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  • Title: Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling.
    Author: Hoekstra WJ, Patel HS, Liang X, Blanc JB, Heyer DO, Willson TM, Iannone MA, Kadwell SH, Miller LA, Pearce KH, Simmons CA, Shearin J.
    Journal: J Med Chem; 2005 Mar 24; 48(6):2243-7. PubMed ID: 15771467.
    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 ERalpha interactions with conformation-sensing cofactor or phage display peptides. Peptide profiles of constrained triarenes were compared to known proliferative and nonproliferative ER ligands to discover potent quinoline-based ligands with minimal Ishikawa cell stimulation.
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