Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling

…, KH Pearce, CA Simmons, J Shearin

Index: Hoekstra, William J.; Patel, Hari S.; Liang, Xi; Blanc, Jean-Baptiste E.; Heyer, Dennis O.; Willson, Timothy M.; Iannone, Marie A.; Kadwell, Sue H.; Miller, Lisa A.; Pearce, Kenneth H.; Simmons, Catherine A.; Shearin, Jean Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 2243 - 2247

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Citation Number: 26

Abstract

Traditional approaches to discovery of selective estrogen receptor modulators (SERMs) have relied on ER binding and cell-based estrogen response element-driven assays to identify compounds that are osteoprotective but nonproliferative in breast and uterine tissues. To discover new classes of potential SERMs, we have employed a cell-free microsphere-based binding assay to rapidly characterize ERα interactions with ...