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Title: Activity of a tamoxifen-raloxifene hybrid ligand for estrogen receptors at an AP-1 site. Author: Weatherman RV, Carroll DC, Scanlan TS. Journal: Bioorg Med Chem Lett; 2001 Dec 17; 11(24):3129-31. PubMed ID: 11720858. Abstract: To test the effect of ligand flexibility on the selective transcriptional activities of ERalpha and ERbeta from an AP-1 site, an analogue of raloxifene was made that removed the ketone functionality and made the ligand more planar and conformationally more similar to 4-hydroxytamoxifen. Desketoraloxifene was found to be a much stronger activator at an AP-1 site with ERalpha than with ERbeta, mimicking 4-hydroxytamoxifen more than raloxifene.[Abstract] [Full Text] [Related] [New Search]