4.7 Article

Rapid on-line profiling of estrogen receptor binding metabolites of tamoxifen

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JOURNAL OF MEDICINAL CHEMISTRY
卷 49, 期 11, 页码 3287-3292

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AMER CHEMICAL SOC
DOI: 10.1021/jm0507936

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Here we present a high-resolution screening (HRS) methodology for postcolumn on-line profiling of metabolites with affinity for the estrogen receptor alpha ( ER alpha). Tamoxifen, which is metabolized into multiple metabolites, was used as the model compound. Most of the 14 metabolites detected exhibited affinity for the ER alpha. The HRS methodology shows great potential for metabolite bio-affinity profiling and application in drug discovery and development.

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