding

Using the X-ray structure of human group X secreted phospholipase A(2) (hGX), we carried out structure-based design of indole-based inhibitors and prepared the compounds using a new synthetic route. The most potent compound inhibited hGX and the mouse orthologue with an IC(50) of 75 nM. This compoun...

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Autores principales: Smart, Brian P., Oslund, Rob C., Walsh, Laura A., Gelb, Michael H.
Formato: Artigo
Lenguaje:Inglês
Publicado: 2006
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Acceso en línea:https://ncbi.nlm.nih.gov/pmc/articles/PMC2963729/
https://ncbi.nlm.nih.gov/pubmed/16686528
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm060136t
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